Literature DB >> 10340605

Synthesis and evaluation of geldanamycin-estradiol hybrids.

S D Kuduk1, F F Zheng, L Sepp-Lorenzino, N Rosen, S J Danishefsky.   

Abstract

Geldanamycin (GDM) binds to the Hsp90 chaperone protein and causes the degradation of several important signalling proteins. A series of novel estradiol-geldanamycin hybrids has been synthesized and evaluated for their ability to induce the selective degradation of the estrogen receptor (ER). The hybrid compounds are active and more selective than the parent causing degradation of ER and HER2, but not other GDM targets.

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Year:  1999        PMID: 10340605     DOI: 10.1016/s0960-894x(99)00185-7

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


  19 in total

1.  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

2.  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

Review 3.  Chemical approaches to controlling intracellular protein degradation.

Authors:  John S Schneekloth; Craig M Crews
Journal:  Chembiochem       Date:  2005-01       Impact factor: 3.164

Review 4.  Heat shock proteins as emerging therapeutic targets.

Authors:  Csaba Sõti; Enikõ Nagy; Zoltán Giricz; László Vígh; Péter Csermely; Péter Ferdinandy
Journal:  Br J Pharmacol       Date:  2005-11       Impact factor: 8.739

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

Authors:  Manikandadas M Madathil; Omar M Khdour; Jennifer Jaruvangsanti; Sidney M Hecht
Journal:  ACS Med Chem Lett       Date:  2013-07-25       Impact factor: 4.345

6.  Biomolecular engineering of intracellular switches in eukaryotes.

Authors:  M K Pastuszka; J A Mackay
Journal:  J Drug Deliv Sci Technol       Date:  2010-05       Impact factor: 3.981

7.  Probing the topological tolerance of multimeric protein interactions: evaluation of an estrogen/synthetic ligand for FK506 binding protein conjugate.

Authors:  Terry W Moore; Jillian R Gunther; John A Katzenellenbogen
Journal:  Bioconjug Chem       Date:  2010-10-20       Impact factor: 4.774

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

Authors:  Ashton C Lai; Craig M Crews
Journal:  Nat Rev Drug Discov       Date:  2016-11-25       Impact factor: 84.694

9.  Chaperone-dependent E3 ubiquitin ligase CHIP mediates a degradative pathway for c-ErbB2/Neu.

Authors:  Wanping Xu; Monica Marcu; Xitong Yuan; Edward Mimnaugh; Cam Patterson; Len Neckers
Journal:  Proc Natl Acad Sci U S A       Date:  2002-09-18       Impact factor: 11.205

10.  Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using "click" chemistry.

Authors:  Robert N Hanson; Edward Hua; David Labaree; Richard B Hochberg; Kyle Proffitt; John M Essigmann; Robert G Croy
Journal:  Org Biomol Chem       Date:  2012-09-25       Impact factor: 3.876

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