Molecular structural characteristics of estrogen receptor modulators as determinants of estrogen receptor selectivity.
This review will discuss the structural determinants and requirements necessary for estrogen receptors alpha and beta selectivity and ligand-receptor binding affinity. In addition, strategies likely to result in the development of a pharmacophore model that account for the differences in estrogenic effects between different ligands will be discussed.
Agatonovic-Kustrin
S
S
School of Pharmacy and Molecular Sciences, James Cook University, Townsville, Australia.
Turner
J V
JV
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D020847:Estrogen Receptor Modulators / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D004967:Estrogens / Q000737:chemistry; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D011487:Protein Conformation; D011725:Pyridines / Q000737:chemistry; D011960:Receptors, Estrogen / Q000378:metabolism*; D012984:Software; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods*
C506487:ESR1 protein, human; D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D004967:Estrogens; D008024:Ligands; D011725:Pyridines; D011960:Receptors, Estrogen