title: Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway.
abstract: BACKGROUND
  Among promising targeted therapies for cancer treatment, phosphatidylinositol 3-kinase pathway inhibitors have in the last 3 years continued to retain the attention of both academic institutions and pharmaceutical companies. The large amount of published clinical and preclinical data has indeed confirmed the preponderant role of this so-called survival pathway for tumor maintenance.
  
  
  CONCLUSIONS
  Global efforts have, therefore, been deployed that have led to the genesis of a panoply of small molecule inhibitors. This review will focus on updating the reader on the current medicinal chemistry efforts targeting this pathway.
  
  
  CONCLUSIONS
  Recent discoveries important for patient stratification, quantification of target modulation in humans and combination therapies will be presented and discussed.
authors.affiliation: NIBR GDC and Oncology, Novartis Pharma AG, CH4002 Basel, Switzerland.
authors.forename: Sauveur-Michel
authors.initials: SM
authors.lastname: Maira
authors.forename: Pascal
authors.initials: P
authors.lastname: Furet
authors.forename: Frédéric
authors.initials: F
authors.lastname: Stauffer
mesh_terms: D000494:Allosteric Regulation; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D015415:Biomarkers / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D000081082:Phosphoinositide-3 Kinase Inhibitors; D051057:Proto-Oncogene Proteins c-akt / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction; D054852:Small Molecule Libraries / Q000737:chemistry / Q000627:therapeutic use; D058570:TOR Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D015415:Biomarkers; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D051057:Proto-Oncogene Proteins c-akt; D054852:Small Molecule Libraries; D058570:TOR Serine-Threonine Kinases; C546842:MTOR protein, human