Synthesis and evaluation of geldanamycin-estradiol hybrids Journal Article


Authors: Kuduk, S. D.; Zheng, F. F.; Sepp-Lorenzino, L.; Rosen, N.; Danishefsky, S. J.
Article Title: Synthesis and evaluation of geldanamycin-estradiol hybrids
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.
Keywords: protein degradation; protein targeting; protein binding; drug structure; tumor cells, cultured; drug synthesis; enzyme inhibitors; hsp90 heat-shock proteins; quinones; down regulation; receptors, estrogen; estrogen receptor; inhibitory concentration 50; estradiol; reaction analysis; models, chemical; chemical reaction; benzoquinones; lactams, macrocyclic; geldanamycin; chaperone; hybridization; humans; article; streptomyces hygroscopicus
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 9
Issue: 9
ISSN: 0960-894X
Publisher: Pergamon-Elsevier Science Ltd  
Date Published: 1999-05-03
Start Page: 1233
End Page: 1238
Language: English
DOI: 10.1016/s0960-894x(99)00185-7
PUBMED: 10340605
PROVIDER: scopus
DOI/URL:
Notes: Article -- Export Date: 16 August 2016 -- Source: Scopus
Altmetric Score
MSK Authors
  1. Neal Rosen
    364 Rosen
  2. Fuzhong F Zheng
    11 Zheng
  3. Scott D Kuduk
    21 Kuduk