Halting ionic shuttle to disrupt the synthetic machinery—Structural and molecular insights into the inhibitory roles of Bedaquiline towards Mycobacterium tuberculosis ATP synthase in the treatment of tuberculosis
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.28891
Abstract: Therapeutic targeting of the adenosine triphosphate (ATP) machinery of Mycobacterium tuberculosis (Mtb) has recently presented a potent and alternative measure to halt the pathogenesis of tuberculosis. This has been potentiated by the development of bedaquiline… read more here.
Keywords: atp synthase; molecule; machinery; bdq ... See more keywords
Defining Bedaquiline Susceptibility, Resistance, Cross-Resistance and Associated Genetic Determinants: A Retrospective Cohort Study
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DOI: 10.1016/j.ebiom.2018.01.005
Abstract: Background Bedaquiline (BDQ) is a novel agent approved for use in combination treatment of multi-drug resistant tuberculosis (MDR-TB). We sought to determine BDQ epidemiological cut-off values (ECVs), define and assess interpretive criteria against putative resistance… read more here.
Keywords: cross resistance; resistance cross; bdq; resistance ... See more keywords
Bedaquiline Phenotypic and Genotypic Susceptibility Testing, Work in Progress!
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DOI: 10.1016/j.ebiom.2018.02.006
Abstract: Criteria to definephenotypic resistance to bedaquiline (BDQ) are not variants were all found among susceptible isolates. All CFZ susceptible well determined and uncertainties around the genetic basis of resistance and cross resistance with clofazimine (CFZ)… read more here.
Keywords: susceptibility testing; susceptibility; bedaquiline; drug ... See more keywords
Bedaquiline inhibits the yeast and human mitochondrial ATP synthases
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DOI: 10.1038/s42003-020-01173-z
Abstract: Bedaquiline (BDQ, Sirturo) has been approved to treat multidrug resistant forms of Mycobacterium tuberculosis. Prior studies suggested that BDQ was a selective inhibitor of the ATP synthase from M. tuberculosis. However, Sirturo treatment leads to… read more here.
Keywords: human mitochondrial; mitochondrial atp; bdq; atp synthases ... See more keywords
Superior Efficacy of a TBI-166, Bedaquiline, and Pyrazinamide Combination Regimen in a Murine Model of Tuberculosis
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DOI: 10.1128/aac.00658-22
Abstract: TBI-166, derived from riminophenazine analogues, shows more potent anti-TB activity than clofazimine and is being assessed against tuberculosis (TB) in a phase IIa clinical trial in China. Preclinical regimen studies containing TBI-166 will support the… read more here.
Keywords: 166 bdq; tbi 166; bdq; activity ... See more keywords
Sudapyridine (WX-081), a Novel Compound against Mycobacterium tuberculosis
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DOI: 10.1128/spectrum.02477-21
Abstract: This study is aimed at chemotherapy for multidrug-resistant tuberculosis (MDR-TB), mainly to develop new anti-TB drugs to kill Mycobacterium tuberculosis, a microorganism with strong drug resistance. In this study, the structure of a potent antituberculosis… read more here.
Keywords: tuberculosis; sudapyridine 081; bdq; resistant tuberculosis ... See more keywords
Variants associated with Bedaquiline (BDQ) resistance identified in Rv0678 and efflux pump genes in Mycobacterium tuberculosis isolates from BDQ naïve TB patients in Pakistan
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DOI: 10.1186/s12866-022-02475-4
Abstract: Background Mutations in the Rv0678 , pepQ and atpE genes of Mycobacterium tuberculosis (MTB) have been reported to be associated with reduced antimycobacterial susceptibility to bedaquiline (BDQ). Resistance conferring mutations in treatment naïve MTB strains… read more here.
Keywords: isolates bdq; resistance; bdq; bdq patients ... See more keywords
Bedaquiline-based treatment for extensively drug-resistant tuberculosis in South Africa: A cost-effectiveness analysis
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DOI: 10.1371/journal.pone.0272770
Abstract: Background The treatment success rate of conventional anti-tuberculosis (TB) regimens for extensively drug-resistant TB (XDR-TB) is low, resulting in high morbidity and healthcare cost especially in the high TB burden countries. Recent clinical findings reported… read more here.
Keywords: cost; bdq; analysis; treatment ... See more keywords
In vitro and Intracellular Antibacterial Activity of Sudapyridine (WX-081) Against Tuberculosis
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DOI: 10.2147/idr.s390187
Abstract: Background Sudapyridine (WX-081) has exhibited equivalent efficacy than its counterpart parent drug bedaquiline (BDQ) but better safety profile against Mycobacterium tuberculosis (Mtb). Our study was aimed to evaluate in vitro activity of WX-081 against the… read more here.
Keywords: tuberculosis; sudapyridine 081; bdq; activity ... See more keywords
Whole Genome Sequencing Identifies Novel Mutations Associated With Bedaquiline Resistance in Mycobacterium tuberculosis
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cellular and Infection Microbiology"
DOI: 10.3389/fcimb.2022.807095
Abstract: Bedaquiline (BDQ), a new antitubercular agent, has been used to treat drug-resistant tuberculosis (TB). Although mutations in atpE, rv0678, and pepQ confer major resistance to BDQ, the mechanisms of resistance to BDQ in vitro and… read more here.
Keywords: genome sequencing; mutations associated; bdq; resistance ... See more keywords
Re-Understanding the Mechanisms of Action of the Anti-Mycobacterial Drug Bedaquiline
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DOI: 10.3390/antibiotics8040261
Abstract: Bedaquiline (BDQ) inhibits ATP generation in Mycobacterium tuberculosis by interfering with the F-ATP synthase activity. Two mechanisms of action of BDQ are broadly accepted. A direct mechanism involves BDQ binding to the enzyme’s c-ring to… read more here.
Keywords: anti mycobacterial; bedaquiline; mechanism; mechanisms action ... See more keywords