Target Validation Information
Target ID T18477
Target Name Heat shock protein HSP 90
Target Type
Clinical Trial
Drug Potency against Target ZEARALANONE Drug Info IC50 = 2197.6 nM [531262]
RHEIN Drug Info IC50 = 3339.3 nM [531262]
GNF-PF-67 Drug Info IC50 < 1875 nM [531262]
Tanespimycin Drug Info IC50 = 33 nM [552619]
Alvespimycin hydrochloride Drug Info IC50 = 68 nM [536622]
VER-49009 Drug Info IC50 = 25 nM [527601]
Retaspimycin Drug Info IC50 = 80000 nM [552871]
Ganetespib Drug Info IC50 < 36 nM
Action against Disease Model Retaspimycin IPI-504 induces cytotoxicity in MM cells in a dose-dependent manner with an EC50 of growth inhibition of about 300 nM after 72 h incubation [552716] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations To study the role of Hsp90|??, an endoplasmic chaperone, we have built a conditional knockout by crossing Hsp90|??(flox/flox) with the Vasa-Cre transgenic line. Spermatozoa deficient in Hsp90|?? could not naturally fertilize oocytes and exhibited large and globular heads with abnormal intermediate pieces, a phenotype reminiscent of h uMan globozoospermia. [552716]
References
Ref 552716IPI-504, a novel and soluble HSP-90 inhibitor, blocks the unfolded protein response in multiple myeloma cells. Cancer Chemother Pharmacol. 2008 May;61(6):923-32. Epub 2007 Jul 12.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 552619Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site. Curr Top Med Chem. 2006;6(11):1173-82.
Ref 536622Stage 1 testing and pharmacodynamic evaluation of the HSP90 inhibitor alvespimycin (17-DMAG, KOS-1022) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jul;51(1):34-41.
Ref 527601J Med Chem. 2005 Jun 30;48(13):4212-5.Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.
Ref 552871Recent advances in the research of HIV-1 RNase H inhibitors. Mini Rev Med Chem. 2008 Oct;8(12):1243-51.

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