6fzm | pdb_00006fzm

Human PARP14 (ARTD8), catalytic fragment in complex with inhibitor ITK6

spinqualitylabelsall models 6fzm, resolution 2.67Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6fzm 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 2.67Å Ligands: EE5 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function PAR14_HUMAN Enhances STAT6-dependent transcription (By similarity). Has ADP-ribosyltransferase activity. Publication Abstract from PubMed Poly-ADP-ribose polymerases (PARPs1-16) play pivotal roles in diverse cellular processes. PARPs that catalyze poly-ADP-ribosylation (PARylation) are the best characterized PARP family members because of the availability of potent and selective inhibitors for these PARPs. There has been comparatively little success in developing selective small-molecule inhibitors of PARPs that catalyze mono-ADP-ribosylation (MARylation), limiting our understanding of the cellular role of MARylation. Here we describe the structure-guided design of inhibitors of PARPs that catalyze MARylation. The most selective analog, ITK7, potently inhibits the MARylation activity of PARP11, a nuclear envelope-localized PARP. ITK7 is greater than 200-fold selective over other PARP family members. Using live-cell imaging, we show that ITK7 causes PARP11 to dissociate from the nuclear envelope. These results suggest that the cellular localization of PARP11 is regulated by its catalytic activity. A Potent and Selective PARP11 Inhibitor Suggests Coupling between Cellular Localization and Catalytic Activity.,Kirby IT, Kojic A, Arnold MR, Thorsell AG, Karlberg T, Vermehren-Schmaedick A, Sreenivasan R, Schultz C, Schuler H, Cohen MS Cell Chem Biol. 2018 Dec 20;25(12):1547-1553.e12. doi:, 10.1016/j.chembiol.2018.09.011. Epub 2018 Oct 18. PMID:30344052 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Poly(ADP-ribose) polymerase 3D structures

Proteopedia Page Contributors and Editors (what is this?)

OCA