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Literature DB >> 10866406

Synthesis and evaluation of geldanamycin-testosterone hybrids.

S D Kuduk¹, T C Harris, F F Zheng, L Sepp-Lorenzino, Q Ouerfelli, N Rosen, S J Danishefsky.

Abstract

Geldanamycin (GDM) binds to the Hsp90 chaperone protein resulting in the degradation of several important signaling proteins. A series of GDM-testosterone linked hybrids has been synthesized and evaluated for activity against prostate cancer cell lines. The hybrid with the greatest activity exhibits potent and selective cytotoxicity against prostate cancer cells containing the androgen receptor.

Entities: Chemical Disease Gene

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Year: 2000 PMID： 10866406 DOI： 10.1016/s0960-894x(00)00208-0

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

16 in total

Review 1. Pharmacological approaches to defining the role of chaperones in aging and prostate cancer progression.

Authors: Sarah A Harvey; Keith O Jensen; Lynne W Elmore; Shawn E Holt
Journal: Cell Stress Chaperones Date: 2002-04 Impact factor: 3.667

2. Impact of linker length on the activity of PROTACs.

Authors: Kedra Cyrus; Marie Wehenkel; Eun-Young Choi; Hyeong-Jun Han; Hyosung Lee; Hollie Swanson; Kyung-Bo Kim
Journal: Mol Biosyst Date: 2010-10-04

3. Design, synthesis, and initial biological evaluation of a steroidal anti-estrogen-doxorubicin bioconjugate for targeting estrogen receptor-positive breast cancer cells.

Authors: Kinh-Luan Dao; Rupa R Sawant; J Adam Hendricks; Victoria Ronga; Vladimir P Torchilin; Robert N Hanson
Journal: Bioconjug Chem Date: 2012-04-04 Impact factor: 4.774

Synthesis and evaluation of geldanamycin-testosterone hybrids.

Review 1. Pharmacological approaches to defining the role of chaperones in aging and prostate cancer progression.

2. Impact of linker length on the activity of PROTACs.

3. Design, synthesis, and initial biological evaluation of a steroidal anti-estrogen-doxorubicin bioconjugate for targeting estrogen receptor-positive breast cancer cells.

Review 4. Chemical approaches to controlling intracellular protein degradation.

Review 5. Heat shock proteins as emerging therapeutic targets.

6. A structurally simplified analogue of geldanamycin exhibits neuroprotective activity.

7. Two-headed PROTAC: an effective new tool for targeted protein degradation.

Review 8. Induced protein degradation: an emerging drug discovery paradigm.

9. Enzyme specific activation of benzoquinone ansamycin prodrugs using HuCC49DeltaCH2-beta-galactosidase conjugates.

10. Characterization of celastrol to inhibit hsp90 and cdc37 interaction.