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ID: ALA4715850

Journal: Bioorg Med Chem Lett

Title: Exploiting binding-site arginines in drug design: Recent examples.

Authors: Lin H,Luengo JI

Abstract: Active or allosteric site arginines can form diverse interactions with ligands including different types of cation-π interactions, H-bond interactions and non-bond, non-canonical interactions. This provides many opportunities for creative structure-based drug design to improve potency, introduce novelty, and modulate MoA (mode of action), and even to achieve selectivity. This digest will use some recent drug targets of interest as examples to illustrate different types of interactions and how these interactions impact on potency, MoA, and selectivity.

CiteXplore: 32730944

DOI: 10.1016/j.bmcl.2020.127442