Advances in the development of class I phosphoinositide 3-kinase (PI3K) inhibitors

Dima A. Sabbah, Jian Hu, Haizhen A. Zhong

Research output: Contribution to journalReview articlepeer-review

26 Scopus citations


The PI3K signaling cascade is the key moderator of cell proliferation, survival, motility, and apoptosis. Class I PI3K proteins are well characterized and linked to thrombosis (PI3Kβ), rheumatoid arthritis (PI3Kδ), and cancer (PI3Kα). In this review, we explore the latest progress in the design and development of selective Class I PI3K inhibitors from the perspective of drug design and structure activity relationships.

Original languageEnglish (US)
Pages (from-to)1413-1426
Number of pages14
JournalCurrent Topics in Medicinal Chemistry
Issue number13
StatePublished - May 1 2016


  • Anticancer
  • BRAF
  • Class I PI3Ks
  • Drug design
  • EGFR
  • GDC-0941
  • GSK2118436
  • KRAS
  • LY294002
  • MEK
  • Mutation
  • NVP-BEZ235
  • P100α
  • PI3K/AKT
  • PI3Kγ
  • Selectivity
  • mTOR

ASJC Scopus subject areas

  • Drug Discovery


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