ArticleThe Journal of biological chemistry2014
Modification of rifamycin polyketide backbone leads to improved drug activity against rifampicin-resistant Mycobacterium tuberculosis.
Article in The Journal of biological chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 48 citations in OpenAlex.
- Genome assembly, comparative genomics, and identification of genes/pathways underlying plant growth-promoting traits of an actinobacterial strain, Amycolatopsis sp. (BCA-696).Scientific reports · 2024Article
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- Genomic modifications for enhanced antibiotic production in rifamycin derivative-producingFrontiers in antibiotics · 2024Article
- Recent Advances in Genomics-Based Approaches for the Development of Intracellular Bacterial Pathogen Vaccines.Pharmaceutics · 2022Review
- C25-modified rifamycin derivatives with improved activity againstPNAS nexus · 2022Article
- Looking Back toAntibiotics (Basel, Switzerland) · 2021Review
- Article
- Secondary Metabolites of the GenusMolecules (Basel, Switzerland) · 2021Review
- Biosynthesis of the Nuclear Factor of Activated T Cells Inhibitor NFAT-133 inACS chemical biology · 2020Article
- Anti-tubercular derivatives of rhein require activation by the monoglyceride lipase Rv0183.Cell surface (Amsterdam, Netherlands) · 2020Article
- Prediction of Transcription Factors and Their Involvement in Regulating Rifamycin Production inIndian journal of microbiology · 2020Article
- Amycolatopsis pithecelloba sp. nov., a novel actinomycete isolated from roots of Pithecellobium dulce in Thailand.The Journal of antibiotics · 2020Article
- Inhibition of RNA Polymerase by Rifampicin and Rifamycin-Like Molecules.EcoSal Plus · 2020Article
- Discovery of 16-Demethylrifamycins by Removing the Predominant Polyketide Biosynthesis Pathway inApplied and environmental microbiology · 2019Article
- The Quest for Novel Antimicrobial Compounds: Emerging Trends in Research, Development, and Technologies.Antibiotics (Basel, Switzerland) · 2019Review
- Bedaquiline: Fallible Hope Against Drug Resistant Tuberculosis.Indian journal of microbiology · 2017Review
- Structural basis for rifamycin resistance of bacterial RNA polymerase by the three most clinically important RpoB mutations found in Mycobacterium tuberculosis.Molecular microbiology · 2017Article
- Inversion of Extender Unit Selectivity in the Erythromycin Polyketide Synthase by Acyltransferase Domain Engineering.ACS chemical biology · 2017Article
- Genetics and Genomics of the Genus Amycolatopsis.Indian journal of microbiology · 2016Article
- Identification of KasA as the cellular target of an anti-tubercular scaffold.Nature communications · 2016Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rifamycin B, a product of Amycolatopsis mediterranei S699, is the precursor of clinically used antibiotics that are effective against tuberculosis, leprosy, and AIDS-related mycobacterial infections. However, prolonged usage of these antibiotics has resulted in the emergence of rifamycin-resistant strains of Mycobacterium tuberculosis. As part of our effort to generate better analogs of rifamycin, we substituted the acyltransferase domain of module 6 of rifamycin polyketide synthase with that of module 2 of rapamycin polyketide synthase. The resulting mutants (rifAT6::rapAT2) of A. mediterranei S699 produced new rifamycin analogs, 24-desmethylrifamycin B and 24-desmethylrifamycin SV, which contained modification in the polyketide backbone. 24-Desmethylrifamycin B was then converted to 24-desmethylrifamycin S, whose structure was confirmed by MS, NMR, and X-ray crystallography. Subsequently, 24-desmethylrifamycin S was converted to 24-desmethylrifampicin, which showed excellent antibacterial activity against several rifampicin-resistant M. tuberculosis strains.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.