mTORmTOR is a protein kinase that, through the phosphorylation of specific substrates, regulates the expression of proteins involved in cell growth and proliferation. As such, mTOR plays an integral role in the response to numerous hormones and growth factors. mTOR activity is up-regulated in a large percentage of human cancers, due to either:
Amplification and over-expression of growth factors or growth factor receptors
Activating mutations in growth factor receptors or in PI3-Kinase
Loss of tumour suppressors such as PTEN, TSC1/2 or LKB1.
Current inhibitors of mTOR include the large natural product rapamycin and derivatives thereof (rapalogs). Rapamycin has been extensively used to demonstrate the effect of mTOR inhibition on key cellular processes such as cell growth and proliferation, apoptosis, and autophagy. Rapamycin and the rapalogs have also helped generate an extensive pre-clinical validation of mTOR as a very promising anti-cancer target, and rapalogs have shown promising anti-cancer activity in the clinic.Useful links : Development programmes - mTOR
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