Patrick Papa
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View article: Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation Open
Modulating the chemical composition of cereblon (CRBN) binders is a critical step in the optimization process of protein degraders that seek to hijack the function of this E3 ligase. Small structural changes can have profound impacts on th…
View article: Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005
Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005 Open
The PKC-θ isoform of protein kinase C is selectively expressed in T lymphocytes and plays an important role in the T cell antigen receptor (TCR)-triggered activation of mature T cells, T cell proliferation, and the subsequent release of cy…
View article: Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115 Open
We report here the synthesis and structure-activity relationship (SAR) of a novel series of triazole containing mammalian target of rapamycin (mTOR) kinase inhibitors. SAR studies examining the potency, selectivity, and PK parameters for a…
View article: Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223
Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223 Open
We report here the synthesis and structure-activity relationship (SAR) of a novel series of mammalian target of rapamycin (mTOR) kinase inhibitors. A series of 4,6- or 1,7-disubstituted-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-ones were op…