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primary topic: Structure-Guided Designing and Evaluation of Peptides Targeting Bacterial Transcription

Structure-Guided Designing and Evaluation of Peptides Targeting Bacterial Transcription
type: AcademicArticle
type: Article
abstract: The mycobacterial RNA polymerase (RNAP) is an essential and validated drug target for developing antibacterial drugs. The β-subunit of Mycobacterium tuberculosis (Mtb) RNAP (RpoB) interacts with an essential and global transcription factor, CarD, and confers antibiotic and oxidative stress resistance to Mtb. Compromising the RpoB/CarD interactions results in the killing of mycobacteria, hence disrupting the RpoB/CarD interaction has been proposed as a novel strategy for the development of anti-tubercular drugs. Here, we describe the first approach to rationally design and test the efficacy of the peptide-based inhibitors which specifically target the conserved PPI interface between the bacterial RNAP β/transcription factor complex. We performed in silico protein-peptide docking studies along with biochemical assays to characterize the novel peptide-based inhibitors. Our results suggest that the top ranked peptides are highly stable, soluble in aqueous buffer, and capable of inhibiting transcription with IC50 > 50 μM concentration. Using peptide-based molecules, our study provides the first piece of evidence to target the conserved RNAP β/transcription factor interface for designing new inhibitors. Our results may hence form the basis to further improve the potential of these novel peptides in modulating bacterial gene expression, thus inhibiting bacterial growth and combating bacterial infections.
date: 2020-09-08
volume: 8
is part of: Frontiers in bioengineering and biotechnology
status: peerReviewed
status: published
author list: authors
type: EPrint
type: ArticleEPrint
is part of: repository
subject: QR Microbiology

Frontiers Media S.A.
type: Organization

Frontiers in bioengineering and biotechnology
type: Collection
issn: 22964185

Dipak Dutta
type: Person
given name: Dipak
family name: Dutta

Gundeep Kaur
type: Person
given name: Gundeep
family name: Kaur

Soni Kaundal
type: Person
given name: Soni
family name: Kaundal

Srajan Kapoor
type: Person
given name: Srajan
family name: Kapoor

Krishan Gopal Thakur
type: Person
given name: Krishan Gopal
family name: Thakur

HTML Summary of #2615 Structure-Guided Designing and Evaluation of Peptides Targeting Bacterial Transcription
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primary topic: Structure-Guided Designing and Evaluation of Peptides Targeting Bacterial Transcription

QR Microbiology
type: Concept