WebBacterial DNA-dependent RNA polymerase is an attractive drug target because RNA chain elongation is essential for bacterial growth (6, 16).Among those antibiotics discovered in the last 50 years, there are several known, or suspected, inhibitors of bacterial DNA-dependent RNA polymerase that have not been developed and could be candidates for new drugs. WebIt is reported that the RNA polymerase β-subunit encoded by rpoB is a target for rifamycin drugs, and some amino acid changes in this protein can lead to rifamycin resistance. 27–30 Our study showed that 93.7% (119/127 isolates) of RIF-resistant isolates and 95.3% (101/106 isolates) of RFB-resistant isolates harbored at least one mutation in ...
The rifamycins—Relation of chemical structure and action on RNA polymerase
WebRNA polymerase Although not a novel target, the RNA polymerase remains an important drug target in TB chemotherapy research due to the potent bactericidal activity of semisynthetic rifamycins against Mtb, with rifampicin providing one of the most effective treatments for TB [53,54,77]. WebJun 14, 2024 · 8.7. Optimization of non-rifamycin RNA polymerase inhibitors. As the mycobacterial RNA polymerase is a validated drug target, screening for non-rifamycin RNA polymerase inhibitors should also be considered. In a screen of the Medicines for Malaria Venture (MMV) Pathogen Box, Low et al. identified MMV688845 (GSK1729177A) as an … mbti of enhypen
Rifamycin - an overview ScienceDirect Topics
WebMar 16, 2024 · RNA polymerase consists of a core enzyme made up of four polypeptide subunits, and rifampicin specifically binds to the β subunit where it blocks initiation of RNA synthesis, but is without effect on RNA polymerase elongation complexes. ... It is a semisynthetic derivative of rifamycin B, a macrocyclic antibiotic produced by the mold ... WebMar 25, 2024 · RNA polymerase is a multi-unit enzyme that synthesizes RNA molecules from a template of DNA through a process called transcription. The transcription of genetic information into RNA is the first step in gene expression that precedes translation, the process of decoding RNA into proteins. WebJun 7, 2005 · DNA-dependent RNA polymerase (RNAP) catalyzes the transcription of DNA into RNA using the four ribonucleoside triphosphates as substrates. Resistance to the antibiotics salinamide A, salinamide B, rifampicin, streptolydigin, CBR703, myxopyronin, and lipiarmycin can result from mutations in this protein. mbti official website