Development of Photoswitchable Estrogen Receptor Ligands

Keisuke Tsuchiya, Tomohiro Umeno, Genichiro Tsuji, Hidetomo Yokoo, Masakazu Tanaka, Kiyoshi Fukuhara, Yosuke Demizu, Takashi Misawa
2020 Chemical and pharmaceutical bulletin  
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
more » ... ion 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.
doi:10.1248/cpb.c19-01108 pmid:32238658 fatcat:3epp5ky7f5egfndv5tavfhy2sq