Small molecule inhibitors of bacterial condensins

NIH RePORTER · NIH · R21 · $193,750 · view on reporter.nih.gov ↗

Abstract

Small molecule inhibitors of bacterial condensins ABSTRACT The emergence and spread of antibiotic resistant pathogenic bacteria presents a rapidly expanding threat to public health. Among enteric bacteria, in particular, several species have evolved that are resistant to all presently available antibiotics resulting in high mortality rates among affected patients. This proposal aims to develop bacterial condensins as a novel antimicrobial drug target. Condensins play a central role in chromosome organization, an essential cellular function, and are required for cell viability and pathogenicity in a diverse range of organisms. Bacterial and eukaryotic condensins display sufficient sequence divergence to expect the existence of highly selective inhibitors. The applicant has recently developed and validated a novel high throughput screening cascade for condensin inhibitors. This proposal seeks to perform the screen on a large library of compounds and natural products. The results will likely yield novel chemical probes for chromosome biology and new chemical scaffolds against a novel target suitable for further preclinical development.

Key facts

NIH application ID
9964657
Project number
5R21AI141927-02
Recipient
UNIVERSITY OF OKLAHOMA
Principal Investigator
VALENTIN V RYBENKOV
Activity code
R21
Funding institute
NIH
Fiscal year
2020
Award amount
$193,750
Award type
5
Project period
2019-07-01 → 2022-06-30