Re-discovery of PF-3845 as a new chemical scaffold inhibiting phenylalanyl-tRNA synthetase in

Mycobacterium tuberculosis Phenylalanyl-tRNA synthetase aminoacyl tRNA synthetase crystallography high-throughput screening (HTS) inhibition mechanism

Journal

The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R

Informations de publication

Date de publication:
04 Jan 2021
Historique:
accepted: 04 01 2021
received: 27 10 2020
entrez: 5 1 2021
pubmed: 6 1 2021
medline: 6 1 2021
Statut: aheadofprint

Résumé

Mycobacteria tuberculosis (Mtb) remains the deadliest pathogenic bacteria worldwide. The search for new antibiotics to treat drug-sensitive as well as drug-resistant tuberculosis has become a priority. The essential enzyme phenylalanyl-tRNA synthetase (PheRS) is an antibacterial drug target because of the large differences between bacterial and human PheRS counterparts. In a high-throughput screening of 2148 bioactive compounds, PF-3845, which is a known inhibitor of human fatty acid amide hydrolase (FAAH), was identified inhibiting Mtb PheRS at

Identifiants

pubmed: 33397709
pii: RA120.016477
doi: 10.1074/jbc.RA120.016477
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Informations de copyright

Published under license by The American Society for Biochemistry and Molecular Biology, Inc.

Auteurs

Heng Wang (H)

Global Health Drug Discovery Institute, China.

Min Xu (M)

Global Health Drug Discovery Institute, China.

Curtis A Engelhart (CA)

Microbiology & Immunology, Weill Cornell Medical College, United States.

Xi Zhang (X)

Global Health Drug Discovery Institute, China.

Baohua Yan (B)

Tsinghua University, China.

Miaomiao Pan (M)

Global Health Drug Discovery Institute, China.

Yuanyuan Xu (Y)

Global Health Drug Discovery Institute, China.

Shilong Fan (S)

Tsinghua University, China.

Renhe Liu (R)

Global Health Drug Discovery Institute, China.

Lan Xu (L)

Global Health Drug Discovery Institute, China.

Lan Hua (L)

Global Health Drug Discovery Institute, China.

Dirk Schnappinger (D)

Weill Cornell Medical College.

Shawn Chen (S)

Global Health Drug Discovery Institute, China.

Classifications MeSH