Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
23 Nov 2023
Historique:
medline: 24 11 2023
pubmed: 10 11 2023
entrez: 10 11 2023
Statut: ppublish

Résumé

There is an urgent need for new tuberculosis (TB) treatments, with novel modes of action, to reduce the incidence/mortality of TB and to combat resistance to current treatments. Through both chemical and genetic methodologies, polyketide synthase 13 (Pks13) has been validated as essential for mycobacterial survival and as an attractive target for

Identifiants

pubmed: 37948640
doi: 10.1021/acs.jmedchem.3c01514
pmc: PMC10683028
doi:

Substances chimiques

Polyketide Synthases 79956-01-7
Antitubercular Agents 0
Benzofurans 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

15380-15408

Subventions

Organisme : Wellcome Trust
Pays : United Kingdom

Références

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Auteurs

Simon R Green (SR)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Caroline Wilson (C)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Thomas C Eadsforth (TC)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Avinash S Punekar (AS)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Fabio K Tamaki (FK)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Gavin Wood (G)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Nicola Caldwell (N)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Barbara Forte (B)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Neil R Norcross (NR)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Michael Kiczun (M)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

John M Post (JM)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Eva Maria Lopez-Román (EM)

Global Health Medicines R&D, GlaxoSmithKline, Severo Ochoa 2, Tres Cantos, 28760 Madrid Spain.

Curtis A Engelhart (CA)

Department of Microbiology and Immunology, Weill Cornell Medical College, New York, New York 10065, United States.

Iva Lukac (I)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Fabio Zuccotto (F)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Ola Epemolu (O)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Helena I M Boshoff (HIM)

Tuberculosis Research Section, Laboratory of Clinical Immunology and Microbiology, NIAID, National Institutes of Health, 9000 Rockville Pike, Bethesda, Maryland 20892, United States.

Dirk Schnappinger (D)

Department of Microbiology and Immunology, Weill Cornell Medical College, New York, New York 10065, United States.

Chris Walpole (C)

Structural Genomics Consortium, Research Institute of the McGill University Health Centre, 1001 Boulevard Décarie, Site Glen Block E, ES1.1614, Montréal, QC H4A 3J1, Canada.

Ian H Gilbert (IH)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Kevin D Read (KD)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Paul G Wyatt (PG)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

Beatriz Baragaña (B)

Drug Discovery Unit, Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, Dundee DD1 5EH, U.K.

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Classifications MeSH