4w9x

Crystal Structure of BMP-2-inducible kinase in complex with baricitinib

spinqualitylabelsall models 4w9x, resolution 2.14Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4w9x is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.14Å Ligands: 3JW, EDO Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function BMP2K_HUMAN May be involved in osteoblast differentiation. Publication Abstract from PubMed The highly diverse Numb-associated kinase (NAK) family has been linked to broad cellular functions including receptor-mediated endocytosis, Notch pathway modulation, osteoblast differentiation, and dendrite morphogenesis. Consequently, NAK kinases play a key role in a diverse range of diseases from Parkinson's and prostate cancer to HIV. Due to the plasticity of this kinase family, NAK kinases are often inhibited by approved or investigational drugs and have been associated with side effects, but they are also potential drug targets. The presence of cysteine residues in some NAK family members provides the possibility for selective targeting via covalent inhibition. Here we report the first high-resolution structures of kinases AAK1 and BIKE in complex with two drug candidates. The presented data allow a comprehensive structural characterization of the NAK kinase family and provide the basis for rational design of selective NAK inhibitors. Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.,Sorrell FJ, Szklarz M, Abdul Azeez KR, Elkins JM, Knapp S Structure. 2016 Jan 29. pii: S0969-2126(16)00008-3. doi:, 10.1016/j.str.2015.12.015. PMID:26853940 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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