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Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2

[Image: see text] trans-2-Phenylcycloproylamine (trans-PCPA) has been used as the scaffold to develop covalent-binding inhibitors against lysine-specific demethylase 1 (LSD1/KDM1A), a therapeutic target for several cancers. However, the effects of different structural moieties on the inhibitory acti...

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Detalles Bibliográficos
Autores principales: Niwa, Hideaki, Watanabe, Chiduru, Sato, Shin, Harada, Toshiyuki, Watanabe, Hisami, Tabusa, Ryo, Fukasawa, Shunsuke, Shiobara, Ayane, Hashimoto, Tomoko, Ohno, Osamu, Nakamura, Kana, Tsuganezawa, Keiko, Tanaka, Akiko, Shirouzu, Mikako, Honma, Teruki, Matsuno, Kenji, Umehara, Takashi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9465824/
https://www.ncbi.nlm.nih.gov/pubmed/36105323
http://dx.doi.org/10.1021/acsmedchemlett.2c00294