Small molecules targeting phosphoinositide 3-kinases

Peng Wu, Yongzhou Hu

Research output: Contribution to journalJournal articleResearchpeer-review


The phosphoinositide 3-kinase (PI3K) pathway is one of the most important signaling cascades in cancer, and PI3K is a well established target for anticancer therapy. Since the discovery of the first two compounds that inhibit PI3K, wortmannin and LY294002, a wealth of PI3K inhibitors of various chemotypes have been identified, and nearly twenty of them are currently in various stages of clinical trials. This review outlines the current landscape of the development of small molecule PI3K inhibitors with a focus on structure-activity relationships (SAR) and discussion of co-crystal structures.
Original languageEnglish
Issue number11
Pages (from-to)1337-1355
Publication statusPublished - 2012
Externally publishedYes


  • co-crystal structure
  • drug discovery
  • signaling cascade
  • structure-activity relationship
  • Primates Mammalia Vertebrata Chordata Animalia (Animals, Chordates, Humans, Mammals, Primates, Vertebrates) - Hominidae [86215] U87MG cell line cell_line human glioma cells A549 cell line cell_line human nonsmall cell lung cancer cells H460 cell line cell_line human pleural effusion adenocarcinoma cells
  • Rodentia Mammalia Vertebrata Chordata Animalia (Animals, Chordates, Mammals, Nonhuman Vertebrates, Nonhuman Mammals, Rodents, Vertebrates) - Muridae [86375] mouse common nude, xenograft
  • LY294002 154447-36-6 enzyme inhibitor-drug
  • phosphoinositide 3-kinase PI3K 115926-52-8 EC
  • wortmannin 19545-26-7 enzyme inhibitor-drug
  • 02506, Cytology - Animal
  • 02508, Cytology - Human
  • 10068, Biochemistry studies - Carbohydrates
  • 10802, Enzymes - General and comparative studies: coenzymes
  • 12512, Pathology - Therapy
  • 22002, Pharmacology - General
  • 22005, Pharmacology - Clinical pharmacology
  • Pharmacology


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