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Piqur developing next-generation dual PI3K/mTOR inhibitors optimized for cancer
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Piqur: Optimizing dual inhibition
Monday, June 4, 2012
Therapeutics Inc. has developed a dual inhibitor of PI3K and mTOR that
it says could treat solid tumors more effectively than dual PI3K/mTOR inhibitors
in the clinic because it hits both targets with potencies that are optimized to
enhance the overall inhibitory effect on PI3K/mTOR signaling.
Signaling by phosphoinositide
3-kinase (PI3K) and mammalian target of rapamycin (mTOR; FRAP; RAFT1) promotes
cell proliferation and survival. Because the PI3K/mTOR pathway is
over-activated in cancer, the original rationale behind dual PI3K/mTOR
inhibition was straightforward: hit both targets with equal potency and block
signaling through the pathway.
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