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Tag Archives: rapamycin
Discovery of PF-04691502 (PI3K/mTOR dual inhibitor)
Rapamycin and it’s analogues (or rapalogues e.g. CCI-779) modulate the phosphatidylinositol 3-kinase (PI3K) signalling cascade by binding to an allosteric site on the mTORC1 complex (Mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, forms two functional complexes, … Continue reading →
Posted in Clinical Candidates, Enzyme Inhibitors, Kinase Inhibitors, Kinases, Med Chem Strategy
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Tagged allosteric, cancer, CCI-779, dual inhibitor, H-bond, isostere, kinase, ligand efficiency, LipE, lipophilic efficiency, metabolism, mTOR, mTORC, PDB3ML8, PDB3ML9, PF-04691502, Pfizer, phosphatidylinositol 3-kinase, pI3K, rapalogues, rapamycin, solubility, Structure Based Design, X-ray data
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