Target intelligence / Profile preview

DNA-directed RNA polymerase beta subunit (bacterial) (RNA polymerase β subunit)

Target
RNA polymerase β subunit
Molecular classification
Enzyme, Transcription factor, DNA-directed RNA polymerase
01

Overview

The DNA-directed RNA polymerase beta subunit (encoded by rpoB) is an essential bacterial enzyme responsible for catalyzing the transcription of DNA into RNA. Rifampicin exerts its antibacterial activity by binding to the beta subunit of bacterial RNA polymerase, specifically in the DNA/RNA channel. This binding blocks RNA chain elongation after the initiation step, preventing the synthesis of bacterial proteins crucial for survival. Resistance to rifampicin typically emerges through mutations in the rpoB gene, particularly in the rifampicin resistance-determining region, which reduce drug binding affinity. Rifampicin does not affect mammalian RNA polymerase, contributing to its selectivity for bacterial pathogens.

Other names
rpoBBacterial RNA polymeraseDNA-dependent RNA polymerase β subunitRNAP β subunit
02

Mechanism of action

Inhibits bacterial DNA-dependent RNA polymerase by binding to its beta subunit, blocking RNA chain elongation and thus impeding bacterial RNA and protein synthesis (steric-occlusion mechanism)

03

Biological functions

TranscriptionProtein synthesis
04

Disease associations

Infection
05

Safety considerations

Rapid emergence of resistance due to point mutations in rpoBDrug interactions (rifampicin induces hepatic enzymes, especially CYP3A4 and CYP2C9, affecting metabolism of many drugs)HepatotoxicityNephrotoxicityHypersensitivity reactionsPossible alteration of color of body fluids (orange-red)
06

Interacting drugs

Rifampicin (rifampin)

1 more in the full profile.

07

Biomarkers

Mutations in the rpoB gene (especially in the rifampicin resistance-determining region, RRDR) for resistance screening

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