Literature DB >> 24563587

Bedaquiline - The first ATP synthase inhibitor against multi drug resistant tuberculosis.

Mageshwaran Lakshmanan1, Alphienes Stanley Xavier1.   

Abstract

Increasing incidence of MDR-TB, long duration of treatment and co-infection with HIV are the significant problems in achieving the eradication of tuberculosis. Bedaquiline is an anti-tuberculosis drug with unique mechanism of action. It selectively inhibits the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis like active, dormant, replicating, non-replicating, intracellular and extracellular. Preclinical studies have shown the efficacy of bedaquiline in terms of reduction in bacterial load and treatment duration. Phase II clinical studies have established the safety, tolerability and earlier sputum conversion time in patients with MDR-TB. In 2012 FDA approved bedaquiline for treatment of MDR-TB and XDR-TB.

Entities:  

Keywords:  ATP synthase inhibitor; Bedaquiline; MDR-TB; Tuberculosis; XDR-TB

Year:  2013        PMID: 24563587      PMCID: PMC3930122          DOI: 10.1016/j.jyp.2013.12.002

Source DB:  PubMed          Journal:  J Young Pharm        ISSN: 0975-1483


  26 in total

1.  The diarylquinoline TMC207 for multidrug-resistant tuberculosis.

Authors:  Andreas H Diacon; Alexander Pym; Martin Grobusch; Ramonde Patientia; Roxana Rustomjee; Liesl Page-Shipp; Christoffel Pistorius; Rene Krause; Mampedi Bogoshi; Gavin Churchyard; Amour Venter; Jenny Allen; Juan Carlos Palomino; Tine De Marez; Rolf P G van Heeswijk; Nacer Lounis; Paul Meyvisch; Johan Verbeeck; Wim Parys; Karel de Beule; Koen Andries; David F Mc Neeley
Journal:  N Engl J Med       Date:  2009-06-04       Impact factor: 91.245

2.  ATP synthase inhibition of Mycobacterium avium is not bactericidal.

Authors:  Nacer Lounis; Tom Gevers; Joke Van den Berg; Luc Vranckx; Koen Andries
Journal:  Antimicrob Agents Chemother       Date:  2009-09-08       Impact factor: 5.191

3.  The F1Fo-ATP synthase of Mycobacterium smegmatis is essential for growth.

Authors:  Sieu L Tran; Gregory M Cook
Journal:  J Bacteriol       Date:  2005-07       Impact factor: 3.490

4.  Randomized pilot trial of eight weeks of bedaquiline (TMC207) treatment for multidrug-resistant tuberculosis: long-term outcome, tolerability, and effect on emergence of drug resistance.

Authors:  A H Diacon; P R Donald; A Pym; M Grobusch; R F Patientia; R Mahanyele; N Bantubani; R Narasimooloo; T De Marez; R van Heeswijk; N Lounis; P Meyvisch; K Andries; D F McNeeley
Journal:  Antimicrob Agents Chemother       Date:  2012-03-05       Impact factor: 5.191

5.  A computational model of the inhibition of Mycobacterium tuberculosis ATPase by a new drug candidate R207910.

Authors:  Marc R de Jonge; Luc H M Koymans; Jérôme E G Guillemont; Anil Koul; Koen Andries
Journal:  Proteins       Date:  2007-06-01

6.  Activities of TMC207, rifampin, and pyrazinamide against Mycobacterium tuberculosis infection in guinea pigs.

Authors:  Shaobin Shang; Crystal A Shanley; Megan L Caraway; Eileen A Orme; Marcela Henao-Tamayo; Laurel Hascall-Dove; David Ackart; Anne J Lenaerts; Randall J Basaraba; Ian M Orme; Diane J Ordway
Journal:  Antimicrob Agents Chemother       Date:  2010-10-11       Impact factor: 5.191

7.  Location of persisting mycobacteria in a Guinea pig model of tuberculosis revealed by r207910.

Authors:  Anne J Lenaerts; Donald Hoff; Sahar Aly; Stefan Ehlers; Koen Andries; Luis Cantarero; Ian M Orme; Randall J Basaraba
Journal:  Antimicrob Agents Chemother       Date:  2007-05-21       Impact factor: 5.191

