Designing novel possible kinase inhibitor derivatives as therapeutics against Mycobacterium tuberculosis: An in silico study.


Journal

Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288

Informations de publication

Date de publication:
13 03 2019
Historique:
received: 08 06 2018
accepted: 18 02 2019
entrez: 15 3 2019
pubmed: 15 3 2019
medline: 29 9 2020
Statut: epublish

Résumé

Rv2984 is one of the polyphosphate kinases present in Mycobacterium tuberculosis involved in the catalytic synthesis of inorganic polyphosphate, which plays an essential role in bacterial virulence and drug resistance. Consequently, the structure of Rv2984 was investigated and an 18 membered compound library was designed by altering the scaffolds of computationally identified inhibitors. The virtual screening of these altered inhibitors was performed against Rv2984 and the top three scoring inhibitors were selected, exhibiting the free energy of binding between 8.2-9 kcal mol

Identifiants

pubmed: 30867456
doi: 10.1038/s41598-019-40621-7
pii: 10.1038/s41598-019-40621-7
pmc: PMC6416319
doi:

Substances chimiques

Antitubercular Agents 0
Protein Kinase Inhibitors 0
Isoniazid V83O1VOZ8L
Rifampin VJT6J7R4TR

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

4405

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Auteurs

Mohd Shahbaaz (M)

South African National Bioinformatics Institute (SANBI), SA Medical Research Council Bioinformatics Unit, University of the Western Cape, Private Bag X17, Bellville, 7535, Cape Town, South Africa.

Anati Nkaule (A)

South African National Bioinformatics Institute (SANBI), SA Medical Research Council Bioinformatics Unit, University of the Western Cape, Private Bag X17, Bellville, 7535, Cape Town, South Africa.

Alan Christoffels (A)

South African National Bioinformatics Institute (SANBI), SA Medical Research Council Bioinformatics Unit, University of the Western Cape, Private Bag X17, Bellville, 7535, Cape Town, South Africa. alan@sanbi.ac.za.

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Classifications MeSH