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

Hideaki Niwa, Chiduru Watanabe, Shin Sato, Toshiyuki Harada, Hisami Watanabe, Ryo Tabusa, Shunsuke Fukasawa, Ayane Shiobara, Tomoko Hashimoto, Osamu Ohno, Kana Nakamura, Keiko Tsuganezawa, Akiko Tanaka, Mikako Shirouzu, Teruki Honma, Kenji Matsuno, Takashi Umehara

2022ACS Medicinal Chemistry Letters17 citationsDOIOpen Access PDF

Abstract

. The present methodology would be useful when designing covalent-binding inhibitors for other enzymes.

Topics & Concepts

In silicoDemethylaseChemistryHistoneStereochemistryLysineEnzymeCovalent bondComputational biologyBiochemistryBiologyAmino acidGeneOrganic chemistryEpigenetics and DNA MethylationHistone Deacetylase Inhibitors Research
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