Somatic mutations in PI3Kα: Structural basis for enzyme activation and drug design

Sandra B Gabelli, Diana Mandelker, Oleg Schmidt-Kittler, Bert Vogelstein, L. Mario Amzel

Research output: Contribution to journalReview article

Abstract

The PI3K pathway is a communication hub coordinating critical cell functions including cell survival, cell growth, proliferation, motility and metabolism. Because PI3Kα harbors recurrent somatic mutations resulting in gains of function in human cancers, it has emerged as an important drug target for many types of solid tumors. Various PI3K isoforms are also being evaluated as potential therapeutic targets for inflammation, heart disease, and hematological malignancies. Structural biology is providing insights into the flexibility of the PI3Ks, and providing basis for understanding the effects of mutations, drug resistance and specificity.

Original languageEnglish (US)
Pages (from-to)533-540
Number of pages8
JournalBiochimica et Biophysica Acta - Proteins and Proteomics
Volume1804
Issue number3
DOIs
StatePublished - Mar 1 2010

Keywords

  • Gain of function
  • H1047R mutant
  • PI3K
  • Somatic mutation
  • p110/p85

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biophysics
  • Biochemistry
  • Molecular Biology

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