Matthew Correa
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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: CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia
CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia Open
Acute myeloid leukemia (AML) is marked by significant unmet clinical need due to both poor survival and high relapse rates where long-term disease control for most patients with relapsed or refractory AML remain dismal. Inspired to bring n…
View article: Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma Open
Many patients with multiple myeloma (MM) initially respond to treatment with modern combination regimens including immunomodulatory agents (lenalidomide and pomalidomide) and proteasome inhibitors. However, some patients lack an initial re…
View article: Discovery of CRBNE3 Ligase Modulator CC-92480 forthe Treatment of Relapsed and Refractory Multiple Myeloma
Discovery of CRBNE3 Ligase Modulator CC-92480 forthe Treatment of Relapsed and Refractory Multiple Myeloma Open
Many\npatients with multiple myeloma (MM) initially respond to treatment\nwith modern combination regimens including immunomodulatory agents\n(lenalidomide and pomalidomide) and proteasome inhibitors. However,\nsome patients lack an initia…
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…