Publications from the Gestwicki Group


(194) Lee K., Thwin, A. C., Nadel, C. M., Tse, E., Gates, S. N., Gestwicki, J. E., Southworth, D. R. “Structure of an Hsp90-immunophilin complex reveals cochaperone recognition of a client maturation state” 2021 Mol. Cell. (in press).

(193) Opoku-Nsiah, K.A., de la Pena, A. H., Williams, S. K., Chopra, N., Sali, A., Lander, G. C., Gestwicki, J.E. “The Y Motif defines the structure-activity relationships of human 20S proteasome activators” 2021 Nat. Commun. (in press). 

(192) Tharp, K. M., Higuchi-Sanabria, R., Timblin, G. A., Ford, B., Garzon-Coral, C., Schneider, C., Muncie, J. M., Stashko, C., Daniele, J. R., Moore, A. S., Frankino, P. A., Manoli, S. S., Shao, H., Richards, A. L., Chen, K.-H., Ku, G. M., Hellerstein, M., Nomura, D. K., Saijo, K., Gestwicki, J. E., Dunn, A. R., Krogan, N. J., Swaney, D. L., Dillin, A., Weaver, V.M. “Adhesion-mediated mechanosignaling forces mitohormesis” 2021 Cell Metabolism 33:1322-1341. 

(191) Tao, J., Berthet, A., Citron, Y. R., Tsiolaki, P. L., Stanley, R., Gestwicki, J. E., Agard, D. A., McConlogue, L. “Hsp70 chaperone blocks -synuclein oligomer formation via a novel engagement mechanism” 2021 J. Biol. Chem. 296:100613. PMC8102405

(190) Caballero, B., Bourdenx, M., Martin, E. L., Diaz, A., Sohn, P., Chen, X., Wang, C., Juste, Y., Wegmann, S., Patel, B., Young, Z., Kuo, S. Y., Rodriguez-Navarro, J. A., Shao, H., Lopez, M., Karch, C., Goate, A., Gestwicki, J. E., Hyman, B., Gan., L., Cuervo, A. M. “Acetylated tau inhibits chaperone-mediated autophagy and promotes tau pathology propagation in mice” 2021 Nat. Commun. 12:2238. PMC8047017 

(189) Shuller, M., Correy, G. J., Gahbauer, S., Fearon, D., Wu, T. S., Diaz, R. E., Young, I. D., Martins, L. C., Smith, D. H., Schulze-Gahmen, U., Owens, T. W., Deshpande, I., Merz, G. E., Thwin, A. C., Biel, J. T., Peters, J. K., Moritz, M., Herrera, N., Kratochvil, H. T., QCRG Structural Biology Consortium, Aimon, A., Bennet, J. M., Neto, J. B., Cohen, A. E., Dias, A., Douangamath, A., Dunnett, L., Fedorov, O., Ferla, M.P., Fuchs, M., Gorrie-Stone, T. J., Holton, J. M., Johnson, M. G., Krojer, T., Meigs, G., Powell, A. J., Rack, J. G. M., Rangel, V. L., Wierman, J. L., Zhu, K., Jura, N., Ashworth, A., Irwin, J., Thompson, M. C., Gestwicki, J. E., von Delft, F., Shoichet, B. K., Fraser, J. S., Ahel, I.  “Fragment binding to the Nsp3 macrodomain of SARS-Cov-2 identified through crystallographic screening and computational docking” 2021 Science Advances 7:eabf8711. PMC8046379

(188) Shao, H., Li, X., Hayashi, S., Bertron, J., Schwarz, D. M. C., Tang, B., Gestwicki, J .E. “Inhibitors of heat shock protein 70 (Hsp70) with enhanced metabolic stability reduce tau levels” 2021 Bioorgan. Med. Chem. Lett. 41:128025. 

(187) Abrams, J.*, Arhar, T.*, Mok, S.-A., Taylor, I. R., Kampmann, M., Gestwicki, J. E. “Functional genomics screen identifies proteostasis targets that modulate prion protein (PrP) stability” 2021 Cell Stress Chaperones 26:443-452. *these authors contributed equally. PMC7925731

(186) Makley, L. N.*, Johnson, O. T.*, Ghanakota, P., Rauch, J. N., Osborn, D. Wu, T. S., Cierpicki, T., Carlson, H. A., Gestwicki, J. E. “Chemical validation of a druggable site on Hsp27/HSPB1 using in silico mapping and biophysical methods” 2021 Bioorg. Med. Chem. 34:115990. *these authors contributed equally. PMC7968374

(185) Dutta, T., Singh, H., Gestwicki, J. E., Blatch, G. L. “Exported plasmodial Hsp40, PFE0055c, and pfHsp70-x form a specific co-chaperone-chaperone partnership” 2021 Cell Stress Chaperones 26:355-366. PMC7925779




(184) Nadel, C. M., Ran, X., Gestwicki, J. E. “Luminescence complementation assay for measurement of binding to protein C-termini in live cells” 2020 Anal. Biochem. 611:113947. PMC8054679.

(183) Schwarz, D. M. C., Williams, S. K., Dillenberg, M., Wagner, C. R., Gestwicki, J. E. “A phosphoramidate strategy enables membrane permeability of a non-nucleoside inhibitor of the prolyl isomerase, Pin1” 2020 ACS Med. Chem. Lett. 11(9):1704-1710. PMC7488286. 

(182) Shao, S., Oltion, K., Wu, T., Gestwicki, J. E. “Differential scanning fluorimetry (DSF) screen to identify inhibitors of Hsp60 protein-protein interactions” 2020 Org. Biomol. Chem. 18:4157-4163. 

(181) Bengoechea, R., Findlay, A. R., Bharda, A. K., Shao, H., Stein, K. C., Pittman, S. K., Daw, J., Gestwicki, J. E., True, H. L., Weihl, C. C. “Inhibition of DNAJ-HSP70 interaction improves strength in muscular dystrophy” 2020 J. Clin. Invest. 130(8):4470-4485. PMC7410071. 

(180) Huang, Y., Zhao, N., Wang, Y.-H., Truillet, C., Wei, J., Blecha, J. E., VanBrocklin H. F., Seo, Y., Sayeed, M., Feldman, B. J., Aggarwal, R., Behr, S. C., Shao, H., Wilson, D. M., Villanueva-Meyer, J. E., Gestwicki, J. E., Evans, M. J. “A novel radioligand reveals tissue specific pharmacological modulation of glucocorticoid receptor expression with positron emission tomography” 2020 ACS Chem. Biol. 15:1381-1391.

(179) Wu, P.-K., Hong, S.-K., Starenki, D., Oshima, K., Shao, H., Gestwicki, J. E., Tsai, S., Park, J.-I. “Mortalin/HSPA9 targeting selectively induces KRAS tumor death by perturbing mitochondrial membrane permeability” 2020 Oncogene 39:4257-4270. PMC7244387.

(178) Jackson, J. W., Rivera-Marquez, G., Beebe, K., Tran, A. D., Trepel, J. B., Gestwicki, J. E., Blagg, B. S. J., Ohkubo, S., Neckers, L. M. “Pharmacologic dissection of the overlapping impact of heat shock protein family members on platelet function” 2020 J. Thromb. Haemostasis. 18:1197-1209. PMC7497839.

(177) Wu, P.-K., Hong, S.-K., Chen, W., Becker, A. E., Gundry, R. L., Lin, C.-W., Shao, H., Gestwicki, J. E., Park, J.-I. “Mortalin (HSPA9) facilitates BRAF–mutant tumor cell survival by suppressing ANT3-mediated mitochondrial membrane permeability” 2020 Science Signal. 10:622. PMC7099430.

(176) Taylor, I. R.*, Assimon, V. A.*, Kuo, S. Y.*, Rinaldi, S., Li, X., Young, Z. T., Morra, G., Green, K., Nguyen, D., Shao, H., Garneau-Tsodikova, S., Columbo, G., Gestwicki, J. E. “Tryptophan scanning mutagenesis as a way to mimic the compound-bound state and probe the selectivity of allosteric inhibitors in cells” 2020 Chem. Sci. 11:1892-1904. *these authors contributed equally. 

(175) Chen, X., Li, Y., Wang, C., Tang, Y., Mok, S.-A., Tsai, R. M., Rojas, J. C., Karydas, A., Miller, B. L., Boxer, A. L., Gestwicki, J. E., Arkin, M., Cuervo, A. M., Gan, L. “Promoting tau secretion and propagation by hyperactive p300/CBP via autophagy-lysosomal pathway in tauopathy” 2020 Mol. Neurodegen. 15:2. PMC6916486.

