A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors

A unique binding pocket induced by a noncanonical SAH mimic to develop potent and selective PRMT inhibitors

Protein arginine methyltransferases (PRMTs) are attractive targets for developing therapeutic agents, but selective PRMT inhibitors targeting the cofactor SAM binding site are limited. Herein, we report the discovery of a noncanonical but less polar SAH surrogate YD1113 by replacing the benzyl guani...

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Bibliographic Details
Main Authors: Youchao Deng, Xiaosheng Song, Iredia D. Iyamu, Aiping Dong, Jinrong Min, Rong Huang
Format: Article
Language:English
Published: Elsevier 2023-12-01
Series:Acta Pharmaceutica Sinica B
Subjects:
PRMTs
Structure based inhibitor design
Benzyl urea
Noncanonical SAH mimic
Homocysteine binding pocket
Crystal structure
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383523002848

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http://www.sciencedirect.com/science/article/pii/S2211383523002848

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