Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as


Journal

ACS infectious diseases
ISSN: 2373-8227
Titre abrégé: ACS Infect Dis
Pays: United States
ID NLM: 101654580

Informations de publication

Date de publication:
11 06 2021
Historique:
pubmed: 1 5 2021
medline: 24 6 2021
entrez: 30 4 2021
Statut: ppublish

Résumé

Prolyl-tRNA synthetase (PRS) is a clinically validated antimalarial target. Screening of a set of PRS ATP-site binders, initially designed for human indications, led to identification of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives representing a novel antimalarial scaffold. Evidence designates cytoplasmic PRS as the drug target. The frontrunner

Identifiants

pubmed: 33929818
doi: 10.1021/acsinfecdis.1c00020
pmc: PMC8204304
doi:

Substances chimiques

Antimalarials 0
Amino Acyl-tRNA Synthetases EC 6.1.1.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1680-1689

Subventions

Organisme : Wellcome Trust
Pays : United Kingdom
Organisme : Wellcome Trust
ID : 100993/B/13/Z
Pays : United Kingdom

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Auteurs

Masanori Okaniwa (M)

Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.

Akira Shibata (A)

Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.

Atsuko Ochida (A)

Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.

Yuichiro Akao (Y)

Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan.

Karen L White (KL)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.

David M Shackleford (DM)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.

Sandra Duffy (S)

Discovery Biology, Griffith University, Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia.

Leonardo Lucantoni (L)

Discovery Biology, Griffith University, Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia.

Sumanta Dey (S)

Department of Biological Engineering, Massachusetts Institute of Technology, 77 Massachusetts Ave., Cambridge, Massachusetts 02139, United States.

Josefine Striepen (J)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.

Tomas Yeo (T)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.

Sachel Mok (S)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.

Anna Caroline C Aguiar (ACC)

Sao Carlos Institute of Physics, University of São Paulo, Av. João Dagnone, 1100, São Carlos, São Paulo 13563-120, Brazil.

Angelika Sturm (A)

TropIQ Health Sciences, Transistorweg 5-C02, 6534 AT Nijmegen, The Netherlands.

Benigno Crespo (B)

Global Health, GlaxoSmithKline R&D, Tres Cantos, Madrid 28760, Spain.

Laura M Sanz (LM)

Global Health, GlaxoSmithKline R&D, Tres Cantos, Madrid 28760, Spain.

Alisje Churchyard (A)

Department of Life Sciences, Imperial College London, South Kensington, London, SW7 2AZ, United Kingdom.

Jake Baum (J)

Department of Life Sciences, Imperial College London, South Kensington, London, SW7 2AZ, United Kingdom.

Dhelio B Pereira (DB)

Tropical Medicine Research Center of Rondonia, Av. Guaporé, 215, Porto Velho, Rondonia 76812-329, Brazil.

Rafael V C Guido (RVC)

Sao Carlos Institute of Physics, University of São Paulo, Av. João Dagnone, 1100, São Carlos, São Paulo 13563-120, Brazil.

Koen J Dechering (KJ)

TropIQ Health Sciences, Transistorweg 5-C02, 6534 AT Nijmegen, The Netherlands.

Sergio Wittlin (S)

Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
University of Basel, 4002 Basel, Switzerland.

Anne-Catrin Uhlemann (AC)

Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, New York 10032, United States.

David A Fidock (DA)

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Division of Infectious Diseases, Department of Medicine, Columbia University Irving Medical Center, New York, New York 10032, United States.

Jacquin C Niles (JC)

Department of Biological Engineering, Massachusetts Institute of Technology, 77 Massachusetts Ave., Cambridge, Massachusetts 02139, United States.

Vicky M Avery (VM)

Discovery Biology, Griffith University, Brisbane Innovation Park, Don Young Road, Nathan, Queensland 4111, Australia.

Susan A Charman (SA)

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.

Benoît Laleu (B)

Medicines for Malaria Venture, ICC, Route de Pré-Bois 20, 1215 Geneva, Switzerland.

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Classifications MeSH