GSK2556286 Is a Novel Antitubercular Drug Candidate Effective <i>In Vivo</i> with the Potential To Shorten Tuberculosis Treatment-Reference-Cited by-同舟云学术

GSK2556286 Is a Novel Antitubercular Drug Candidate Effective In Vivo with the Potential To Shorten Tuberculosis Treatment

Published:2022-06-21 Issue:6 Volume:66 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Nuermberger Eric L.¹^ORCID,Martínez-Martínez Maria Santos²,Sanz Olalla²,Urones Beatriz²,Esquivias Jorge²,Soni Heena¹,Tasneen Rokeya¹,Tyagi Sandeep¹,Li Si-Yang¹,Converse Paul J.¹,Boshoff Helena I.³,Robertson Gregory T.⁴^ORCID,Besra Gurdyal S.⁵,Abrahams Katherine A.⁵,Upton Anna M.⁶,Mdluli Khisimuzi⁶,Boyle Gary W.⁷,Turner Sam⁷,Fotouhi Nader⁶,Cammack Nicholas C.²,Siles Juan Miguel²,Alonso Marta²,Escribano Jaime²,Lelievre Joel²,Rullas-Trincado Joaquin²,Pérez-Herrán Esther²,Bates Robert H.²,Maher-Edwards Gareth⁸,Barros David²^ORCID,Ballell Lluís²,Jiménez Elena²

Affiliation:

1. Center for Tuberculosis Research, Division of Infectious Diseases, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA

2. Diseases of the Developing World, GlaxoSmithKline R+D Limited, Tres Cantos, Madrid, Spain

3. Tuberculosis Research Section, Laboratory of Clinical Immunology and Microbiology, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland, USA

4. Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA

5. Institute of Microbiology and Infection, School of Biosciences, University of Birmingham, Birmingham, United Kingdom

6. TB Alliance: Global Alliance for Tuberculosis Drug Development, New York, New York, USA

7. GSK: Research, GlaxoSmithKline R&D, Ware, United Kingdom

8. GSK, Brentford, Middlesex, United Kingdom

Abstract

As a result of a high-throughput compound screening campaign using Mycobacterium tuberculosis -infected macrophages, a new drug candidate for the treatment of tuberculosis has been identified. GSK2556286 inhibits growth within human macrophages (50% inhibitory concentration [IC 50 ] = 0.07 μM), is active against extracellular bacteria in cholesterol-containing culture medium, and exhibits no cross-resistance with known antitubercular drugs.

Funder

Tres Cantos Open Lab Foundation

European Union 7th Framework Program, Orchid

Division of Intramural Research, National Institute of Allergy and Infectious Diseases

Bill and Melinda Gates Foundation

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/aac.00132-22

Reference31 articles.