Development of Photoswitchable Estrogen Receptor Ligands.

Development of Photoswitchable Estrogen Receptor Ligands.
Chem Pharm Bull (Tokyo). 2020;68(4):398-402
Authors: Tsuchiya K, Umeno T, Tsuji G, Yokoo H, Tanaka M, Fukuhara K, Demizu Y, Misawa T
Abstract
Photopharmacology has attracted attention as an approach for the development of novel therapeutics because it allows regulation of the bioactivity of compounds based on their conformational change by photo-irradiation. Previously, we have reported several types of selective estrogen receptor (ER) modulators based on diphenylmethane skeleton. To develop novel photopharmacological reagents, we designed and synthesized a set of ER ligands based on azobenzene skeleton, which can switch its conformation following UV irradiation. Our results showed that after UV irradiation, the Z-form of the synthesized compound 9 interacted with ERα, with a KD value of 2.5 µM, whereas the E-form of compound 9 did not bind ability to ERα at 10 µM.
PMID: 32238658 [PubMed - in process]

Source: Chemical and Pharmaceutical Bulletin - April 4, 2020 Category: Drugs & Pharmacology Authors: Tsuchiya K, Umeno T, Tsuji G, Yokoo H, Tanaka M, Fukuhara K, Demizu Y, Misawa T Tags: Chem Pharm Bull (Tokyo) Source Type: research