(174) Shao, H. and Gestwicki, J. E. “Neutral analogs of the heat shock protein 70 (Hsp70) inhibitor, JG-98” 2020 Bioorg. Med. Chem. Lett. 30:126954. PMC7205417.

(173) Singh, J., Tait, B., Hutt, D. H., Guy, N., Sivil, J. C., Culbertson, D., Dickey, C. A., Kuo, S. Y., Chadli, A., Finley, D., Dyson, J. H., Cox, M. B., Gestwicki, J. E., Balch, W. E. “Management of Hsp90-dependent protein folding by a small molecule targeting the Aha1 co-chaperone” 2020 Cell Chem. Biol. 27:292-305. PMC7144688.

(172) Ravalin, M. Basu, K., Gestwicki, J. E., Craik, C. S. “End-binding E3 ubiquitin ligases enable protease signaling” 2020 ACS Chem. Biol. (in press). PMC7400744.

(171) Wang, C., Scott, S. M., Sun, S., Zhao, P., Hutt, D. M., Shao, H., Gestwicki, J. E., Balch, W. E. “Individualized management of genetic diversity in Niemann-Pick C1 through modulation of the Hsp70 chaperone system” 2020 Hum. Mol. Genetics 29:1-19. PMC7001602.





 (170) Chen, J. J., Nathaniel, D. L., Raghavan, P., Nelson, M., Tian, R., Tse, E., Hong, J. Y., See, S. K., Mok, S.-A., Hein, M., Southworth, D., Grinberg, L. T., Gestwicki, J. E., Loenetti, M., Kampmann, M. “Compromised function of the ESCRT pathway promotes endolysosomal escape of tau seeds and propagation of tau aggregation” 2019 J. Biol. Chem. (in press). 

 (169) Sohn, P. D., Huang, C. T.-L., Yan, R., Tracy, T. E., Camargo, C. M., Montgomery, K., Arhar, T., Mok, S.-A., Freilich, R., Baik, J., He, M., Gong, S., Roberson, E. D., Karch, C. M., Gestwicki, J. E., Xu, K., Kosik, K. S., Gan., L. “Pathogenic tau impairs axon initial segment plasticity and excitability homeostasis” 2019 Neuron (in press). 

 (168) Eftekharzadh, B., Banduseela, V. C., Chiesa, G., Martinez-Cristobal, P., Rauch, J. N., Schwarz, D. M. C., Shao, H., Marin-Argany, M., Di Sanze, C., Giorgetti, E., Nath, S. R., Yu, Z., Pieratelli, R., Felli, I. C., Brun-Heath, I., Garcia, J., Nebreda, A. R., Gestwicki, J. E.*, Lieberman, A. P.*, Salvatella, X*. “Hsp70 and Hsp40 bind to the transactivation domain of the androgen receptor and inhibit an inter-domain interaction necessary for transcriptional activity” 2019 Nat. Commun. 10:3562. *co-corresponding authors. PMC6687723.

 (167) Molnar, K. S., Dunyak, B. M., Su, B., Izrayelit, Y., McGlasson-Naumann, Hamilton, P. D., Qian, M., Covey, D. F., Gestwicki, J. E., Makley, L. N., Andley, U. P. “Mechanism of action of VP1-001 in cryAB(R120G)-associated and age-related cataract” 2019 Invest. Ophthalm. Visual Sci. 60:3320-3331. PMC6676924. 

 (166) Ravalin, M., Theofilas, P., Basu, K., Opoku-Nsiah, K. A., Assimon, V. A., Medina-Cleghorn, D., Chen, Y.-F., Bohn, M. F., Arkin, M., Grinberg, L. T., Craik, C. S.*, Gestwicki, J. E.*, “Specificity for latent C-termini links E3 ubiquitin ligase CHIP to caspases” 2019 Nat. Chem. Biol. 15:786-794. PMC6693490.

 (165) Taguwa, S., Yeh, M.-T., Rainbolt, K., Nayak, A., Shao, H., Gestwicki, J. E., Andino, R., Frydman, J. “Dissection of Zika virus dependence on host Hsp70 provides a strategy protecting animal models from infection and disease” 2019 Cell Reports 26:906-920. 

 (164) Moss, S. M., Taylor, I. R., Ruggero, D., Gestwicki, J. E., Shokat, K. M., Mukherjee S. “A bacterial kinase phosphorylates the Hsp70 chaperone family to inhibit eukaryotic protein synthesis” 2019 Cell Host Microb. 25:1-9. 

 (163) Zaiter, S. S., Huo, Y., Gestwicki, J. E., McAlpine, S. R. “Designing do novo small molecules that control heat shock protein 70 (Hsp70) and heat shock organizing protein (HOP) within the chaperone protein-folding machinery” 2019 J. Med. Chem. (in press). 

 (162) Gestwicki, J. E. and Shao, H. “Inhibitors and chemical probes for molecular chaperone networks” 2019 J. Biol. Chem. 294:2151-2161. 

 (161) Lee, E., Ouzounova, M., Piranlioglu, R., Ma, M. T., Guzel, M., Marasco, D., Chadli, A., Gestwicki, J. E., Cowell, J., Wicha, M., Hassan, K., Korkaya, H. “The pleiotropic effects of TNF in breast cancer subtypes is regulated by TNFAIP3/A20” 2019 Oncogene 38:469-482.




 (160) Pabon, N. A., Xia, Y., Estabrooks, S., Ye, Z., Herbardn, A. K., Sub, E., Biondi, R. M., Assimon, V. A., Gestwicki, J. E., Brodsky, J. L., Camacho, C. J., Bar-Joseph, Z. “Predicting protein targets for drug-like compounds using transcriptomics” 2018 PLoS Comp. Biol. 14:e1006651. PMC6300300

 (159) Meister-Broekema, M.*, Freilich, R.*, Jagadeesan, C.*, Rauch, J. N.*, Bengoecha, R., Motley, W. W., Kuiper, E. F. E., Minioia, M.,m Furtado, G. V., van Waarde, M. A. W. H., Bird, S. J., Rebelo, A., Zuchner, S., Pytel, P., Scherer, S. S., Morelli, F. F., Carra, S., Weihl, C. C., Bergink, S.#, Gestwicki, J. E.#, Kampinga, H. H.# “Myopathy associated BAG3 mutations lead to protein aggregation by stalling Hsp70 networks” 2018 Nat. Commun. 9:5342. * these authors contributed equally. #co-corresponding authors. PMC6297355

 (158) Rinaldi, S., Assimon, V. A., Young, Z. T., Murra, G., Shao, H., Taylor, A. R., Gestwicki, J. E.*, Columbo, G.* “A local allosteric network in heat shock protein 70 (Hsp70) links inhibitor binding to enzyme activity and distal protein-protein interactions” 2018 ACS Chem. Biol. 13:3142-3152. * co-corresponding authors. 

 (157) Frielich, R., Betegon, M., Tse, E., Mok, S.-A., Julien, O., Agard, D. A., Southworth, D. R., Takeuchi, K., Gestwicki, J. E. “Competing protein-protein interactions regulate binding of Hsp27 to tau” 2018 Nat. Commun. 9:4563. PMC6212398.  

 (156) Shao, H.*, Li, X.*, Moses, M. A., Gilbert, L. A., Kalyanaraman, C., Young, Z. T., Chernova, M., Journey, S. N., Weissman, J. S., Hann, B., Jacobson, M. P., Neckers, L. and Gestwicki, J. E. “Exploration of benothiazole-rhodacyanines as allosteric inhibitors of protein-protein interactions with heat shock protein 70 (Hsp70)” 2018 J. Med. Chem. 61:6163-6177. *these authors contributed equally. PMC6104643.

 (155) Polson, E. S.; Kuchler, V.B.; Abbosh, C.; Ross, E. M.; Mathew, R. K.; Beard, H. A.; da Silva, B.; Holding, A. N.; Ballereau, S.; Chuntharpursat-Bon, E.; Williams, J.; Griffiths, H. B. S.; Shao, H. Patel, A.; Davies, A. J.; Droop, A.; Chumas, P.; Short, S. C.; Lorger, M.; Gestwicki, J. E.; Roberts, L. D.; Bon, R. S.; Allison, S. J.; Zhu, S.; Markowetz, F.; Wurdak, H. “KHS101 disrupts mitochondrial HSPD1 and energy metabolism in human glioblastoma cells” Sci. Trans. Med. 2018, 10:eaaar2718. 

