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Current Medicinal Chemistry

Volume 18 Issue 18
ISSN: 0929-8673
eISSN: 1875-533X

 

   All Titles

  Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
  pp.2686-2714 (29) Authors: S. J. Shuttleworth, F. A. Silva, A. R.L. Cecil, C. D. Tomassi, T. J. Hill, F. I. Raynaud, P. A. Clarke, P. Workman
 
 
      Abstract

The phosphoinositide 3-kinases (PI3Ks) constitute an important family of lipid kinase enzymes that control a range of cellular processes through their regulation of a network of signal transduction pathways, and have emerged as important therapeutic targets in the context of cancer, inflammation and cardiovascular diseases. Since the mid-late 1990s, considerable progress has been made in the discovery and development of small molecule ATP-competitive PI3K inhibitors, a number of which have entered early phase human trials over recent years from which key clinical results are now being disclosed. This review summarizes progress made to date, primarily on the discovery and characterization of class I and dual class I/IV subtype inhibitors, together with advances that have been made in translational and clinical research, notably in cancer.

 
  Keywords: PI3K, inhibitor, p110α, p110β, p110δ, p110ggr;, mTOR, cancer, inflammation, cardiovascular, phosphoinositide
  Affiliation: Karus Therapeutics Ltd., Southampton Science Park, 2 Venture Road, Southampton, SO16 7NP, UK.
 
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