Open AccessTargeting the PI3K/Akt/mTOR pathway--beyond rapalogs.
Author(s) -
Benjamin Markman,
Rodrigo Dienstmann,
Josep Tabernero
Publication year - 2010
Publication title -
pubmed
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.373
H-Index - 127
eISSN - 1949-2553
DOI - 10.18632/oncotarget.101012
Subject(s) - pi3k/akt/mtor pathway , mtorc1 , medicine , receptor tyrosine kinase , protein kinase b , cancer research , signal transduction , bioinformatics , biology , receptor , microbiology and biotechnology
It is well established that the PI3K pathway plays a central role in various cellular processes that can contribute to the malignant phenotype. Accordingly, pharmacological inhibition of key nodes in this signaling cascade has been a focus in developmental therapeutics. To date, agents targeting upstream receptor tyrosine kinases are best studied and have achieved greatest clinical success. Further downstream, despite efficacy in certain tumor types, the rapalogs have been somewhat disappointing in the clinic. Novel inhibitors of PI3K, Akt, and mTORC1 and 2 are now passing through early phase clinical trials. It is hoped that these agents will circumvent some of the shortcomings of the rapalogs and lead to meaningful benefits for cancer patients.