 (154) Glazier, A. A., Hafeez, N., Mellacheruvu, D., Basrur, V., Neshvizhskii, A. I., Lee, L.M., Shao, H., Tang, V., Yob, J. M., Gestwicki, J E., Helms, A. S., Day, S.N. “Hsc70 is a chaperone for wild-type and mutant cardiac myosin binding protein C” 2018 JCI Insights 3:e99319. PMC6124431. 

 (153) Ran, X. and Gestwicki, J. E. “Inhibitors of protein-protein interactions (PPIs): An analysis of scaffold choices and buried surface area” 2018 Curr. Opin. Chem. Biol. 44:75-86. PMC6066447. 

 (152) Opoku-Nsiah, K., A. and Gestwicki, J. E. “Aim for the core: Suitability of the ubiquitin-independent 20S proteasome as a drug target in neurodegeneration” 2018 Trans. Res. 198:48-57. PMC6154511. 

 (151) Taylor, I. R., Ahmad, A., Wu, T., Nordhues, B. A., Bhullar, A., Gestwicki, J. E.*, Zuiderweg, E. R. P.* “The disorderly conduct of Hsc70 and its interaction with the Alzheimer’s related tau protein” 2018 J. Biol. Chem. 293:10796-10809. *co-corresponding authors. PMC6036187.

 (150) Moses, M. A., Kim, Y. S., Rivera-Marquez, G. M., Oshima, N., Watson, M. J., Beebe, K. E., Wells, C., Zuehlke, A. D., Shao, H., Bingham III, W. E., Kumar, V., Malhotra, S. V., Weigel, N. L., Gestwicki, J. E., Trepel, J. B., Neckers, L. M. “Targeting the Hsp40/Hsp70 chaperone axis identifies a novel strategy to treat castration-resistant prostate cancer” 2018 Cancer Res. 78:4022-4035. PMC6050126.

 (149) Ran, X., Burchfiel, E. T., Dong, B., Rettko, N. J., Dunyak, B. M., Shao, H., Thiele, D. J., Gestwicki, J. E. “Rational design and screening of peptide-based inhibitors of heat shock factor 1 (HSF1)” 2018 Bioorg. Med. Chem. 26:5299-5306. PMC6174099.

 (148) Mok, S.A., Condello, C., Gillies, A., Freilich, R., Oroz, J., Kadavath, H., Julien, O., Johnson, N., Assimon, V. A., Rauch, J. N., Dunyak, B.M., Lee, J., Tsai, F. T. F., Wilson, W. R., Zweckstetter, M., Dickey, C. A., Gestwicki, J. E. “Mapping interactions with the chaperone network reveals proteostasis factors that protect against tau aggregation” 2018 Nat. Struct. Mol. Biol. 25:384-393. PMC5942583.

 (147) Min, S.-W., Sohn, P. D., Li, Y., Devidze, N., Johnson, J. R., Krogen, N. J., Masliah, E., Mok, S.-A., Gestwicki, J. E., Gan, L. “SIRT1 deacetylates tau and reduces pathogenic tau spread in a mouse model of tauopathy” 2018 J. Neurosci. 38:3690-3688. PMC5895994.

 (146) Freilich, R. Arhar, T., Abrams, J. L., Gestwicki, J. E. “Protein-protein interactions in the molecular chaperone network” 2018 Acc. Chem. Res. 51:940-949. PMC6082625. 

 (145) Taylor, I. R., Dunyak, B. M., Komiyama, T., Shao, H., Ran, X., Assimon, V. A., Kalyanaraman, C., Rauch, J. N., Jacobson, M. P., Zuiderweg, E. R. P., Gestwicki, J. E. “High throughput screen for inhibitors of protein-protein interactions in a reconstituted heat shock protein 70 (Hsp70) complex” 2018 J. Biol. Chem. 293:4014-4025. PMC5857975.

 (144) Ouimet, C. M., Dawod, M., Grinias, J., Assimon, V. A., Lodge, J., Mapp, A. K., Gestwicki, J. E., Kennedy, R. T. “Protein cross-linking capillary electrophoresis at increased throughput for a range of protein-protein interactions” 2018 Analyst 143:1805-1812. PMC5902653.

 (143) Cesa, L. C., Shao, H., Srinivasan, S. R., Tse, E. Jain, C., Zuiderweg, E. R. P., Southworth, D. R., Mapp, A. K., Gestwicki, J. E. “X-Linked inhibitor of apoptosis (XIAP) is a client of heat shock protein 70 (Hsp70) and a biomarker of its inhibition” 2018 J. Biol. Chem. 293:2370-2380. PMC5818200. 

 (142) Srinivasan, S. R., Cesa, L.C, Li, X., Julien, O., Zhuang, M., Shao, H., Chung, J., Maillard, I., Wells, J. A., Duckett, C., Gestwicki, J. E. “Heat shock protein 70 (Hsp70) suppresses RIP1-dependent apoptotic and necroptotic cascades” 2018 Mol. Cancer Res. 16:58-68. PMC6101036. PMC6101036.

 (141) Young, Z. T., Mok, S. A., Gestwicki, J E. “Therapeutic strategies for restoring tau homeostasis” 2018 Prion Diseases, CSHL Press. PMC5540800.


 (140) Zuiderweg, E. R. P., Hightower, L. E. and Gestwicki, J. E. “The amazing multivalency of the Hsp70 chaperone” 2017 Cell Stress Chaperones 22:173-189. PMC5352603.

 (139) Pricer, R., Gestwicki, J. E., Mapp, A. K. “From fuzzy to function: the new frontier of protein-protein interactions” 2017 Acc. Chem. Res. 50:584-589. 

 (138) Rauch, J. N., Tse, E., Freilich, R., Mok, S.-A., Makley, L. N., Southworth, D. R., Gestwicki, J. E. “BAG3 is a modular scaffolding protein that physically links heat shock protein 70 (Hsp70) to the small heat shock proteins” 2017 J. Mol. Biol. 429:128-141. PMC5186407.

 (137) Rauch, J. N., Olson, S. H., Gestwicki, J. E. “Interactions between microtubule-binding protein tau (MAPT) and small molecules” 2017 Prion Disease, CSHL Press. PMC5495054.

 (136) Zuiderweg, E. R. P. and Gestwicki, J. E. “Backbone and methyl resonance assignments of the 42 kDa human Hsc70 nucleotide binding domain in the ADP state” 2017 J. Biomolecular NMR 11:11-15. PMC5344757.




  (135) Gabai, V. L., Yaglom, J. A., Wang, Y., Meng, L., Shao, H., Kim, G., Colvin, T., Gestwicki, J. E., Sherman, M. Y. “Anti-cancer effects of targeting Hsp70 in tumor stromal cells” 2016 Cancer Res. 76:5926-5932. PMC5065765. 

 (134) Rauch, J. N., Zuiderweg, E. R. P., Gestwicki, J. E. “Non-canonical interactions between heat shock cognate protein 70 (Hsc70) and Bcl2-associated anthanogene (BAG) co-chaperones are important for client release” 2016 J. Biol. Chem. 291:19848-19857. PMC5025674. 

 (133) Costa, M. D., Ashraf, N.S., Fischer, S., Yang, Y., Schapka, E. Joshi, G., McQuade, T.J., Dharia, R. M., Dulchavsky, M., Ouyang, M., Cook, D., Sun, D., Larsen, M. J., Gestwicki, J. E., Todi, S. V., Ivanova, M. I., Paulson, H. L. “Unbiased screen identifies aripiprazole as a modulator of abundance of the polyglutamine protein, ataxin-3” 2016 Brain (in press). 

 (132) Morozova, K., Clement, C. C., Kaushik, S., Stiller, B., Arias, E., Ahmad, A., Rauch, J. N., Chatterjee, V., Melis, C., Scharf, B., Gestwicki, J. E., Cuervo, A. M., Zuiderweg, E. R., Santambrogio, L. “Hsc70 structural and biological interactions with phosphatidylserine in endosomal microautophagy” 2016 J. Biol. Chem. 291:18096-18106. PMC5000059. 

