Synthesis and evaluation of geldanamycin-estradiol hybrids Academic Article Article uri icon

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.

publication date

  • May 3, 1999

Research

keywords

  • Academic Article

Identity

Digital Object Identifier (DOI)

  • 10.1016/S0960-894X(99)00185-7

PubMed ID

  • 10340605

Additional Document Info

start page

  • 1233

end page

  • 8

volume

  • 9

number

  • 9