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Showing 1 to 2 of 2 for “"Heterobifunctional Molecule"”.
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The Design, Synthesis and in vitro Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Degradation of Protein Arginine Methyltransferase 1
… PROTACs led to the isolation of a heterobifunctional molecule with the linker attached to the binding pharmacophore of the CRBN ligand. This molecule was found to degrade PRMT1 and is proposed to be a monomeric degrader that destabilises the structure of PRMT1 upon binding. This …
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Developing Computational Methods in Proximity Pharmacology for Enzyme Discovery, PROTAC Screening, and Conformational Space Exploration
Traditional drug discovery focuses on small molecules that target single proteins. Molecular glues, discovered in the 1990s while studying natural products like cyclosporin, induce de novo protein-protein interaction between proteins. Later, heterobifunctional compounds consisting of two ligands …