 (131) Ouimet, C. M., Shao, H., Rauch, J.N., Dawod, M., Nordhues, B., Dickey, C. A., Gestwicki, J. E., Kennedy, R. T. “Protein cross-linking capillary electrophoresis (PXPE) for protein-protein interaction analysis” 2016 Anal. Chem. 88:8272-8278. PMC5111828.

 (130) Dunyak, B. M and Gestwicki, J. E. “Peptidyl-proline isomerases (PPIases): Targets for natural products and natural product-inspired compounds” 2016 J. Med. Chem. 59:9622-9644. PMC5501181.

 (129) Martin, M. D., Baker, J. D., Suntharalingam, A., Nordhues, B. A, Shelton, L. B., Zheng, D., Sabbagh, J. J., Haystead, T. A., Gestwicki, J. E., Dickey, C. A. “Inhibition of both Hsp70 activity and tau aggregation in vitro predicts tau lowering activity of small molecules” 2016 ACS Chem. Biol. 11:2041-2048. PMC5111430.

 (128) Young, Z. T., Rauch, J. N., Assimon, V. A., Jinwal, U. K., Ahn, M., Li, X., Dunyak, B. M., Ahmad, A., Carlson, G. A., Srinivasan, S. R., Zuiderweg, E. R. P., Dickey, C. A., Gestwicki, J. E. “Stabilizing the Hsp70-tau complex normalizes proteostasis in a model of tauopathy” 2016 Cell Chem. Biol. 23:992-1001. PMC4992411.

 (127) Sabnis, A. J., Guerriero, C. J., Olivas, V., Sayana, A., Shue, J. H., Flanagan, J., Asthana, S., Paton, A. W., Paton, J. C., Gestwicki, J. E., Walter, P., Weissman, J. S., Wipf, P., Brodsky, J. L., Bivona, T. G. “A combined chemical-genetic approach identifies cytosolic HSP70 dependence in rhabdomyosarcoma” 2016 Proc. Natl. Acad. Sci. 113:9015-9020. PMC4987817.

 (126) Paatero, A., Kellosalo, J., Dunyak, B. M., Almaliti, J., Gestwicki, J. E., Gerwick, W., Taunton, J., Paavilainen, V. O. “Apratoxin kills cells by direct, indiscriminate blockade of the Sec61 protein translocation channel” 2016 Cell Chem. Biol. 23:561-566.

 (125) Khachatoorian, R., Riahi, R., Ganapathy, E., Shao, H., Wheatley, N.M., Sundberg, C., Jung, C. L., Ruchala, P., Dasgupta, A., Arumugaswami, V. Gestwicki, J. E., French, S. W. “Allosteric heat shock protein 70 inhibitors block hepatitis C virus assembly” 2016 Int. J. Antimicrob Agents 47:289-296. PMC4833571.

 (124) Li, X., Shao, H., Taylor, I. R., Gestwicki, J. E. “Targeting allosteric control mechanisms in heat shock protein 70 (Hsp70)” 2016 Curr. Topics. Med. Chem. 16:2729-2740. PMC5502483. 

 (123) Srinivasan, S. R., Shao, H., Li, X., Gestwicki, J. E. “Allosteric inhibitors of Hsp70: Drugging the second chaperone of tumorigenesis” 2016 Topics Med. Chem. 19: 131-162. 

 (122) Klionsky, D. J. et al. “Guidelines for the use and interpretation of assays for monitoring autophagy (2nd edition)” 2016 Autophagy 12:1-222. PMC4835977.




(121) Assimon, V. A., Southworth, D. R., Gestwicki, J. E. “Specific binding of tetratricopeptide (TPR) proteins to heat shock protein 70 (Hsp70) and heat shock protein 90 (Hsp90) is regulated by affinity and phosphorylation” 2015 Biochemistry 54:7120-7131. PMC4714923.

(120) Taguwa, S., Maringer, K., Li, X., Bemal-Rubio, D., Rauch, J. N., Gestwicki, J. E., Andino, R., Fernandez-Sesma, A., Frydman, J. “Defining host Hsp70 subnetworks in Dengue virus replication reveals key vulnerability in flavivirus infection” 2015 Cell 163:1108-1123.

(119) Dunyak, B. M., Nakamura, R. L., Frankel, A. D., Gestwicki, J. E. “Selective targeting of cells via bi-specific molecules that exploit co-expression of two intracellular proteins” 2015 ACS Chem. Biol. 10:2441-2447. PMC4714926.

(118) Makley, L. N., McMenimen, K. A., DeVree, B. T., Goldman, J. W., McGlasson, B. N., Rajagopal, P., Dunyak, B. M., McQuade, T. J., Thompson, A. D., Sunahara, R., Klevit, R. E., Andley, U. P., Gestwicki, J. E. “Pharmacological chaperone for α-crystallin partially restores transparency in cataract models” 2015 Science 350:674-677. PMC4725592

(117) Min, S.-W., Chen, X., Tracy, T. E., Li, Y., Zhou, Y., Wang, C., Shirakawa, K., Minami, S. S., Defensor, E., Mok, S. A., Sohn, P. D., Schilling, B., Cong, X., Ellerby, L., Gibson, B. W., Johnson, J., Krogan, N., Chamloo, M., Gestwicki J. E., Masliah, E., Verdin, E., Gan, L. “Critical role of acetylation in tau-mediated neurodegeneration and cognitive deficits” 2015 Nat. Med. 21:1154-1162. PMC4598295

(116) Cesa, L. C., Mapp, A. K., Gestwicki, J. E. “Direct and propagated effects of small molecules on protein-protein interaction networks” 2015 Frontiers Bioengin. Biotechnol. 3:119. PMC4547496.

(115) Guan, S., Trnka, M. J., Bushnell, D. A., Robinson, P. J., Gestwicki, J. E., Burlingame, A. L. “Deconvolution method for specific and nonspecific binding of ligand to multiprotein complex by native mass spectrometry” 2015 Anal. Chem. 87:8541-8546. PMC4714924

(114) Fontaine, S. N., Martin, M. D., Akoury, E., Assimon, V. A., Borysov, S., Nordhues, B. A., Sabbagh, J. J., Cockman, M., Gestwicki, J. E., Zweckstetter, M., Dickey, C. A. “The active Hsc70/tau complex can be exploited to enhance tau turnover without damaging microtubule dynamics” 2015 Hum. Mol. Genetics 24:3971-3981. PMC4560066.

(113) Fontaine, S. N., Rauch, J. N., Stothert, A., Fertig, A., Assimon, V. A., Cockman, M., Chang, L., Li, P., Thompson, A. D., Sabbagh, J. J., Nordues, B. A., Jinwal, U. K., Stevens, S. M., Zweckstetter, M., Zuiderweg, E. R. P., Gestwicki, J. E., Dickey, C. A. “Isoform selective genetic inhibition of constitutive cytosolic Hsp70 activity promotes client tau degradation using an altered co-chaperone complement” 2015 J. Biol. Chem. 290:13115-13127. PMC4505567. 

(112) Assimon, V. A., Shao, H., Garneau-Tsodikova, S., Gestwicki, J. E. “Concise synthesis of spergualin-inspired molecules with broad-spectrum antibiotic activity” 2015 MedChemComm 6:912-918. PMC4829345. 

(111) Martin, M. D., Calcul, L., Smith, C., Umesh, J., Fontaine, S. N., Darlin, A., Seeley, K., Wojtas, L., Narayan, M., Gestwicki, J. E., Smith, G., Reitz, A., Baker, B., Dickey, C. A. “Synthesis, stereochemical analysis and derivatization of myricanol provide new probes that promote autophagic tau clearance” 2015 ACS Chem. Biol. 10:1099-1109. 

(110) Li, X., Colvin, T., Rauch, J.N., Acosta-Alvear, D., Kampmann, M., Dunyak, B., Hann, B., Aftab, B. T., Murnane, M., Cho, M., Walter, P., Weissman, J. S., Sherman, M. Y., Gestwicki, J. E. “Validation of the Hsp70-Bag3 protein-protein interaction as a potential therapeutic target in cancer” 2015 Mol. Cancer Therapeutics 14:643-648. PMC4456214. 

(109) Pratt, W. B., Gestwicki, J. E., Osawa, Y., Lieberman, A. “Targeting the protein quality control function of the Hsp90/Hsp70-based chaperone machinery for treatment of adult onset neurodegenerative diseases” 2015 Annu. Rev. Pharmacol. Toxicol. 53:353-371. PMC4372135. 




