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Ganetespib and HSP90: translating preclinical hypotheses into clinical promise.

Proia DA, Bates RC.

Cancer Res. 2014 Mar 1;74(5):1294-300. doi: 10.1158/0008-5472.CAN-13-3263. Epub 2014 Feb 20. Review.


Ganetespib, a unique triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy.

Ying W, Du Z, Sun L, Foley KP, Proia DA, Blackman RK, Zhou D, Inoue T, Tatsuta N, Sang J, Ye S, Acquaviva J, Ogawa LS, Wada Y, Barsoum J, Koya K.

Mol Cancer Ther. 2012 Feb;11(2):475-84. doi: 10.1158/1535-7163.MCT-11-0755. Epub 2011 Dec 5.


Recent updates on the development of ganetespib as a Hsp90 inhibitor.

Choi HK, Lee K.

Arch Pharm Res. 2012 Nov;35(11):1855-9. doi: 10.1007/s12272-012-1101-z. Review.


Preclinical activity profile and therapeutic efficacy of the HSP90 inhibitor ganetespib in triple-negative breast cancer.

Proia DA, Zhang C, Sequeira M, Jimenez JP, He S, Spector N, Shapiro GI, Tolaney S, Nagai M, Acquaviva J, Smith DL, Sang J, Bates RC, El-Hariry I.

Clin Cancer Res. 2014 Jan 15;20(2):413-24. doi: 10.1158/1078-0432.CCR-13-2166. Epub 2013 Oct 30.


Targeted inhibition of Hsp90 by ganetespib is effective across a broad spectrum of breast cancer subtypes.

Friedland JC, Smith DL, Sang J, Acquaviva J, He S, Zhang C, Proia DA.

Invest New Drugs. 2014 Feb;32(1):14-24. doi: 10.1007/s10637-013-9971-6. Epub 2013 May 18.


STA-9090, a small-molecule Hsp90 inhibitor for the potential treatment of cancer.

Wang Y, Trepel JB, Neckers LM, Giaccone G.

Curr Opin Investig Drugs. 2010 Dec;11(12):1466-76. Review.


HSP90 inhibitors for cancer therapy and overcoming drug resistance.

Jhaveri K, Modi S.

Adv Pharmacol. 2012;65:471-517. doi: 10.1016/B978-0-12-397927-8.00015-4. Review.


Synergistic activity of the Hsp90 inhibitor ganetespib with taxanes in non-small cell lung cancer models.

Proia DA, Sang J, He S, Smith DL, Sequeira M, Zhang C, Liu Y, Ye S, Zhou D, Blackman RK, Foley KP, Koya K, Wada Y.

Invest New Drugs. 2012 Dec;30(6):2201-9. doi: 10.1007/s10637-011-9790-6. Epub 2012 Jan 10.


Drug-mediated targeted disruption of multiple protein activities through functional inhibition of the Hsp90 chaperone complex.

Stravopodis DJ, Margaritis LH, Voutsinas GE.

Curr Med Chem. 2007;14(29):3122-38. Review.


mTOR inhibition potentiates HSP90 inhibitor activity via cessation of HSP synthesis.

Acquaviva J, He S, Sang J, Smith DL, Sequeira M, Zhang C, Bates RC, Proia DA.

Mol Cancer Res. 2014 May;12(5):703-13. doi: 10.1158/1541-7786.MCR-13-0605. Epub 2014 Feb 19.


A phase II trial of ganetespib, a heat shock protein 90 Hsp90) inhibitor, in patients with docetaxel-pretreated metastatic castrate-resistant prostate cancer (CRPC)-a prostate cancer clinical trials consortium (PCCTC) study.

Thakur MK, Heilbrun LK, Sheng S, Stein M, Liu G, Antonarakis ES, Vaishampayan U, Dzinic SH, Li X, Freeman S, Smith D, Heath EI.

Invest New Drugs. 2016 Feb;34(1):112-8. doi: 10.1007/s10637-015-0307-6. Epub 2015 Nov 18.


Heat-shock protein 90 inhibitors in antineoplastic therapy: is it all wrapped up?

Isaacs JS.

Expert Opin Investig Drugs. 2005 Jun;14(6):569-89. Review.


Antiangiogenic effects of ganetespib in colorectal cancer mediated through inhibition of HIF-1α and STAT-3.

Nagaraju GP, Park W, Wen J, Mahaseth H, Landry J, Farris AB, Willingham F, Sullivan PS, Proia DA, El-Hariry I, Taliaferro-Smith L, Diaz R, El-Rayes BF.

Angiogenesis. 2013 Oct;16(4):903-17. doi: 10.1007/s10456-013-9364-7. Epub 2013 Jul 10. Erratum in: Angiogenesis. 2013 Oct;16(4):919. Ganji, Purnachandra Nagaraju [corrected to Nagaraju, Ganji Purnachandra].


FGFR3 translocations in bladder cancer: differential sensitivity to HSP90 inhibition based on drug metabolism.

Acquaviva J, He S, Zhang C, Jimenez JP, Nagai M, Sang J, Sequeira M, Smith DL, Ogawa LS, Inoue T, Tatsuta N, Knowles MA, Bates RC, Proia DA.

Mol Cancer Res. 2014 Jul;12(7):1042-54. doi: 10.1158/1541-7786.MCR-14-0004. Epub 2014 Apr 30.


Targeting heat-shock protein 90 with ganetespib for molecularly targeted therapy of gastric cancer.

Liu H, Lu J, Hua Y, Zhang P, Liang Z, Ruan L, Lian C, Shi H, Chen K, Tu Z.

Cell Death Dis. 2015 Jan 15;6:e1595. doi: 10.1038/cddis.2014.555.


UDP glucuronosyltransferase 1A expression levels determine the response of colorectal cancer cells to the heat shock protein 90 inhibitor ganetespib.

Landmann H, Proia DA, He S, Ogawa LS, Kramer F, Beißbarth T, Grade M, Gaedcke J, Ghadimi M, Moll U, Dobbelstein M.

Cell Death Dis. 2014 Sep 11;5:e1411. doi: 10.1038/cddis.2014.378.


Heat-shock protein 90 inhibitors as antitumor agents: a survey of the literature from 2005 to 2010.

Messaoudi S, Peyrat JF, Brion JD, Alami M.

Expert Opin Ther Pat. 2011 Oct;21(10):1501-42. doi: 10.1517/13543776.2011.594041. Epub 2011 Jun 21. Review.


NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models.

Jensen MR, Schoepfer J, Radimerski T, Massey A, Guy CT, Brueggen J, Quadt C, Buckler A, Cozens R, Drysdale MJ, Garcia-Echeverria C, Chène P.

Breast Cancer Res. 2008;10(2):R33. doi: 10.1186/bcr1996. Epub 2008 Apr 22.


Drugging the cancer chaperone HSP90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress.

Workman P, Burrows F, Neckers L, Rosen N.

Ann N Y Acad Sci. 2007 Oct;1113:202-16. Epub 2007 May 18. Review.


Activity of the heat shock protein 90 inhibitor ganetespib in melanoma.

Wu X, Marmarelis ME, Hodi FS.

PLoS One. 2013;8(2):e56134. doi: 10.1371/journal.pone.0056134. Epub 2013 Feb 13.

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