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Natural Product Inspired N-Terminal Hsp90 Inhibitors: From Bench to Bedside?

Khandelwal A, Crowley VM, Blagg BS.

Med Res Rev. 2016 Jan;36(1):92-118. doi: 10.1002/med.21351. Review.


The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis.

Brandvold KR, Morimoto RI.

J Mol Biol. 2015 Sep 11;427(18):2931-47. doi: 10.1016/j.jmb.2015.05.010. Review.


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.


The G protein α chaperone Ric-8 as a potential therapeutic target.

Papasergi MM, Patel BR, Tall GG.

Mol Pharmacol. 2015 Jan;87(1):52-63. doi: 10.1124/mol.114.094664. Review.


Anti-tumor activity of WK88-1, a novel geldanamycin derivative, in gefitinib-resistant non-small cell lung cancers with Met amplification.

Jang WJ, Jung SK, Kang JS, Jeong JW, Bae MK, Joo SH, Park GH, Kundu JK, Hong YS, Jeong CH.

Cancer Sci. 2014 Oct;105(10):1245-53. doi: 10.1111/cas.12497.


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.


A purine analog synergizes with chloroquine (CQ) by targeting Plasmodium falciparum Hsp90 (PfHsp90).

Shahinas D, Folefoc A, Taldone T, Chiosis G, Crandall I, Pillai DR.

PLoS One. 2013 Sep 30;8(9):e75446. doi: 10.1371/journal.pone.0075446.


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.


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.


Thermodynamics of aryl-dihydroxyphenyl-thiadiazole binding to human Hsp90.

Kazlauskas E, Petrikaitė V, Michailovienė V, Revuckienė J, Matulienė J, Grinius L, Matulis D.

PLoS One. 2012;7(5):e36899. doi: 10.1371/journal.pone.0036899. Erratum in: PLoS One. 2012;7(6). doi:10.1371/annotation/fb1b3941-789b-4d6f-8463-19a877124f78.


Identifying HER2 inhibitors from natural products database.

Yang SC, Chang SS, Chen CY.

PLoS One. 2011;6(12):e28793. doi: 10.1371/journal.pone.0028793.


Hsp90 as a gatekeeper of tumor angiogenesis: clinical promise and potential pitfalls.

Bohonowych JE, Gopal U, Isaacs JS.

J Oncol. 2010;2010:412985. doi: 10.1155/2010/412985.


A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6-dependent B cell lymphomas.

Cerchietti LC, Lopes EC, Yang SN, Hatzi K, Bunting KL, Tsikitas LA, Mallik A, Robles AI, Walling J, Varticovski L, Shaknovich R, Bhalla KN, Chiosis G, Melnick A.

Nat Med. 2009 Dec;15(12):1369-76. doi: 10.1038/nm.2059.


Purine-scaffold Hsp90 inhibitors.

Taldone T, Chiosis G.

Curr Top Med Chem. 2009;9(15):1436-46. Review.


Different poses for ligand and chaperone in inhibitor-bound Hsp90 and GRP94: implications for paralog-specific drug design.

Immormino RM, Metzger LE 4th, Reardon PN, Dollins DE, Blagg BS, Gewirth DT.

J Mol Biol. 2009 May 22;388(5):1033-42. doi: 10.1016/j.jmb.2009.03.071.


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. Review.


Dynamics of conserved waters in human Hsp90: implications for drug design.

Yan A, Grant GH, Richards WG.

J R Soc Interface. 2008 Dec 6;5 Suppl 3:S199-205. doi: 10.1098/rsif.2008.0331.focus.


Heat shock protein 90 inhibition in lung cancer.

Shimamura T, Shapiro GI.

J Thorac Oncol. 2008 Jun;3(6 Suppl 2):S152-9. doi: 10.1097/JTO.0b013e318174ea3a. Review.


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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