(108) Selenica, M. L., Davtyan, H., Housley, S. B., Blair, L. J., Gillies, A., Nordhues, B. A., Zhang, B., Liu, J. Gestwicki, J. E., Lee, D. C. Gordon, M. N., Morgan D., Dickey, C. A. “Epitope analysis following active immunization with tau proteins reveals immunogens implicated in tau pathogenesis” 2014 J. Neuroinflammation 11:152. PMC4167523.

(107) Ung, P. M.-U., Dunbar Jr., J. B., Gestwicki, J. E., Carlson, H. A. “An allosteric modulator of HIV-1 protease shows equipotent inhibition of wild type and drug-resistant proteases” 2014 J. Med. Chem. 57:6488-78. PMC4136727.

(106) Jaeger, A. M., Makley, L. N., Gestwicki, J. E., Thiele, D. J. “Genomic heat shock element sequences drive cooperative human heat shock transcription factor 1 DNA binding and selectivity” 2014 J. Biol. Chem. 289:30459-30469. PMC4215228. 

(105) Colvin, T., Gabai, V. L., Gong, J., Calderwood, S. K., Li, H., Gummuluru, S., Matchuk, O., Smirnova, S., Orlova, N., Zamulaeva, I., Garcia-Marcos, M., Li, X., Young, Z. T., Rauch, J. N., Gestwicki, J. E.*, Takayama, S., Sherman, M. Y.* “Hsp70-BAG3 module regulates cancer-related signaling networks” 2014 Cancer Research 74:4731-4740. *co-corresponding authors PMC4174322.

(104) Pratt, W. B., Morishima, Y., Gestwicki, J. E., Lieberman, A. P., Osawa, Y. “A model in which Hsp90 targets protein folding clefts leads to a new approach to neuroprotective treatment of protein folding diseases” 2014 Experimental Biology and Medicine 239:1405-1413. PMC4318483.

(103) Connarn, J. N., Assimon, V. A., Reed, R. A., Tse, E., Southworth, D. R., Zuiderweg, E. R. P., Gestwicki, J. E., Sun, D. “The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the TPR domain” 2014 J. Biol. Chem. 289:2908-2917. PMC3908423.

(102) Rauch, J. N. and Gestwicki, J. E. “Binding of human nucleotide exchange factors to heat shock protein 70 (Hsp70) generates functionally distinct complexes in vitro” 2014 J. Biol. Chem. 289:1402-1414. PMC3894324.

(101) Walter, G. M., Raveh, A., Mok, S.-A., McQuade, T. J., Arevang, C. J., Schultz, P. J., Smith, M. C., Asare, S., Cruz, P. G., Wisen, S., Matainaho, T., Sherman, D. H., Gestwicki, J. E. “High throughput screen of natural product extracts in a yeast model of polyglutamine proteotoxicity” 2014 Chem. Biol. Drug Design 83:440-449. PMC4068144.




(100) Li, X., Srinivasan, S. R., Connarn, J., Ahmad, A., Young, Z. T., Kabza, A. M., Zuiderweg, E. R. P., Sun, D., Gestwicki, J. E. “Analogs of the allosteric heat shock protein 70 (Hsp70) inhibitor, MKT-077, as anti-cancer agents” 2013 ACS Med. Chem. Lett. 4:1042-1047. PMC3845967.

(99) Ung, P. M-U., Thompson, A. D., Chang, L., Gestwicki, J. E., Carlson, H. A. “Identification of key hinge residues important for nucleotide-dependent allostery in E. coli Hsp70/DnaK” 2013 PLoS Comp. Biol. 9:e1003279. PMC3836694.

(98) Rauch, J. N.*, Nie, J.*, Buchholz, T. J., Gestwicki, J. E., Kennedy, R. E. “Development of a capillary electrophoresis platform for identifying inhibitors of protein-protein interactions” 2013 Anal. Chem. 85:9824-9831. * these authors contributed equally. PMC3845662.

(97) Smith, M. C., Scaglione, K. M., Assimon, V. A., Patury, S., Thompson, A. D., Dickey, C. A., Southworth, D. R., Paulson, H. L., Gestwicki, J. E.*, Zuiderweg, E. R. P.* “The E3 ubiquitin ligase CHIP and the molecular chaperone Hsc70 form a dynamic, tethered complex” 2013 Biochemistry 52:5354-5364. * co-corresponding authors. PMC3856692.

(96) Cesa, L. C.*, Patury, S.*, Komiyama, T., Ahmad, A., Zuiderweg, E. R. P., Gestwicki, J. E. “Inhibitors of difficult protein-protein interactions identified by high throughput screening of multi-protein complexes” 2013 ACS Chem. Biol. (in press). * these authors contributed equally. 

(95) Dunbar, J. B., Smith, R. D., Damm-Ganamet, K. L., Ahmed, A., Esposito, E. X., Delproposto, J., Chinnaswarmy, K., Kang, Y.N., Kubish, G., Gestwicki, J. E., Stuckey, J. A., Carlson, H. A. “CSAR Dataset Release 2012: Ligands, affinities, complexes and docking decoys” 2013 J. Chem. Inf. Model. (in press). 

(94) Miyata, Y., Li, X., Lee, H.-F., Jinwal, U.K., Srinivasan, S.R., Seguin, S.P., Young, Z. T., Brodsky, J. L., Dickey, C. A., Sun, D., Gestwicki, J. E. “Synthesis and initial evaluation of YM-08, a blood-brain barrier permeable derivative of the heat shock protein 70 (Hsp70) inhibitor, MKT-077, which reduces tau levels” 2013 ACS Chem. Neurosci. (in press).

(93) Abisambra, J., Jinwal, U. K., Miyata, Y., Rogers, J., Blair, L., Li, X., Seguin, S. P., Wang, L., Jin, Y., Bacon, J., Brady, S., Cockman, M., Guidi, C., Zhang, J., Koren, J., Young, Z. T., Atkins, C. A., Zhang, B., Lawson, L. Y., Weeber, E. J., Brodsky, J. L., Gestwicki, J. E., Dickey, C. A. “Allosteric Hsc70 inhibitors rapidly rescue synaptic plasticity deficits by reducing aberrant tau” 2013 Biol. Psych. (in press).

(92) Jinwal, U.K., Akoury, E., Abisambra, J.F., O’Leary, J.C., Thompson, A.D., Blair, L.J., Ying, J., Bacon, J., Nordhues, B.A., Cockman, M., Zhang, J., Li, P., Zhang, B., Borysov, S., Uversky, V.N., Biernat, J., Mandelkow, E., Gestwicki, J. E., Zweckstetter, M., Dickey, C. A. “Imbalance of Hsp70 family variants fosters tau accumulation” 2013 FASEB J. 27:1450-1459. PMC3606536.

(91) Makley, L. N. and Gestwicki, J. E. “Expanding the number of “druggable” targets: non-enzymes and protein-protein interactions” 2013 Chem. Biol. Drug Design 81:22-32. PMC3531880.

(90) Assimon, V. A., Gillies, A. T., Rauch, J. N., Gestwicki, J. E. “The Hsp70 multi-protein complex as a drug target” 2013 Current Pharm. Design 19:404-417.

(89) Wang, A. M., Miyata, Y., Klinedinst, S., Peng, H.-M., Chua, J. C., Li, X., Pratt, W. B., Osawa, Y., Collins, C. A., Gestwicki, J. E.*, Lieberman, A. P.* “Activation of Hsp70 reduces neurotoxicity by promoting polyglutamine protein degradation” 2013 Nat Chem. Biol. 9:112-118. * co-corresponding authors PMC3552084.




(88) Davis, M. J., Gregorka, B., Gestwicki, J. E., Swanson, J. A. “Inducible lysosome renitence in macrophages limits Listeria monocytogenes infection” 2012 J. Immunol. 189:4488-4495. PMC3478491.

(87) Seguin, S. P., Ireland, A. W., Miyata, Y., Wipf, P., Pipas, J. M., Gestwicki, J. E., Brodsky, J. L. “A screen for modulators of large T antigen’s ATPase activity uncovers novel inhibitors of simian virus 40 and BK virus replication” 2012 Antiviral Res. 96:70-81. PMC3465505.

(86) Gillies, A. T., Taylor, R., Gestwicki, J. E. “Synthetic lethal interactions in yeast reveal functional roles of J protein co-chaperones” 2012 Mol. Biosystems 8:2901-2908. PMC3463740.

