Target-selective degradation of proteins by a light-activated 2-phenylquinoline-estradiol hybrid.
A designed 2-phenylquinoline-estradiol hybrid effectively and selectively degraded the target transcription factor, human estrogen receptor-alpha (hER-alpha), which has a high affinity with the estradiol moiety, under long-wavelength UV photo-irradiation, without additives and under neutral conditions.
Suzuki
Akane
A
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.
Tsumura
Kana
K
Tsuzuki
Takeo
T
Matsumura
Shuichi
S
Toshima
Kazunobu
K
D004958:Estradiol / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000528:radiation effects; D047628:Estrogen Receptor alpha / Q000737:chemistry* / Q000528:radiation effects; D006801:Humans; D008968:Molecular Conformation; D010777:Photochemistry; D011804:Quinolines / Q000737:chemistry* / Q000528:radiation effects; D014466:Ultraviolet Rays
C526991:17-(3-((2-phenylquinolin-4-yl)carbonyloxy)propynyl)estradiol; D047628:Estrogen Receptor alpha; D011804:Quinolines; D004958:Estradiol