High-throughput screening of natural product and synthetic molecule libraries for antibacterial drug discovery

NJ Ayon - Metabolites, 2023 - mdpi.com
Due to the continued emergence of resistance and a lack of new and promising antibiotics,
bacterial infection has become a major public threat. High-throughput screening (HTS) …

Structural and functional features of enzymes of Mycobacterium tuberculosis peptidoglycan biosynthesis as targets for drug development

GL Moraes, GC Gomes, PRM De Sousa, CN Alves… - Tuberculosis, 2015 - Elsevier
Tuberculosis (TB) is the second leading cause of human mortality from infectious diseases
worldwide. The WHO reported 1.3 million deaths and 8.6 million new cases of TB in 2012 …

Inhibitors of the acetyltransferase domain of N-acetylglucosamine-1-phosphate-uridylyltransferase/glucosamine-1-phosphate-acetyltransferase (GlmU). Part 2 …

SS Stokes, R Albert, ET Buurman, B Andrews… - Bioorganic & medicinal …, 2012 - Elsevier
A previously described aryl sulfonamide series, originally found through HTS, targets GlmU,
a bifunctional essential enzyme involved in bacterial cell wall synthesis. Using structure …

Viable screening targets related to the bacterial cell wall

LL Silver - Annals of the New York Academy of Sciences, 2013 - Wiley Online Library
The synthesis of the bacterial peptidoglycan has been recognized for over 50 years as fertile
ground for antibacterial discovery. Initially, empirical screening of natural products for …

Depletion of M. tuberculosis GlmU from Infected Murine Lungs Effects the Clearance of the Pathogen

V Soni, S Upadhayay, P Suryadevara, G Samla… - PLoS …, 2015 - journals.plos.org
M. tuberculosis N-acetyl-glucosamine-1-phosphate uridyltransferase (GlmUMtb) is a bi-
functional enzyme engaged in the synthesis of two metabolic intermediates N …

Design and synthesis of novel cell wall inhibitors of Mycobacterium tuberculosis GlmM and GlmU

Y Li, Y Zhou, Y Ma, X Li - Carbohydrate research, 2011 - Elsevier
GlmM and GlmU are key enzymes in the biosynthesis of UDP-N-acetyl-d-glucosamine (UDP-
GlcNAc), an essential precursor of peptidoglycan and the rhamnose–GlcNAc linker region in …

A high-throughput screen identifies a new natural product with broad-spectrum antibacterial activity

P Ymele-Leki, S Cao, J Sharp, KG Lambert… - PloS one, 2012 - journals.plos.org
Due to the inexorable invasion of our hospitals and communities by drug-resistant bacteria,
there is a pressing need for novel antibacterial agents. Here we report the development of a …

CoA Adducts of 4-Oxo-4-phenylbut-2-enoates: Inhibitors of MenB from the M. tuberculosis Menaquinone Biosynthesis Pathway

X Li, N Liu, H Zhang, SE Knudson, HJ Li… - ACS medicinal …, 2011 - ACS Publications
A high-throughput screen led to the discovery of 2-amino-4-oxo-4-phenylbutanoate
inhibitors of the 1, 4-dihydroxy-2-naphthoyl-CoA synthase (MenB) from the menaquinone …

Insights into the central role of N-acetyl-glucosamine-1-phosphate uridyltransferase (GlmU) in peptidoglycan metabolism and its potential as a therapeutic target

V Soni, EH Rosenn, R Venkataraman - Biochemical Journal, 2023 - portlandpress.com
Several decades after the discovery of the first antibiotic (penicillin) microbes have evolved
novel mechanisms of resistance; endangering not only our abilities to combat future …

UDP-GlcNAc pathway: Potential target for inhibitor discovery against M. tuberculosis

C Rani, IA Khan - European Journal of Pharmaceutical Sciences, 2016 - Elsevier
In the past five years, an alarming increase in the number of patients with multidrug resistant
tuberculosis (MDR TB) and extensively drug-resistant tuberculosis (XDR TB) has been …