Contemporary design of small-molecule kinase modulators: orthosteric, allosteric and induced-proximity strategies
Arvin C. Dar
Nature Reviews Drug Discovery, Published online: 28 April 2026; doi:10.1038/s41573-026-01411-9 Kinases represent one of the largest superfamilies of drug targets, but many members have remained notoriously challenging to drug by traditional small-molecule approaches. This Review assesses approaches and agents aimed at therapeutically modulating kinases, comparing orthosteric, allosteric and induced-proximity strategies. Key obstacles and future directions are considered.