Covalent allosteric inhibitors of Akt generated using a click fragment approach.
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DOI: 10.1002/cmdc.202100776
Abstract: Akt is a protein kinase that has been implicated in the progression of cancerous tumors. A number of covalent allosteric Akt inhibitors are known, and based on these scaffolds, a small library of novel potential… read more here.
Keywords: covalent; allosteric inhibitors; covalent allosteric; inhibitors akt ... See more keywords
Discovery of a First-In-Class Covalent Allosteric Inhibitor of SUMO E1 Activating Enzyme.
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DOI: 10.1016/j.chembiol.2019.02.006
Abstract: SUMOylation is a post-translational modification with important roles in normal physiology and whose dysregulation is associated with human diseases. In this issue of Cell Chemical Biology, Li et al. (2019) describe a covalent, allosteric inhibitor of… read more here.
Keywords: covalent allosteric; allosteric inhibitor; biology; inhibitor sumo ... See more keywords
Structure-Guided Discovery of the Novel Covalent Allosteric Site and Covalent Inhibitors of Fructose-1,6-Bisphosphate Aldolase to Overcome the Azole Resistance of Candidiasis.
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DOI: 10.1021/acs.jmedchem.1c02102
Abstract: Fructose-1,6-bisphosphate aldolase (FBA) represents an attractive new antifungal target. Here, we employed a structure-based optimization strategy to discover a novel covalent binding site (C292 site) and the first-in-class covalent allosteric inhibitors of FBA from Candida… read more here.
Keywords: bisphosphate aldolase; covalent; covalent inhibitors; covalent allosteric ... See more keywords
Molecular mechanism of a covalent allosteric inhibitor of SUMO E1 activating enzyme
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DOI: 10.1038/s41467-018-07015-1
Abstract: E1 enzymes activate ubiquitin (Ub) and ubiquitin-like modifiers (Ubls) in the first step of Ub/Ubl conjugation cascades and represent potential targets for therapeutic intervention in cancer and other life-threatening diseases. Here, we report the crystal… read more here.
Keywords: covalent allosteric; allosteric inhibitor; mechanism; sumo ... See more keywords