5nqe

Human PARP14 (ARTD8), catalytic fragment in complex with an N-aryl piperazine inhibitor

spinqualitylabelsall models 5nqe, resolution 2.71Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5nqe is a 2 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 2.71Å Ligands: 94Z Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function PAR14_HUMAN Enhances STAT6-dependent transcription (By similarity). Has ADP-ribosyltransferase activity. Publication Abstract from PubMed A series of (Z)-4-(3-carbamoylphenylamino)-4-oxobut-2-enyl amides were synthesized and tested for their ability to inhibit the mono-(ADP-ribosyl)transferase, PARP14 (a.k.a. BAL-2; ARTD-8). Two synthetic routes were established for this series and several compounds were identified as sub-micromolar inhibitors of PARP14, the most potent of which was compound 4t, IC50=160nM. Furthermore, profiling other members of this series identified compounds with >20-fold selectivity over PARP5a/TNKS1, and modest selectivity over PARP10, a closely related mono-(ADP-ribosyl)transferase. Design and synthesis of potent inhibitors of the mono(ADP-ribosyl)transferase, PARP14.,Upton K, Meyers M, Thorsell AG, Karlberg T, Holechek J, Lease R, Schey G, Wolf E, Lucente A, Schuler H, Ferraris D Bioorg Med Chem Lett. 2017 Apr 29. pii: S0960-894X(17)30473-0. doi:, 10.1016/j.bmcl.2017.04.089. PMID:28495083 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Poly(ADP-ribose) polymerase 3D structures

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