Small molecules targeting phosphoinositide 3-kinases

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Small molecules targeting phosphoinositide 3-kinases

Authors
Publisher
Royal Society of Chemistry
Keywords
  • Pharmacology
  • Humans
  • Mammals
  • Primates
  • Drug Discovery
  • Structure-Activity Relationship
  • Xenograft
  • Primates Mammalia Vertebrata Chordata Animalia (Animals
  • Chordates
  • 10802
  • Enzymes - General And Comparative Studies: Coenzymes
  • 12512
  • Pathology - Therapy
  • 22002
  • Pharmacology - General
  • 22005
  • Pharmacology - Clinical Pharmacology
  • 02508
  • Cytology - Human
  • Nonhuman Vertebrates
  • Nonhuman Mammals
  • Rodentia Mammalia Vertebrata Chordata Animalia (Animals
  • Rodents
  • 02506
  • Cytology - Animal
  • 10068
  • Biochemistry Studies - Carbohydrates
  • Co-Crystal Structure
  • Signaling Cascade
  • Vertebrates) - Hominidae [86215] U87Mg Cell Line Cell_Line Human Glioma Cells A549 Cell Line Cell_Li
  • Vertebrates) - Muridae [86375] Mouse Common Nude
  • Ly294002 154447-36-6 Enzyme Inhibitor-Drug
  • Phosphoinositide 3-Kinase Pi3K 115926-52-8 Ec 2.7.1.154
  • Wortmannin 19545-26-7 Enzyme Inhibitor-Drug

Abstract

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.

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