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ARTICLE | Emerging Company Profile

Piqur: Optimizing dual inhibition

Piqur developing next-generation dual PI3K/mTOR inhibitors optimized for cancer

June 4, 2012 7:00 AM UTC

Piqur 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...