Search Results - "Rožman, Kaja"
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Synthesis and structure–activity relationship study of novel quinazolinone-based inhibitors of MurA
Published in Bioorganic & medicinal chemistry letters (01-08-2017)“…[Display omitted] •Synthesis and extensive SAR of a series of quinazolinone-based inhibitors of MurA.•Potent MurA inhibitors with IC50 in low micromolar range…”
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Discovery of Mycobacterium tuberculosis InhA Inhibitors by Binding Sites Comparison and Ligands Prediction
Published in Journal of medicinal chemistry (22-12-2016)“…Drug discovery is usually focused on a single protein target; in this process, existing compounds that bind to related proteins are often ignored. We describe…”
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3
Cardiac ryanodine receptor N-terminal region biosensors identify novel inhibitors via FRET-based high-throughput screening
Published in The Journal of biological chemistry (01-01-2022)“…The N-terminal region (NTR) of ryanodine receptor (RyR) channels is critical for the regulation of Ca2+ release during excitation–contraction (EC) coupling in…”
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4
Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2019)“…The Mur ligases form a series of consecutive enzymes that participate in the intracellular steps of bacterial peptidoglycan biosynthesis. They therefore…”
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A new ‘golden age’ for the antitubercular target InhA
Published in Drug discovery today (01-03-2017)“…•Recent advances in development of InhA inhibitors are presented.•We focus on inhibitors with a clear link to their in vivo activity.•Collected…”
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Recent Advances in the Development of Undecaprenyl Pyrophosphate Synthase Inhibitors as Potential Antibacterials
Published in Current medicinal chemistry (01-02-2016)“…Expanding antibiotic use in clinical practice and emergence of bacterial resistance are fueling research efforts for the development of novel antibacterials…”
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Anthranilic Acid Inhibitors of Undecaprenyl Pyrophosphate Synthase (UppS), an Essential Enzyme for Bacterial Cell Wall Biosynthesis
Published in Frontiers in microbiology (14-01-2019)“…We report the successful implementation of virtual screening in the discovery of new inhibitors of undecaprenyl pyrophosphate synthase (UppS) from UppS is an…”
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Psoralen Derivatives as Inhibitors of Mycobacterium tuberculosis Proteasome
Published in Molecules (Basel, Switzerland) (12-03-2020)“…Protein degradation is a fundamental process in all living organisms. An important part of this system is a multisubunit, barrel-shaped protease complex called…”
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Discovery of new MurA inhibitors using induced-fit simulation and docking
Published in Bioorganic & medicinal chemistry letters (15-02-2017)“…[Display omitted] We report on the successful application of ProBiS-CHARMMing web server in the discovery of new inhibitors of MurA, an enzyme that catalyzes…”
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Synthesis and Biological Evaluation of N-Aryl-N'-(5-(2-hydroxybenzoyl) pyrimidin-2-yl)guanidines as Toll-Like Receptor 4 Antagonists
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-12-2016)“…Toll-like receptor 4 (TLR4) has been associated with several inflammatory diseases, such as sepsis, atherosclerosis and chronic pain. The aim of the present…”
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Docking study with biological validation on bacterial enzyme MurD
Published in Chemical Data Collections (01-03-2018)“…Approved antibiotics currently target only a small number of bacterial enzymes, despite increasing rates of antibiotic-resistant microbes. New chemical…”
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High-Throughput Screening and Drug Development to Fix RyR Pathology
Published in Biophysical journal (12-02-2021)Get full text
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13
High-Throughput Screening Yields Allosteric Inhibitors of Leaky RyRs for Therapeutic Development
Published in Biophysical journal (07-02-2020)Get full text
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14
H Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases
Published in Journal of enzyme inhibition and medicinal chemistry (2019)“…The Mur ligases form a series of consecutive enzymes that participate in the intracellular steps of bacterial peptidoglycan biosynthesis. They therefore…”
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Mycobacterial MenG: Partial Purification, Characterization, and Inhibition
Published in ACS infectious diseases (09-12-2022)“…Menaquinone (MK) is an essential component of the electron transport chain (ETC) in the gram-variable Mycobacterium tuberculosis and many Gram-positive…”
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