(85) Thompson, A. D., Scaglione, K. M., Prensner, J., Gillies, A. T., Chinnaiyan, A., Paulson, H. L., Jinwal, U. K.*, Dickey, C. A.*, Gestwicki, J. E.* “Analysis of the tau-associated proteome reveals that exchange of Hsp70 for Hsp90 is involved in tau degradation” 2012 ACS Chem. Biol. 7:1677-1686. * indicates co-corresponding authors. PMC3477299.

(84) Miyata, Y.*, Rauch, J. N.*, Jinwal, U. K., Thompson, A. D., Srinivasan, S., Dickey, C. A., Gestwicki, J. E. “Cysteine reactivity distinguishes redox sensing by the heat inducible and constitutive forms of heat shock protein 70 (Hsp70). 2012 Chem. Biol. 19:1391-1399. * these authors contributed equally. PMC3508472

(83) Smith, M. C., Gestwicki, J. E. “Features of protein-protein interactions that translate into potent inhibitors: topology, surface area and affinity” 2012 Expert Rev. Mol. Med. 14:e16. PMC3591511.

(82) Thompson, A. D., Dugan, A., Gestwicki, J. E.*, Mapp, A K.* “Fine tuning multi-protein complexes using small molecules” 2012 ACS Chem. Biol. 7:1311-1320. * co-corresponding authors. PMC3477299

(81) Chafekar, S. M., Wisén, S., Thompson, A. D., Echeverria, A., Walter, G. M., Evans, C. G., Makley, L. N., Gestwicki, J. E.*, Duennwald, M. L.* “Pharmacological tuning of heat shock protein 70 modulates polyglutamine toxicity and aggregation” 2012 ACS Chem. Biol. 7:1556-1564. * co-corresponding authors. PMC3448832

(80) Jinwal, U. K., Abisambra, J. F., Zhang, J., Dharia, S., O’Leary, J. C., Patel, T., Braswell, K., Jani, T., Gestwicki, J. E., Dickey, C. A. “Cdc37/Hsp90 complex disruption triggers autophagic clearance cascade for TDP-43” 2012 J. Biol. Chem. 287:24814-24820. PMC3397908

(79) Hammer, N. D., McGuffie, B. A., Zhou, Y., Badtke, M. P., Reinke, A. A., Brännström, K., Gestwicki, J. E., Olofsson, A., Almqvist, F., Chapman, M. R. “The C-terminal repeating units of CsgB direct bacterial functional amyloid nucleation” 2012 J. Mol. Biol. 422:376-389. PMC3423549

(78) Srinivasan, S. R., Gillies, A., Chang, L., Thompson, A. D., Gestwicki, J. E. “Molecular chaperones DnaK and DnaJ share predicted binding sites on most proteins in the E. coli proteome” 2012 Mol. Biosystems 8:2323-2333. PMC3462289

(77) Klionsky et al. “Guidelines for the use and interpretation of assays for monitoring autophagy” 2012 Autophagy 8:445-544.

(76) Koren III, J., Miyata, Y., KIray, J., Nguyen, L., Guo, J., Blair, L. J., O’Leary III, J. O., Abisambra, J. F., Li, X., Jinwal, U. K., Cheng, J. Q., Gestwicki, J. E., Dickey, C. A. “Rhodacyanine derivative selectively targets cancer cells and overcomes tamoxifen resistence”  2012 PLoS One 7:e35566. PMC338522.

(75) Congdon, E. E., Wu, J. W., Myeku, Figueroa, Y. H., Herman, M., Marinec, P. S., Gestwicki, J. E., Dickey, C. A., Yu, W. H., Duff, K. “Methylthioninium choride (methylene blue) induces autophagy and attenuates tauopathy in vitro and in vivo” 2012 Autophagy 8:1-14.

(74) Thompson, A. D., Bernard, S. M., Skiniotis, G., Gestwicki, J. E. “Visualization and functional analysis of the oligomeric states of Escherichia coli heat shock protein 70 (Hsp70/DnaK)” 2012 Cell Stress Chaperones 17:313-327. PMC3312962

(73) Zuiderweg, E. R. P., Bertelsen, E. B., Rousaki, A., Mayer, M. P., Gestwicki, J. E., Ahmad, A. “Allostery in the Hsp70 chaperone proteins” 2012 Topics Curr. Chem. 1-55.

(72) Gestwicki, J. E. and Garza, D. “Protein quality control in neurodegenerative disease” in The Molecular Biology of Neurodegenerative Disease. D. B. Teplow, Ed. Academic Press Inc. 2012, Progress in Molecular Biology and Translational Science, vol. 107. pgs 327-353.




(71) Walter, G. M., Smith, M. C., Wisen, S., Basrur, V., Elenitoba-Johnson, K. S. J., Duennwald, M. L., Kumar, A., Gestwicki, J. E. “Ordered assembly of heat shock proteins, Hsp26, Hsp70, Hsp90 and Hsp104, on expanded polyglutamine fragments revealed by chemical probes” 2011 J. Biol. Chem. 286:40486-40493. PMC3220478

(70) Morishima, Y., Miranda, L., Peng, H-M., Miyata, Y., Gestwicki, J. E., Pratt, W., Osawa, Y. “Heme-dependent activation of neuronal nitric oxide synthase by cytosol is due to an Hsp70-dependent, thioredoxin-mediated thiol-disulfide interchange in the heme/substrate binding cleft” 2011 Biochemistry 50:7146-7156. PMC3156863

(69) Rousaki, K., Miyata, Y., Jinwal, U. K., Dickey, C. A., Gestwicki, J. E.*, Zuiderweg, E. R. P.* “Allosteric drugs: the interaction of anti-tumor compound MKT-077 with human Hsc70 chaperones” 2011 J. Mol. Biol.  411:614-632. * co-corresponding authors. PMC3146629

(68) Scaglione, K. M., Zavodszky, E., Todi, S. V., Patury, S., Xu, P., Rodriguez-Lebron, E., Fischer, S., Djarmata, A., Peng, J., Gestwicki, J. E., Paulson, H. L. “Ube2w and ataxin-3 coordinately regulate the ubiquitin ligase CHIP” 2011 Mol. Cell 43:599-612. PMC3166620

(67) Miyata, Y., Koren III, J., Kiray, J., Dickey, C. A., Gestwicki, J. E. “Molecular chaperones and regulation of tau quality control: Strategies for drug discovery in tauopathies” 2011 Future Med. Chem. 3(12):1523-1537. PMC3190966

(66) Reinke, A. A. and Gestwicki, J. E. “Insights into amyloid structure using chemical probes” 2011 Chem. Biol. Drug Design 77:399-411. PMC3097318

(65) Evans, C. G.*, Smith, M. C.*, Carolan, J. P., Gestwicki, J. E. “Improved synthesis of 15-deoxyspergualin analogs using the Ugi multicomponent reaction” 2011 Bioorgan. Med. Chem. Lett. 21:2587-2590. * these authors contributed equally. PMC3088103

(64) Chang, L., Miyata, Y., Ung, P. M. U., Bertelsen, E. B., McQuade, T. J., Carlson, H. A., Zuiderweg, E. R. P., Gestwicki, J. E. “Chemical screens against a reconstituted multi-protein complex: myricetin blocks DnaJ regulation of DnaK through an allosteric mechanism” 2011 Chem. Biol. 18:210-221. PMC3057461

(63) Bainor, A., Chang, L., McQuade, T. J., Webb, B., Gestwicki, J. E. “Bicinchoninic acid (BCA) assay in low volume” 2011 Anal. Biochem. 410:310-312.

(62) Evans, C. G., Jinwal, U. K., Makley, L. N., Dickey, C. A., Gestwicki, J. E. “Identification of dihydropyridines that reduce cellular tau levels” 2011, Chem. Comm. 47:529-531.  PMC3251959




(61) Reinke, A. A., Ung, P. M.-U., Quintero, J. J., Carlson, H. A., Gestwicki, J. E. “Chemical probes selectively recognize the earliest Aβ oligomers in complex mixtures” 2010, J. Am. Chem. Soc. 132:17655-17657. PMC3005376

(60) O’Leary III, J. C., Li, Q., Marinec, P. S., Blair, L. J., Congdon, E. E., Johnson, A. G., Jinwal, U. K., Koren III, J., Jones, J. R., Kraft, C., Peters, M., Abisambra, J. F., Duff, K. E., Weeber, E. J., Gestwicki, J. E., Dickey, C. A. “Phenothiazine-mediated rescue of cognition in tau transgenic mice requires neuroprotection and reduced soluble tau burden” 2010, Mol. Neurodegen. 5:45. PMC2989315

(59) Xu, T., Johnson, C. A., Gestwicki, J. E., Kumar, A. “Conditionally controlling nuclear trafficking in yeast by chemical-induced protein dimerization” 2010, Nature Protocols 5(11):1831-1843.

