Krishna Deepak RNV

Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery

Keywords: lipid GPCR; ligand access; orthosteric and allosteric binding sites; drug discovery; antibody; computational methods; prostaglandin receptor; platelet-activating factor receptor; sphingosine-1-phosphate receptor; lysophosphatidic acid receptor; leukotriene receptor; free fatty acid receptor; cannabinoid receptor

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Identification of FDA-approved drugs as novel allosteric inhibitors of human executioner caspases

The regulation of apoptosis is a tightly-coordinated process and caspases are its chief regulators. Of special importance are the executioner caspases, caspase-3/7, the activation of which irreversibly sets the cell on the path of death. Dysregulation of apoptosis, particularly an increased rate of cell death lies at the root of numerous human diseases. Although several peptide-based inhibitors targeting the homologous active site region of caspases have been developed, owing to their non-specific activity and poor pharmacological properties their use has largely been restricted.

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