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Review
. 2020 Oct 1;30(19):127442.
doi: 10.1016/j.bmcl.2020.127442. Epub 2020 Jul 27.

Exploiting binding-site arginines in drug design: Recent examples

Hong Lin  1 , Juan I Luengo  1
Affiliations
Review

Exploiting binding-site arginines in drug design: Recent examples

Hong Lin et al. Bioorg Med Chem Lett. .

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.

Keywords: Arginine; Non-canonical interaction; Protein ligand interaction; Structure-based drug design.

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Conflict of interest statement

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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