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Article

Targeting the gatekeeper residue in phosphoinositide 3-kinases.

Bioorganic & medicinal chemistry - 15 Apr 2005

Alaimo Peter J, Knight Zachary A, Shokat Kevan M

Abstract excerpt

A single residue in the ATP binding pocket of protein kinases-termed the gatekeeper-has been shown to control sensitivity to a wide range of small molecule inhibitors (Chem. Biol.2004, 11, 691; Chem. Biol.1999, 6, 671). Kinases that possess a small side chain at this position (Thr, Ala, or Gly) are readily targeted by structurally diverse classes of inhibitors, whereas kinases that possess a larger residue at...

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Identifiers

PMID: 15781393
DOI: 10.1016/j.bmc.2005.02.021

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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