7lun

Human PARP14 (ARTD8), catalytic fragment in complex with RBN011980

spinqualitylabelsall models 7lun, resolution 2.57Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.57Å Ligands: CL, GOL, YFG Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Publication Abstract from PubMed PARP14 is an interferon-stimulated gene that is overexpressed in multiple tumor types, influencing pro-tumor macrophage polarization as well as suppressing the antitumor inflammation response by modulating IFN-gamma and IL-4 signaling. PARP14 is a 203 kDa protein that possesses a catalytic domain responsible for the transfer of mono-ADP-ribose to its substrates. PARP14 also contains three macrodomains and a WWE domain which are binding modules for mono-ADP-ribose and poly-ADP-ribose, respectively, in addition to two RNA recognition motifs. Catalytic inhibitors of PARP14 have been shown to reverse IL-4 driven pro-tumor gene expression in macrophages, however it is not clear what roles the non-enzymatic biomolecular recognition motifs play in PARP14-driven immunology and inflammation. To further understand this, we have discovered a heterobifunctional small molecule designed based on a catalytic inhibitor of PARP14 that binds in the enzyme's NAD + -binding site and recruits the E3 ligase cereblon to ubiquitinate it and selectively target it for degradation. Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule.,Wigle T, Ren Y, Molina JR, Blackwell DJ, Schenkel LB, Swinger KK, Kuplast-Barr K, Majer CR, Church WD, Lu AZ, Mo J, Abo R, Cheung A, Dorsey BW, Niepel M, Perl NR, Vasbinder MM, Keilhack H, Kuntz KW Chembiochem. 2021 Apr 10. doi: 10.1002/cbic.202100047. PMID:33838082 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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