TY - JOUR
T1 - 7α,11β-disubstituted estrogens
T2 - Probes for the shape of the ligand binding pocket in the estrogen receptor
AU - Tedesco, Rosanna
AU - Katzenellenbogen, John A.
AU - Napolitano, Elio
N1 - Funding Information:
We are grateful for support of this research through grants from the National Institutes of Health (PHS 5R37 DK15556 to J.A.K.), and the Ministero della Ricerca Scientifica e Tecnologica (MURST-Roma) and the Consiglio Nazionale delle Ricerche (CNR-Roma). R.T. gratefully acknowleges the University of Pisa for a fellowship (Bursa di studio per corsi di perfezionamento all'estero). We thank Kathryn E. Carlson for determining the ER binding affinities.
PY - 1997/11/18
Y1 - 1997/11/18
N2 - To investigate whether the estrogen receptor accommodates 7α and 11β substituents on estradiol in two subsites or in a single subsite, we have prepared three sets of ligands bearing single (7α or 11β) or double (7α and 11β) substituents and measured their binding affinity. The different behavior of each set precludes a definitive choice, but supports a two subsite model with some limitations.
AB - To investigate whether the estrogen receptor accommodates 7α and 11β substituents on estradiol in two subsites or in a single subsite, we have prepared three sets of ligands bearing single (7α or 11β) or double (7α and 11β) substituents and measured their binding affinity. The different behavior of each set precludes a definitive choice, but supports a two subsite model with some limitations.
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U2 - 10.1016/S0960-894X(97)10099-3
DO - 10.1016/S0960-894X(97)10099-3
M3 - Article
AN - SCOPUS:0030663411
SN - 0960-894X
VL - 7
SP - 2919
EP - 2924
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 22
ER -