Mechanisms of Macromolecular Protease Inhibitors
نویسندگان
چکیده
منابع مشابه
Mechanisms of macromolecular protease inhibitors.
Proteolytic enzymes are ubiquitous in all organisms and constitute 2–4% of encoded gene products. They are critical for diverse biological processes such as digestion, blood clotting, host defense, pathogenic infection, viral replication, wound healing, and disease progression, to name but a few. Because proteases trigger an irreversible event—the cleavage of a protein—their activity must be ti...
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Defective variants of human immunodeficiency virus type 1 (HIV-1) protease (HIV PR) have been engineered to inhibit wild-type (wt) HIV PR activity. These variants were designed to promote the formation of heterodimers and to destabilize the formation of inactive variant homodimers of HIV-1 protease through substitutions at Asp-25, Ile-49, and Gly-50 (Babé, L. M., Rosé, J., and Craik, C. S. (199...
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Background and Aim: Advent of COVID-19 attracted the attentions of researchers to develop drugs for its treatment. Besides efforts on developing new drugs, screening available drugs for efficacy on COVID-19 could be an urgent action of initiating its pharmacotherapy. In this study, efficacy of HIV protease inhibitors on COVID-19 protease has been examined. Methods: Molecular docking based scree...
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Mouse cytotoxic T-lymphocyte antigen-2α (CTLA-2α), Drosophila CTLA-2-like protein (crammer), and Bombyx cysteine protease inhibitor (BCPI) belong to a novel family of cysteine protease inhibitors (I29). Their inhibitory mechanisms were studied comparatively. CTLA-2α contains a cysteine residue (C75), which is essential for its inhibitory potency. The CTLA-2α monomer was converted to a disulfide...
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Dimerization of human immunodeficiency virus type 1 protease (HIV-1 PR) monomers is an essential prerequisite for viral proteolytic activity and the subsequent generation of infectious virus particles. Disruption of the dimer interface inhibits this activity as does formation of heterodimers between wild-type and defective monomers. A structure-based approach was used to identify amino acid sub...
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ژورنال
عنوان ژورنال: ChemBioChem
سال: 2010
ISSN: 1439-4227
DOI: 10.1002/cbic.201000442