Rational design of a new antibiotic class for drug-resistant infections

…, SJ Mayclin, HS Heine, GL Drusano, JE Cummings… - Nature, 2021 - nature.com
The development of new antibiotics to treat infections caused by drug-resistant Gram-negative
pathogens is of paramount importance as antibiotic resistance continues to increase …

Toxin–antitoxin systems and regulatory mechanisms in Mycobacterium tuberculosis

…, CC Dawson, JE Cummings - Pathogens and …, 2018 - academic.oup.com
There has been a significant reduction in annual tuberculosis incidence since the World
Health Organization declared tuberculosis a global health threat. However, treatment of M. …

[HTML][HTML] Rational design of broad spectrum antibacterial activity based on a clinically relevant enoyl-acyl carrier protein (ACP) reductase inhibitor

…, M Tareilus, S Eltschkner, W Yu, JE Cummings… - Journal of Biological …, 2014 - ASBMB
Determining the molecular basis for target selectivity is of particular importance in drug
discovery. The ideal antibiotic should be active against a broad spectrum of pathogenic …

Optimization of TopoIV potency, ADMET properties, and hERG inhibition of 5-amino-1, 3-dioxane-linked novel bacterial topoisomerase inhibitors: Identification of a …

…, LR Duncan, B Roth, JE Cummings… - Journal of Medicinal …, 2021 - ACS Publications
Novel bacterial topoisomerase inhibitors (NBTIs) are among the most promising new antibiotics
in preclinical/clinical development. We previously reported dioxane-linked NBTIs with …

Discovery of a novel type IIb RelBE toxin‐antitoxin system in Mycobacterium tuberculosis defined by co‐regulation with an antisense RNA

CC Dawson, JE Cummings, JM Starkey… - Molecular …, 2022 - Wiley Online Library
Toxin‐antitoxin loci regulate adaptive responses to stresses associated with the host
environment and drug exposure. Phylogenomic studies have shown that Mycobacterium …

Benzimidazole-based antibacterial agents against Francisella tularensis

K Kumar, D Awasthi, SY Lee, JE Cummings… - Bioorganic & medicinal …, 2013 - Elsevier
Francisella tularensis is a highly virulent pathogenic bacterium. In order to identify novel
potential antibacterial agents against F. tularensis, libraries of trisubstituted benzimidazoles …

[HTML][HTML] Structure-activity determinants in Paneth cell α-defensins: loss-of-function in mouse cryptdin-4 by charge-reversal at arginine residue positions

H Tanabe, X Qu, CS Weeks, JE Cummings… - Journal of Biological …, 2004 - ASBMB
Paneth cells secrete microbicidal enteric α-defensins into the small intestinal lumen, and
cryptdin-4 (Crp4) is the most bactericidal of the mouse α-defensin peptides in vitro. Here, site-…

[HTML][HTML] Aggregation and hemi-fusion of anionic vesicles induced by the antimicrobial peptide cryptdin-4

JE Cummings, TK Vanderlick - Biochimica et Biophysica Acta (BBA) …, 2007 - Elsevier
We show that cryptdin-4 (Crp4), an antimicrobial peptide found in mice, induces the aggregation
and hemi-fusion of charged phospholipid vesicles constructed of the anionic lipid POPG …

Thiolactomycin-based inhibitors of bacterial β-ketoacyl-ACP synthases with in vivo activity

…, K Kapilashrami, JE Cummings… - Journal of medicinal …, 2016 - ACS Publications
β-Ketoacyl-ACP synthases (KAS) are key enzymes involved in the type II bacterial fatty acid
biosynthesis (FASII) pathway and are putative targets for antibacterial discovery. Several …

[HTML][HTML] A novel glucocorticoid and androgen receptor modulator reduces viral entry and innate immune inflammatory responses in the Syrian hamster model of SARS …

…, AC Fagre, AS Latham, JE Cummings… - Frontiers in …, 2022 - frontiersin.org
Despite significant research efforts, treatment options for severe acute respiratory syndrome
coronavirus 2 (SARS-CoV-2) remain limited. This is due in part to a lack of therapeutics that …