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Items: 14


The epichaperome is an integrated chaperome network that facilitates tumour survival.

Rodina A, Wang T, Yan P, Gomes ED, Dunphy MP, Pillarsetty N, Koren J, Gerecitano JF, Taldone T, Zong H, Caldas-Lopes E, Alpaugh M, Corben A, Riolo M, Beattie B, Pressl C, Peter RI, Xu C, Trondl R, Patel HJ, Shimizu F, Bolaender A, Yang C, Panchal P, Farooq MF, Kishinevsky S, Modi S, Lin O, Chu F, Patil S, Erdjument-Bromage H, Zanzonico P, Hudis C, Studer L, Roboz GJ, Cesarman E, Cerchietti L, Levine R, Melnick A, Larson SM, Lewis JS, Guzman ML, Chiosis G.

Nature. 2016 Oct 20;538(7625):397-401. doi: 10.1038/nature19807. Epub 2016 Oct 5.


Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.

Patel HJ, Patel PD, Ochiana SO, Yan P, Sun W, Patel MR, Shah SK, Tramentozzi E, Brooks J, Bolaender A, Shrestha L, Stephani R, Finotti P, Leifer C, Li Z, Gewirth DT, Taldone T, Chiosis G.

J Med Chem. 2015 May 14;58(9):3922-43. doi: 10.1021/acs.jmedchem.5b00197. Epub 2015 Apr 22.


Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70.

Kang Y, Taldone T, Patel HJ, Patel PD, Rodina A, Gozman A, Maharaj R, Clement CC, Patel MR, Brodsky JL, Young JC, Chiosis G.

J Med Chem. 2014 Feb 27;57(4):1188-207. doi: 10.1021/jm401551n. Epub 2014 Feb 18.


Identification of an allosteric pocket on human hsp70 reveals a mode of inhibition of this therapeutically important protein.

Rodina A, Patel PD, Kang Y, Patel Y, Baaklini I, Wong MJ, Taldone T, Yan P, Yang C, Maharaj R, Gozman A, Patel MR, Patel HJ, Chirico W, Erdjument-Bromage H, Talele TT, Young JC, Chiosis G.

Chem Biol. 2013 Dec 19;20(12):1469-80. doi: 10.1016/j.chembiol.2013.10.008. Epub 2013 Nov 14.


Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2.

Patel PD, Yan P, Seidler PM, Patel HJ, Sun W, Yang C, Que NS, Taldone T, Finotti P, Stephani RA, Gewirth DT, Chiosis G.

Nat Chem Biol. 2013 Nov;9(11):677-84. doi: 10.1038/nchembio.1335. Epub 2013 Sep 1.


Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.

Taldone T, Patel PD, Patel M, Patel HJ, Evans CE, Rodina A, Ochiana S, Shah SK, Uddin M, Gewirth D, Chiosis G.

J Med Chem. 2013 Sep 12;56(17):6803-18. doi: 10.1021/jm400619b. Epub 2013 Aug 21.


Discovery and validation of small-molecule heat-shock protein 90 inhibitors through multimodality molecular imaging in living subjects.

Chan CT, Reeves RE, Geller R, Yaghoubi SS, Hoehne A, Solow-Cordero DE, Chiosis G, Massoud TF, Paulmurugan R, Gambhir SS.

Proc Natl Acad Sci U S A. 2012 Sep 11;109(37):E2476-85. doi: 10.1073/pnas.1205459109. Epub 2012 Aug 15.


Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use in flow cytometry and fluorescence microscopy.

Taldone T, Gomes-DaGama EM, Zong H, Sen S, Alpaugh ML, Zatorska D, Alonso-Sabadell R, Guzman ML, Chiosis G.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5347-52. doi: 10.1016/j.bmcl.2011.07.026. Epub 2011 Jul 14.


Design of a flexible cell-based assay for the evaluation of heat shock protein 70 expression modulators.

Ahn JH, Luo W, Kim J, Rodina A, Clement CC, Aguirre J, Sun W, Kang Y, Maharaj R, Moulick K, Zatorska D, Kokoszka M, Brodsky JL, Chiosis G.

Assay Drug Dev Technol. 2011 Jun;9(3):236-46. doi: 10.1089/adt.2010.0327. Epub 2010 Dec 6.


Assay strategies for the discovery and validation of therapeutics targeting Brugia pahangi Hsp90.

Taldone T, Gillan V, Sun W, Rodina A, Patel P, Maitland K, O'Neill K, Chiosis G, Devaney E.

PLoS Negl Trop Dis. 2010 Jun 15;4(6):e714. doi: 10.1371/journal.pntd.0000714.


Synthesis of reblastatin, autolytimycin, and non-benzoquinone analogues: potent inhibitors of heat shock protein 90.

Wrona IE, Gozman A, Taldone T, Chiosis G, Panek JS.

J Org Chem. 2010 May 7;75(9):2820-35. doi: 10.1021/jo1000109.


Cancer and virus leads by HTS, chemical design and SEA data mining.

Thepchatri P, Min J, Ganesh T, Du Y, Lewis I, Kurtkaya S, Prussia A, Li L, Sneed B, Plemper RK, Fu H, Liotta DC, Snyder JP, Dingledine R, Sun A.

Curr Top Med Chem. 2009;9(13):1159-71. Review.


Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.

Ganesh T, Min J, Thepchatri P, Du Y, Li L, Lewis I, Wilson L, Fu H, Chiosis G, Dingledine R, Liotta D, Snyder JP, Sun A.

Bioorg Med Chem. 2008 Jul 15;16(14):6903-10. doi: 10.1016/j.bmc.2008.05.047. Epub 2008 May 27.


Molecular imaging of the efficacy of heat shock protein 90 inhibitors in living subjects.

Chan CT, Paulmurugan R, Gheysens OS, Kim J, Chiosis G, Gambhir SS.

Cancer Res. 2008 Jan 1;68(1):216-26. doi: 10.1158/0008-5472.CAN-07-2268.

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