Synthesis and evaluation of geldanamycin-estradiol hybrids
Academic ArticleArticle
Overview
MeSH Major
Antineoplastic Combined Chemotherapy Protocols
HSP90 Heat-Shock Proteins
Neoplasms
Proto-Oncogene Proteins
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.
