Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP‐Dependent Protein Kinase **
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DOI: 10.1002/cbic.202100704
Abstract: Plasmodium falciparum cGMP‐dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors have safety issues that may prevent further development. This work demonstrates isoxazole‐based compounds are potent ATP… read more here.
Keywords: plasmodium falciparum; protein kinase; competitive inhibitors; falciparum cgmp ... See more keywords
Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase
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DOI: 10.1016/j.jorganchem.2021.121822
Abstract: ABSTRACT Ferrocenyl and ruthenocenyl derivatives of ebselen are found to be competitive inhibitors of mammalian TrxR, with IC50 of 4.2 ± 0.3 and 2.5 ± 0.3 µM, respectively. The inhibition of TrxR is selective over… read more here.
Keywords: competitive inhibitors; derivatives ebselen; ebselen selective; inhibitors thioredoxin ... See more keywords
ATP-competitive inhibitors modulate the substrate binding cooperativity of a kinase by altering its conformational entropy
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DOI: 10.1126/sciadv.abo0696
Abstract: ATP-competitive inhibitors are currently the largest class of clinically approved drugs for protein kinases. By targeting the ATP-binding pocket, these compounds block the catalytic activity, preventing substrate phosphorylation. A problem with these drugs, however, is… read more here.
Keywords: binding cooperativity; competitive inhibitors; conformational entropy; substrate binding ... See more keywords
On the development of B-Raf inhibitors acting through innovative mechanisms
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DOI: 10.12688/f1000research.108761.2
Abstract: B-Raf is a protein kinase participating to the regulation of many biological processes in cells. Several studies have demonstrated that this protein is frequently upregulated in human cancers, especially when it bears activating mutations. In… read more here.
Keywords: innovative mechanisms; competitive inhibitors; raf; raf inhibitors ... See more keywords