(58) Reinke, A. A., Abulwerdi, G. A., Gestwicki, J. E. “Quantifying pre-fibrillar amyloids in vitro using a “thioflavin-like” spectroscopic method” 2010, ChemBioChem 11:1889-1895.

(57) Miyata, Y.*, Chang, L.*, Bainor, A., McQuade, T. J., Walczak, C. P., Zhang, Y., Larsen, M. J., Kirchoff, P., Gestwicki, J. E. “High throughput screen for Escherichia coli heat shock protein 70 (Hsp70/DnaK): colorimetric ATPase assay in low volume by exploiting energy transfer” 2010, J. Biomol. Screen. 15:1211-1219. *these authors contributed equally. PMC3052282

(56) Wisén, S., Bertelsen, E. B., Thompson, A. D., Patury, S., Ung, P., Chang, L., Evans, C. G., Walter, G. A. M., Wipf, P., Carlson, H. A., Brodsky, J. L., Zuiderweg, E. R. P., Gestwicki, J. E. “Binding of a small molecule at a protein-protein interface regulates chaperone activity in the Hsp70-Hsp40 complex” 2010 ACS Chemical Biology 5:611-622. PMC2950966

(55) Chang, L.*, Thompson, A. D.*, Ung, P., Carlson, H. A., Gestwicki, J. E. “Mutagenesis reveals the complex relationships between ATPase rate and the chaperone activities of Escherichia coli heat shock protein 70 (Hsp70/DnaK)” 2010, J. Biol. Chem. 285:21282-21291. *denotes equal contribution. PMC2898401

(54) Wang, A. M., Morishima, Y., Clapp, K. M., Peng, H.-M., Pratt, W. B., Gestwicki, J. E., Osawa, Y., Lieberman, A. P. “Inhibition of Hsp70 by methylene blue affects signaling protein function and ubiquitination and modulates polyglutamine protein degradation” 2010, J. Biol. Chem. 285:15714-15723. PMC2871437

 (53) Evans, C. G., Chang, L., Gestwicki, J. E. “Heat shock protein 70 (Hsp70) as an emerging drug target” 2010, J. Med. Chem. 53:4585-4602. PMC2895966

 (52) Jinwal, U. K., O’Leary III, J. C., Borysov, S. I., Jones, J. R., Li, Q., Koren III, J., Abisambra, J. F., Vestal, G. D., Lawson, L. Y., Johnson, A. G., Blair, L. J., Jin, Y., Miyata, Y., Gestwicki, J. E., Dickey, C. A. “Hsc70 rapidly engages tau after microtubule destabilization” 2010, J. Biol. Chem. 285:16798-16805. PMC2878041

(51) Koren III, J., Jinwal, U. K., Jin, Y., O’Leary, J., Jones, J. R., Johnson, A. G., Blair, L. J., Abisambra, J. F., Chang, L., Miyata, Y., Cheng, A. M., Guo, J., Cheng, J. Q., Gestwicki, J. E., Dickey, C. A. “Facilitating Akt clearance via manipulation of Hsp70 activity and levels” 2010, J. Biol. Chem. 285(4):2498-2505. PMC2807306




(50) Patury, S., Miyata, Y., Gestwicki, J. E. “Pharmacological targeting of the Hsp70 chaperone” 2009, Curr. Top. Med. Chem. 9(15):1337-1351. PMC2799686

49) Jinwal, U. K., Miyata, Y., Koren, J., Jones, J. R., Trotter, J. H., Weeber, E. J., Chang, L., Shults, C. L., Rousaki, A. Zuiderweg, E. R. P., Gestwicki, J. E., Dickey, C. A. “Chemical manipulation of Hsp70 ATPase activity regulates tau stability” 2009, J. Neurosci. 29:12079-12088. PMC2775811

(48) Reinke, A. A., Seh, H. Y., Gestwicki, J. E. “A chemical screen approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta” 2009, Bioorg. Med. Chem. Lett. 19:4952-4957. PMC2730169

(47) Marinec, P. S., Evans, C. G., Gibbons, G. S., Tarnowski, M. A., Overbeek, D. L., Gestwicki, J. E. “Synthesis of orthogonally reactive FK506 derivatives via olefin cross metathesis” 2009, Bioorg. Med. Chem. 17:5763-5768. PMC2758530

(46) Evans, C. G. and Gestwicki, J. E. “Enantioselective organocatalytic Hantzsch synthesis of polyhydroquinolines” 2009, Org. Lett. 11(14):2957-2959. PMC2727599

(45) Bertelsen, E. B., Chang. L., Gestwicki, J. E., Zuiderweg, E. R. P. “Solution conformation of wild-type E. coli Hsp70 (DnaK) chaperone complexed with ADP and substrate” 2009, Proc. Natl. Acad. Sci. 106:8471-8476. PMC2689011

(44) Patury, S., Geda, P., Dobry, C. J., Kumar, A., Gestwicki, J.E. “Conditional nuclear import and export of yeast proteins using a chemical inducer of dimerization” 2009, Cell Biochem. Biophys. 53:127-134.

(43) Marinec, P. S., Chen, L., Barr, K. J.; Mutz, M. W.; Crabtree, G. R., Gestwicki, J. E. “FK506-binding protein partitions a modified HIV protease inhibitor into blood cells and prolongs its lifetime in vivo” 2009, Proc. Natl. Acad. Sci. 106(5):1336-1341. PMC2635806

(42) Lexa, K. W., Damm, K. L., Quintero, J. J., Gestwicki, J. E., Carlson, H. A. "Clarifying allosteric control of flap conformations in the 1TW7 crystal structure of HIV-1 protease" 2009, Proteins 74:872-880. PMC2635929




(41) Gestwicki, J. E. and Kumar, A. “Two- and three-hybrid systems” Encyclopedia of Chemical Biology, 2008, p615-629.

(40) Geda, P., Patury, S., Ma, J., Barucha, N., Dobry, C. J., Lawson, S. K., Gestwicki, J. E., Kumar, A. “A small molecule-directed approach to control protein localization and function” 2008, Yeast 25:577-594.

(39) Marinec, P. S., Lancia, J. K., Gestwicki, J. E. “Bifunctional molecules evade cytochrome P450 metabolism by forming protective complexes with FK506-binding protein” Mol. Biosystems. 2008, 4:571-578. (Featured on the Cover).

(38) Damm, K. L., Ung, P. M. U., Quintero, J. J., Gestwicki, J. E., Carlson, H. A. “A poke in the eye: Inhibiting HIV-1 protease through its flap-recognition pocket” Biopolymers 2008, 89:643-652. PMC2859825

(37) Wisén, S. and Gestwicki, J. E. “Identification of small molecules that modify the protein folding activity of heat shock protein 70 (Hsp70)” Anal. Biochem. 2008, 374:371-377.

(36) Wisén, S., Androsavich, J., Evans, C. G., Chang, L. and Gestwicki, J. E. “Chemical modifiers of heat shock protein 70 (Hsp70) by sequential, microwave-accelerated reactions on solid phase” Bioorgan. Med. Chem. Lett. 2008, 18:60-65.

(35) Chang, L., Bertelsen, E. B., Wisén, S., Larsen, E. M., Zuiderweg, E. R. P., Gestwicki, J. E. “High throughput screen for small molecules that modulate the ATPase activity of the molecular chaperone, DnaK” Anal. Biochem. 2008, 372:167-176.




(34) Hadden, M. K., Galam, L. Gestwicki, J. E., Matts, R. L., Blagg, B. S. J. “Derrubone, an inhibitor of the Hsp90 protein folding machinery” J. Nat. Prod. 2007, 70:2014-2018.

(33) Gestwicki, J. E. and Marinec, P. S. “Chemical control over protein-protein interactions: beyond inhibitors” Combi. Chem. High Throughput Screen. 2007, 10(8):667-675.

