Search Results - "Korotkov, Vadim S"
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Oligosubstituted Pyrroles Directly from Substituted Methyl Isocyanides and Acetylenes
Published in Chemistry : a European journal (01-01-2009)“…The formal cycloaddition of α‐metallated methyl isocyanides 1 onto the triple bond of electron‐deficient acetylenes 2 represents a direct and convenient…”
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2
The Mechanism of Caseinolytic Protease (ClpP) Inhibition
Published in Angewandte Chemie International Edition (04-03-2013)“…Catch me if you can: The ClpP protease mediates protein homeostasis and can be efficiently inhibited by β‐lactones. A combination of molecular docking,…”
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3
Synthesis and biological activity of optimized belactosin C congeners
Published in Organic & biomolecular chemistry (26-10-2011)“…Successful biochemical studies of the natural products belactosin A and C as well as their more stable acylated derivatives have proved them to be powerful…”
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4
A Whole Proteome Inventory of Background Photocrosslinker Binding
Published in Angewandte Chemie International Edition (24-01-2017)“…Affinity‐based protein profiling (AfBPP) is a widely applied method for the target identification of bioactive molecules. Probes containing photocrosslinkers,…”
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Neocarzilin A Is a Potent Inhibitor of Cancer Cell Motility Targeting VAT‑1 Controlled Pathways
Published in ACS central science (24-07-2019)“…The natural product neocarzilin A (NCA) was discovered decades ago, and despite its potent cytotoxic effects no mode of action studies have been performed up…”
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Repurposing human kinase inhibitors to create an antibiotic active against drug-resistant Staphylococcus aureus, persisters and biofilms
Published in Nature chemistry (01-02-2020)“…New drugs are desperately needed to combat methicillin-resistant Staphylococcus aureus (MRSA) infections. Here, we report screening commercial kinase…”
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Hydantoin analogs inhibit the fully assembled ClpXP protease without affecting the individual peptidase and chaperone domains
Published in Organic & biomolecular chemistry (14-08-2019)“…Proteolysis mediated by ClpXP is a crucial cellular process linked to bacterial pathogenesis. The development of specific inhibitors has largely focused on…”
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A chemical compound inhibiting the Aha1–Hsp90 chaperone complex
Published in The Journal of biological chemistry (13-10-2017)“…The eukaryotic Hsp90 chaperone machinery comprises many co-chaperones and regulates the conformation of hundreds of cytosolic client proteins. Therefore, it is…”
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Selective Activation of Human Caseinolytic Protease P (ClpP)
Published in Angewandte Chemie International Edition (26-10-2018)“…Caseinolytic protease P (ClpP) is the proteolytic component of the ClpXP protein degradation complex. Eukaryotic ClpP was recently found to act within the…”
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A Chemical Disruptor of the ClpX Chaperone Complex Attenuates the Virulence of Multidrug‐Resistant Staphylococcus aureus
Published in Angewandte Chemie International Edition (04-12-2017)“…The Staphylococcus aureus ClpXP protease is an important regulator of cell homeostasis and virulence. We utilized a high‐throughput screen against the ClpXP…”
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Dual Inhibitor of Staphylococcus aureus Virulence and Biofilm Attenuates Expression of Major Toxins and Adhesins
Published in Biochemistry (Easton) (20-03-2018)“…Staphylococcus aureus is a major bacterial pathogen that invades and damages host tissue by the expression of devastating toxins. We here performed a…”
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Reversible Inhibitors Arrest ClpP in a Defined Conformational State that Can Be Revoked by ClpX Association
Published in Angewandte Chemie International Edition (21-12-2015)“…Caseinolytic protease P (ClpP) is an important regulator of Staphylococcus aureus pathogenesis. A high‐throughput screening for inhibitors of ClpP peptidase…”
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13
A Minimal β-Lactone Fragment for Selective β5c or β5i Proteasome Inhibitors
Published in Angewandte Chemie International Edition (26-06-2015)“…Broad‐spectrum proteasome inhibitors are applied as anticancer drugs, whereas selective blockage of the immunoproteasome represents a promising therapeutic…”
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A Minimal [beta]-Lactone Fragment for Selective [beta]5c or [beta]5i Proteasome Inhibitors
Published in Angewandte Chemie International Edition (26-06-2015)“…Broad-spectrum proteasome inhibitors are applied as anticancer drugs, whereas selective blockage of the immunoproteasome represents a promising therapeutic…”
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15
Development and characterization of improved β-lactone-based anti-virulence drugs targeting ClpP
Published in Bioorganic & medicinal chemistry (15-01-2012)“…Here, we report the synthesis and in depth characterization of a second generation β-lactone derived virulence inhibitors. Based on initial results that…”
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GaCl3-catalyzed insertion of diazene derivatives into the cyclopropane ring
Published in Journal of organic chemistry (28-09-2007)Get full text
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A β-Lactone-Based Antivirulence Drug Ameliorates Staphylococcus aureus Skin Infections in Mice
Published in ChemMedChem (01-04-2014)“…Skin infections caused by Staphylococcus aureus are a major clinical concern, especially if they are caused by multi‐resistant strains. In these cases, a…”
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An Aromatic Hydroxyamide Attenuates Multiresistant Staphylococcus aureus Toxin Expression
Published in Chemistry : a European journal (26-01-2016)“…Methicillin‐resistant Staphylococcus aureus (MRSA) causes severe infections with only few effective antibiotic therapies currently available. To approach this…”
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AAA+ chaperones and acyldepsipeptides activate the ClpP protease via conformational control
Published in Nature communications (19-02-2015)Get full text
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Frontispiece: An Aromatic Hydroxyamide Attenuates Multiresistant Staphylococcus aureus Toxin Expression
Published in Chemistry : a European journal (26-01-2016)“…Anti‐Virulence Strategy The agreement depicted in the figure is between humans, who, instead of killing bacterial cells, just reduce their arsenal of virulence…”
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