A structural-chemical explanation of fungal laccase activity
Abstract Fungal laccases (EC 1.10. 3.2) are multi-copper oxidases that oxidize a wide
variety of substrates. Despite extensive studies, the molecular basis for their diverse activity …
variety of substrates. Despite extensive studies, the molecular basis for their diverse activity …
Fused Tetrahydroquinolines Are Interfering with Your Assay
FM Bashore, J Annor-Gyamfi, Y Du… - Journal of Medicinal …, 2023 - ACS Publications
Tricyclic tetrahydroquinolines (THQs) have been repeatedly reported as hits across a
diverse range of high-throughput screening (HTS) campaigns. The activities of these …
diverse range of high-throughput screening (HTS) campaigns. The activities of these …
QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity
New anti-tuberculosis (anti-TB) drugs are urgently needed to battle drug-resistant
Mycobacterium tuberculosis strains and to shorten the current 6–12-month treatment …
Mycobacterium tuberculosis strains and to shorten the current 6–12-month treatment …
Target-based approaches for the discovery of new antimycobacterial drugs
Highlights•The most recently studied drug targets are reviewed.•The protein–protein
interaction network was generated using STRING database.•Hits and leads were discovered …
interaction network was generated using STRING database.•Hits and leads were discovered …
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 …
novel mechanisms of resistance; endangering not only our abilities to combat future …
High-throughput screen identifies small molecule inhibitors targeting acetyltransferase activity of Mycobacterium tuberculosis GlmU
Summary N-acetylglucosamine-1-phosphate uridyltransferase (GlmU) is a pivotal
bifunctional enzyme, its N and C terminal domains catalyzes uridyltransferase and …
bifunctional enzyme, its N and C terminal domains catalyzes uridyltransferase and …
Identification of potent inhibitors of DNA methyltransferase 1 (DNMT1) through a pharmacophore-based virtual screening approach
DNA methylation is an epigenetic change that results in the addition of a methyl group at the
carbon-5 position of cytosine residues. DNA methyltransferase (DNMT) inhibitors can …
carbon-5 position of cytosine residues. DNA methyltransferase (DNMT) inhibitors can …
The Inhibitory Effect of GlmU Acetyltransferase Inhibitor TPSA on Mycobacterium tuberculosis May Be Affected Due to Its Methylation by Methyltransferase Rv0560c
Mycobacterium tuberculosis bifunctional enzyme GlmU is a novel target for anti-TB drugs
and is involved in glycosyl donor UDP-N-acetylglucosamine biosynthesis. Here, we found …
and is involved in glycosyl donor UDP-N-acetylglucosamine biosynthesis. Here, we found …
Fusion of structure and ligand based methods for identification of novel CDK2 inhibitors
P Mahajan, G Chashoo, M Gupta… - Journal of Chemical …, 2017 - ACS Publications
Cyclin dependent kinases play a central role in cell cycle regulation which makes them a
promising target with multifarious therapeutic potential. CDK2 regulates various events of …
promising target with multifarious therapeutic potential. CDK2 regulates various events of …
Action of Dicumarol on Glucosamine-1-Phosphate Acetyltransferase of GlmU and Mycobacterium tuberculosis
Mycobacterium tuberculosis is one of most pathogenic microorganisms in the world.
Previously, the bifunctional enzyme GlmU with glucosamine-1-phosphate acetyltransferase …
Previously, the bifunctional enzyme GlmU with glucosamine-1-phosphate acetyltransferase …