DFG-1 Binding: A New Residue for Developing Selective Kinase Inhibitors.
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DOI: 10.1021/acs.jmedchem.0c01501
Abstract: Only 15% of human kinases carry a bulky residue at the DFG-1 position, providing an opportunity for the design of selective ATP-site inhibitors without the typical hinge-binding interactions. The low sequence homology among unrelated kinases… read more here.
Keywords: dfg binding; kinase; binding new; new residue ... See more keywords
Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205
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DOI: 10.1158/1538-7445.am2017-979
Abstract: Janus kinases are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling, with constitutive activation of JAK/STAT pathways associated with a wide variety of malignancies.… read more here.
Keywords: kinase; kinase inhibitor; jak1 selective; selective kinase ... See more keywords