8.  Lymphadenitis as a major element of disease in the guinea pig model of tuberculosis.

Authors:  Randall J Basaraba; Deanna D Dailey; Christine T McFarland; Crystal A Shanley; Erin E Smith; David N McMurray; Ian M Orme
Journal:  Tuberculosis (Edinb)       Date:  2006-02-10       Impact factor: 3.131

9.  Probing the interaction of the diarylquinoline TMC207 with its target mycobacterial ATP synthase.

Authors:  Anna C Haagsma; Ioana Podasca; Anil Koul; Koen Andries; Jerome Guillemont; Holger Lill; Dirk Bald
Journal:  PLoS One       Date:  2011-08-17       Impact factor: 3.240

10.  Unique flexibility in energy metabolism allows mycobacteria to combat starvation and hypoxia.

Authors:  Michael Berney; Gregory M Cook
Journal:  PLoS One       Date:  2010-01-07       Impact factor: 3.240

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  14 in total

Review 1.  The c-Ring of the F1FO-ATP Synthase: Facts and Perspectives.

Authors:  Salvatore Nesci; Fabiana Trombetti; Vittoria Ventrella; Alessandra Pagliarani
Journal:  J Membr Biol       Date:  2015-11-30       Impact factor: 1.843

2.  Bedaquiline.

Authors:  Sebastiaan C Goulooze; Adam F Cohen; Robert Rissmann
Journal:  Br J Clin Pharmacol       Date:  2015-07-02       Impact factor: 4.335

Review 3.  Potential anti-TB investigational compounds and drugs with repurposing potential in TB therapy: a conspectus.

Authors:  Adetomiwa A Adeniji; Kirsten E Knoll; Du Toit Loots
Journal:  Appl Microbiol Biotechnol       Date:  2020-05-05       Impact factor: 4.813

4.  New approach to develop ultra-high inhibitory drug using the power function of the stoichiometry of the targeted nanomachine or biocomplex.

Authors:  Dan Shu; Fengmei Pi; Chi Wang; Peng Zhang; Peixuan Guo
Journal:  Nanomedicine (Lond)       Date:  2015-07       Impact factor: 5.307

Review 5.  A Pharmacology Perspective of Simultaneous Tuberculosis and Hepatitis C Treatment.

Authors:  Russell R Kempker; Wael A Alghamdi; Mohammad H Al-Shaer; Gena Burch; Charles A Peloquin
Journal:  Antimicrob Agents Chemother       Date:  2019-10-07       Impact factor: 5.191

6.  Discovery of a new method for potent drug development using power function of stoichiometry of homomeric biocomplexes or biological nanomotors.

Authors:  Fengmei Pi; Mario Vieweger; Zhengyi Zhao; Shaoying Wang; Peixuan Guo
Journal:  Expert Opin Drug Deliv       Date:  2015-08-24       Impact factor: 6.648

Review 7.  Development of Potent Antiviral Drugs Inspired by Viral Hexameric DNA-Packaging Motors with Revolving Mechanism.

Authors:  Fengmei Pi; Zhengyi Zhao; Venkata Chelikani; Kristine Yoder; Mamuka Kvaratskhelia; Peixuan Guo
Journal:  J Virol       Date:  2016-08-26       Impact factor: 5.103

8.  Identification of Potential Binders of Mtb Universal Stress Protein (Rv1636) Through an in silico Approach and Insights Into Compound Selection for Experimental Validation.

Authors:  Sohini Chakraborti; Moubani Chakraborty; Avipsa Bose; Narayanaswamy Srinivasan; Sandhya S Visweswariah
Journal:  Front Mol Biosci       Date:  2021-05-03

9.  Identification and Validation of Aspartic Acid Semialdehyde Dehydrogenase as a New Anti-Mycobacterium Tuberculosis Target.

Authors:  Jianzhou Meng; Yanhui Yang; Chunling Xiao; Yan Guan; Xueqin Hao; Qi Deng; Zhongyang Lu
Journal:  Int J Mol Sci       Date:  2015-09-30       Impact factor: 5.923

10.  Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds.

Authors:  Chunxian He; Laura Preiss; Bin Wang; Lei Fu; Hui Wen; Xiang Zhang; Huaqing Cui; Thomas Meier; Dali Yin
Journal:  ChemMedChem       Date:  2016-10-28       Impact factor: 3.466

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