title: Discovery and total synthesis of a new estrogen receptor heterodimerizing actinopolymorphol A from Actinopolymorpha rutilus.
abstract: Estrogen receptor ERalpha and ERbeta heterodimerization has been implicated in cancer chemoprevention. The discovery, structural elucidation, and total synthesis of a new natural product, actinopolymorphol A (1), from Actinopolymorpha rutilus (YIM45725) that preferentially induces ERalpha/beta heterodimerization is reported. Total synthesis of 1 has allowed us to determine its absolute stereochemistry and that of a previously known deacetylated congener, and 1 represents the first member of a new class of natural products not previously recognized to modulate ER function.
authors.affiliation: Division of Pharmaceutical Sciences, University of Wisconsin-Madison, Madison, Wisconsin 53705, USA.
authors.forename: Sheng-Xiong
authors.initials: SX
authors.lastname: Huang
authors.forename: Emily
authors.initials: E
authors.lastname: Powell
authors.forename: Scott R
authors.initials: SR
authors.lastname: Rajski
authors.forename: Li-Xing
authors.initials: LX
authors.lastname: Zhao
authors.forename: Cheng-Lin
authors.initials: CL
authors.lastname: Jiang
authors.forename: Yanwen
authors.initials: Y
authors.lastname: Duan
authors.forename: Wei
authors.initials: W
authors.lastname: Xu
authors.forename: Ben
authors.initials: B
authors.lastname: Shen
mesh_terms: D000085:Acetates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000192:Actinomycetales / Q000737:chemistry*; D020847:Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D047629:Estrogen Receptor beta / Q000378:metabolism*; D015394:Molecular Structure; D010636:Phenols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000085:Acetates; D020847:Estrogen Receptor Modulators; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D010636:Phenols; C552534:actinopolymorphol A