Targeting PTEN using small molecule inhibitors.
PTEN (phosphatase and tensin homologue deleted on chromosome 10) is well known as a tumour suppressor. It's PI(3,4,5)P3 lipid phosphatase activity is an important counteracting mechanism in PI 3-kinase (phosphoinositide 3-kinase) signalling. Furthermore, PTEN lies upstream of Akt kinase, a key enzyme in insulin signalling regulating glucose uptake and cell growth. Therefore, PTEN has recently gained attention as a valuable drug target for the treatment of diabetes, stroke, cardiac infarct and fertility. This review summarizes the use of small molecules as PTEN inhibitors. Currently available methodologies and techniques for accessing PTEN inhibition in vitro and in cellulo will be discussed.
Department of Chemistry, Imperial College London, Exhibition Road, London SW7 2AZ, UK. Electronic address: lokhangmak@gmail.com.
Lok Hang
LH
Mak
Department of Chemistry, Imperial College London, Exhibition Road, London SW7 2AZ, UK; Institute of Chemical Biology, Imperial College London, Exhibition Road, London SW7 2AZ, UK. Electronic address: r.woscholski@imperial.ac.uk.
Rudiger
R
Woscholski
D000818:Animals; D018390:Gene Targeting / Q000379:methods*; D006801:Humans; D051059:PTEN Phosphohydrolase / Q000032:analysis / Q000235:genetics*; D019869:Phosphatidylinositol 3-Kinases / Q000235:genetics*; D051057:Proto-Oncogene Proteins c-akt / Q000235:genetics*; D025521:Tumor Suppressor Proteins / Q000032:analysis / Q000235:genetics*
D025521:Tumor Suppressor Proteins; D019869:Phosphatidylinositol 3-Kinases; D051057:Proto-Oncogene Proteins c-akt; D051059:PTEN Phosphohydrolase; C494929:PTEN protein, human
Inhibition; OMFP; PTEN; VO-OHpic; Vanadium compounds