(32) Rubinsztein, D. C.; Gestwicki, J. E.; Murphy, L. O.; Klionsky, D. J. “Potential therapeutic applications of autophagy” Nature Rev. Drug Disc. 2007, 6:304-312.

(31) Reinke, A. A. and Gestwicki, J. E. “Structure activity relationships for amyloid beta aggregation inhibitors based on curcumin: Influence of linker length and flexibility” Chem. Biol. Drug Design. 2007, 70:206-215.

(30) Stankunas, K.; Bayle, J. H.; Havranek, J. J.; Wandless, T. J.; Baker, D.; Crabtree, G. R.; Gestwicki, J. E. “Rescue of degradation-prone mutants of the FK506-rapamycin binding (FRB) protein with chemical ligands” ChemBioChem 2007, 8:1162-1169.




(29) Evans, C. G.; Wisén, S.; Gestwicki, J. E. “Heat shock proteins 70 and 90 inhibit early stages of amyloid beta aggregation in vitro” J. Biol. Chem. 2006, 281:33182-33191.


Previous Work (undergraduate, graduate, postdoctoral):


(28) Bayle, J. H.; Grimley, J. S.; Stankunas, K.; Gestwicki, J. E.; Wandless, T. J.; Crabtree, G. R. “Rapamycin analogs with differential binding specificity permit orthogonal control of protein activity” Chem. Biol. 2006, 19:99-107.

(27) Liu, K.; Gestwicki, J. E.; Crabtree, G. R. “Bringing small molecule regulation of protein activity to developmental systems” in Analysis of Growth Factor Signaling in Embryos Whitman, M. and Sater, A. Eds.; CRC Press 2006, 369-393.

(26) Kiessling, L. L.; Gestwicki, J. E.; Strong, L. E. “Synthetic ligands as probes of signal transduction” Angew. Chem. Int. Ed.  2006, 45:2348-2368.

(25) Bose, M.; Gestwicki, J. E.; Devasthali, V.; Crabtree, G. R.; Graef, I. A. “”Nature inspired” drug-protein complexes as inhibitors of Aβ aggregation” Biochem. Soc. Trans. 2005 33(4):543-547.

(24) Gestwicki, J. E.; Crabtree, G. R.; Graef, I. A. “Harnessing chaperones to generate small molecule inhibitors of amyloid β aggregation” Science 2004, 306:865-869.

(23) Chang, C.-P.; Neilson, J. R.; Bayle, J. H.; Gestwicki, J. E.; Kuo, A.; Stankunas, K.; Graef, I. A.; Crabtree, G. R. “A field of myocardial-endocardial NFAT signaling underlies heart valve morphogenesis” Cell 2004, 118(5):649-663.

(22) Stankunas, K.; Bayle, J. H.; Gestwicki, J. E.; Lin, Y.-M.; Wandless, T. J.; Crabtree, G. R. “Conditional protein alleles using knock-in mice and a chemical inducer of dimerization” Mol. Cell 2003, 12:1615-1624.

(21) Gestwicki, J. E.; Cairo, C. W.; Borrok, M. J.; Kiessling, L. L.; “Visualization and characterization of receptor clusters by transmission electron microscopy” Methods Enzymol. 2003, 362:301-312.

(20) Gestwicki, J. E.; Cairo, C. W.; Strong, L. E.; Oetjen, K. A.; Kiessling, L. L. “Influencing receptor-ligand binding mechanisms with multivalent ligand architecture” J. Am. Chem. Soc. 2002, 124(50):14922-14933.

(19) Lamanna, A. C.; Gestwicki, J. E.; Strong, L. E.; Borchardt, S. L.; Owen, R. M.; Kiessling, L. L. “Conserved amplification of chemotactic signals by inter-chemoreceptor interactions” J. Bacteriol. 2002, 184(18):4981-4987.

(18) Owen, R. M.; Gestwicki, J. E.; Young, T.; Kiessling, L. L. “Synthesis of end-labeled neoglycopolymers” Org. Lett. 2002, 4(14):2293-2296.

(17) Gestwicki, J. E.; Cairo, C. W.; Mann, D. A; Owen, R. M.; Kiessling, L. L. “Selective immobilization of multivalent ligands for surface plasmon resonance and fluorescence microscopy experiments” Anal. Biochem. 2002, 305(2):149-155.

(16) Gestwicki, J. E.; Strong, L. E.; Cairo, C. W.; Boehm, F. J.; Kiessling, L. L. “Cell aggregation by scaffolded receptor clusters” Chem. Biol. 2002, 9(2):163-169 (Featured on the Cover).

(15) Cairo, C. W.; Gestwicki, J. E.; Kanai, M.; Kiessling, L. L. “Control of multivalent interactions by ligand epitope density” J. Am. Chem. Soc. 2002, 124(8):1615-1619.

(14) Gestwicki, J. E.; Kiessling, L. L. “Inter-receptor communication through arrays of bacterial chemoreceptors” Nature 2002, 415:81-84.

(13) Gestwicki, J. E.; Hsieh, H. V.; Pitner, J. B. “Using receptor conformational change to detect low molecular weight analytes by surface plasmon resonance” Anal. Chem. 2001, 73:5732-5737.

(12) Gestwicki, J. E.; Strong, L. E.; Borchardt, S. L.; Cairo, C. W.; Schnoes, A. M.; Kiessling, L. L. “Designed potent multivalent chemoattractants for Escherichia coli” Bioorg. Med. Chem. 2001, 9(9):2387-2393.

(11) Kiessling, L. L.; Strong, L. E.; Gestwicki, J. E. “Principles of multivalent ligand design” Annu. Rep. Med. Chem. 2000, 35:321-330.

(10) Kiessling, L. L.; Gestwicki, J. E.; Strong, L. E. “Synthetic multivalent ligands in the exploration of cell surface interactions” Curr. Opin. Chem. Biol. 2000, 4(6):696-703.

(9) Gestwicki, J. E.; Strong, L. E.; Kiessling, L. L. “Visualization of single multivalent receptor-ligand complexes by transmission electron microscopy” Angew. Chem. Int. Ed. Engl. 2000, 39(24):4567-4570.

(8) Gestwicki, J. E.; Lamanna, A. C.; Harshey, R. M.; McCarter, L. L.; Kiessling, L. L.; Adler, J. “Evolutionary conservation of methyl-accepting chemotaxis protein location in Bacteria and Archaea” J. Bacteriol. 2000, 182(22):6499-6502.

(7) Gestwicki, J. E.; Strong, L. E.; Kiessling, L. L. "Tuning chemotactic responses using synthetic multivalent ligands” Chem. Biol. 2000, 7(8):583-591 (Featured on the Cover).

(6) Maki, N.; Gestwicki, J. E.; Lake, E. M.; Kiessling, L. L.; Adler, J. “Motility and chemotaxis of filamentous cells of Escherichia coli " J. Bacteriol. 2000, 182(15):4337-4342.

(5) Gordon, E. J.; Gestwicki, J. E.; Strong, L. E.; Kiessling, L. L. “Synthesis of end-labeled multivalent ligands for exploring cell-surface-receptor-ligand interactions” Chem. Biol. 2000, 7(1):9-16.

(4) Hoag, K. A.; Clise-Dwyer, K.; Lim, Y.-H.; Nashold, F. E.; Gestwicki, J. E.; Cancro, M. P.; Hayes, C. E. “A quantitative trait locus controlling peripheral B-cell deficiencies maps to murine chromosome 15” Immunogenetics 2000, 51(11):924-929.

(3) Kabza, K. G.; Chapados, B. R.; Gestwicki, J. E.; McGrath, J. L. “Microwave induced esterification using heterogeneous acid catalysis in a low dielectric constant medium” J. Org. Chem. 2000, 65(4):1210-1214.

(2) Kabza, K. G.; Gestwicki, J. E.; McGrath, J. L. “Contact angle goniometry as a tool for surface tension measurements of solids, using Zisman plot method: Physical chemistry experiment” J. Chem. Educ. 2000, 77(1):63-65.

(1) Kabza, K. G.; Gestwicki, J. E.; McGrath, J. L.; Petrassi, H. M. “Effect of microwave radiation upon copper (II) 2,2'-bipyridyl mediated hydrolysis of Bis-p-nitrophenolphosphodiester and enzymatic hydrolysis of carbohydrates” J. Org. Chem. 1996, 61:9599-9602.