Journal Article

PUBDB-2021-05007

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics**

Sutherland, M. ; Li, A. ; Kaghad, A. ; Panagopoulos, D. ; Li, F. ; Szewczyk, M. ; Smil, D. ; Scholten, C. ; Bouché, L. ; Stellfeld, T. ; Arrowsmith, C. H. ; Barsyte, D. ; Vedadi, M. ; Hartung, I. V. ; Steuber, H. ; Britton, R. (Corresponding author) ; Santhakumar, V. (Corresponding author)

2021
Wiley-VCH Weinheim [u.a.]

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Please use a persistent id in citations: doi:10.1002/cmdc.202100018  doi:10.3204/PUBDB-2021-05007

Abstract: Protein arginine N-methyl transferase 4 (PRMT4) asymmetricallydimethylates the arginine residues of histone H3 and nonhistoneproteins. The overexpression of PRMT4 in several cancershas stimulated interest in the discovery of inhibitors as biologicaltools and, potentially, therapeutics. Although severalPRMT4 inhibitors have been reported, most display poorselectivity against other members of the PRMT family of methyltransferases. Herein, we report the structure-based design of anew class of alanine-containing 3-arylindoles as potent andselective PRMT4 inhibitors, and describe key structure–activityrelationships for this class of compounds.

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Contributing Institute(s):

1. EMBL-User (EMBL-User)

Research Program(s):

1. 6G3 - PETRA III (DESY) (POF4-6G3) (POF4-6G3)

Experiment(s):

1. PETRA Beamline P13 (PETRA III)

Appears in the scientific report 2021

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Database coverage:
; ; ; BIOSIS Previews ; Biological Abstracts ; Chemical Reactions ; Clarivate Analytics Master Journal List ; Current Contents - Life Sciences ; DEAL Wiley ; Essential Science Indicators ; IF < 5 ; JCR ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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