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Items: 20

1.

Discovery of Dual Inhibitors of MDM2 and XIAP for Cancer Treatment.

Gu L, Zhang H, Liu T, Zhou S, Du Y, Xiong J, Yi S, Qu CK, Fu H, Zhou M.

Cancer Cell. 2016 Oct 10;30(4):623-636. doi: 10.1016/j.ccell.2016.08.015. Epub 2016 Sep 22.

PMID:
27666947
2.

Broad targeting of resistance to apoptosis in cancer.

Mohammad RM, Muqbil I, Lowe L, Yedjou C, Hsu HY, Lin LT, Siegelin MD, Fimognari C, Kumar NB, Dou QP, Yang H, Samadi AK, Russo GL, Spagnuolo C, Ray SK, Chakrabarti M, Morre JD, Coley HM, Honoki K, Fujii H, Georgakilas AG, Amedei A, Niccolai E, Amin A, Ashraf SS, Helferich WG, Yang X, Boosani CS, Guha G, Bhakta D, Ciriolo MR, Aquilano K, Chen S, Mohammed SI, Keith WN, Bilsland A, Halicka D, Nowsheen S, Azmi AS.

Semin Cancer Biol. 2015 Dec;35 Suppl:S78-103. doi: 10.1016/j.semcancer.2015.03.001. Epub 2015 Apr 28. Review.

3.

Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.

Gavenonis J, Jonas NE, Kritzer JA.

Bioorg Med Chem. 2014 Aug 1;22(15):3989-93. doi: 10.1016/j.bmc.2014.06.006. Epub 2014 Jun 14.

4.

A repurposing strategy for Hsp90 inhibitors demonstrates their potency against filarial nematodes.

Gillan V, O'Neill K, Maitland K, Sverdrup FM, Devaney E.

PLoS Negl Trop Dis. 2014 Feb 13;8(2):e2699. doi: 10.1371/journal.pntd.0002699. eCollection 2014 Feb.

5.

Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70.

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

J Med Chem. 2014 Feb 27;57(4):1208-24. doi: 10.1021/jm401552y. Epub 2014 Feb 18.

6.

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.

7.

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.

8.

Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes.

Taldone T, Rodina A, Dagama Gomes EM, Riolo M, Patel HJ, Alonso-Sabadell R, Zatorska D, Patel MR, Kishinevsky S, Chiosis G.

Beilstein J Org Chem. 2013 Mar 15;9:544-56. doi: 10.3762/bjoc.9.60. Print 2013.

9.

Structurally modified curcumin analogs inhibit STAT3 phosphorylation and promote apoptosis of human renal cell carcinoma and melanoma cell lines.

Bill MA, Nicholas C, Mace TA, Etter JP, Li C, Schwartz EB, Fuchs JR, Young GS, Lin L, Lin J, He L, Phelps M, Li PK, Lesinski GB.

PLoS One. 2012;7(8):e40724. doi: 10.1371/journal.pone.0040724. Epub 2012 Aug 10.

10.

Advances in the discovery and development of heat-shock protein 90 inhibitors for cancer treatment.

Patel HJ, Modi S, Chiosis G, Taldone T.

Expert Opin Drug Discov. 2011 May;6(5):559-587.

11.

High throughput screens yield small molecule inhibitors of Leishmania CRK3:CYC6 cyclin-dependent kinase.

Walker RG, Thomson G, Malone K, Nowicki MW, Brown E, Blake DG, Turner NJ, Walkinshaw MD, Grant KM, Mottram JC.

PLoS Negl Trop Dis. 2011 Apr 5;5(4):e1033. doi: 10.1371/journal.pntd.0001033.

12.

Design, synthesis, and evaluation of small molecule Hsp90 probes.

Taldone T, Zatorska D, Patel PD, Zong H, Rodina A, Ahn JH, Moulick K, Guzman ML, Chiosis G.

Bioorg Med Chem. 2011 Apr 15;19(8):2603-14. doi: 10.1016/j.bmc.2011.03.013. Epub 2011 Mar 12. Review.

13.

A dual-readout F2 assay that combines fluorescence resonance energy transfer and fluorescence polarization for monitoring bimolecular interactions.

Du Y, Nikolovska-Coleska Z, Qui M, Li L, Lewis I, Dingledine R, Stuckey JA, Krajewski K, Roller PP, Wang S, Fu H.

Assay Drug Dev Technol. 2011 Aug;9(4):382-93. doi: 10.1089/adt.2010.0292. Epub 2011 Mar 11.

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.

15.

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.

16.

Biophysical characterization of recombinant proteins: a key to higher structural genomics success.

Vedadi M, Arrowsmith CH, Allali-Hassani A, Senisterra G, Wasney GA.

J Struct Biol. 2010 Oct;172(1):107-19. doi: 10.1016/j.jsb.2010.05.005. Epub 2010 May 11. Review.

17.

Development of fluorescence polarization assays for the molecular chaperone Hsp70 family members: Hsp72 and DnaK.

Ricci L, Williams KP.

Curr Chem Genomics. 2008 Dec 30;2:90-5. doi: 10.2174/1875397300802010090.

18.

Discovery and development of heat shock protein 90 inhibitors.

Taldone T, Sun W, Chiosis G.

Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. doi: 10.1016/j.bmc.2008.10.087. Epub 2008 Nov 6. Review.

19.

Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.

Ganesh T, Thepchatri P, Li L, Du Y, Fu H, Snyder JP, Sun A.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4982-7. doi: 10.1016/j.bmcl.2008.08.022. Epub 2008 Aug 14.

20.

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.

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