Human Poly (ADP-ribose) Polymerase Family Member 14 (PARP14)
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TEP details
Summary
This work provides reagents to develop specific inhibitors of the macrodomains of PARP14, for potential use for cancer and/or inflammation. Targeting the macrodomains of PARP14 is an alternative targeting strategy to PARP catalytic domain inhibitors that may allow greater inhibitor selectivity, and an alternative cellular effect.
This package includes protein purification protocols, crystal structures of the 2nd and 3rd macrodomain of PARP14 in complex with small molecule chemical starting points, in vitro assays to measure ligand binding to the macrodomains, as well as validation of a PARP14 antibody and reagents to generate PARP14 knock-out cell lines (CRISPR-Cas9).
Structures
Structures available in TEP:
- PARP14 macrodomain 2 with ligand MnK2-13 (PDB:5O2D ): protein, ligand
- PARP14 macrodomain 3 with fragment N13417a (PDB:5QHT ): protein, ligand
- PARP14 macrodomain 3 with fragment N08149b (PDB:5QHU ): protein, ligand
- PARP14 macrodomain 3 with fragment N13681a (PDB:5QHV ): protein, ligand
- PARP14 macrodomain 3 with fragment N13729a (PDB:5QHW ): protein, ligand
- PARP14 macrodomain 3 with fragment N13734a (PDB:5QI0 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13856a (PDB:5QI1 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13979a (PDB:5QI6 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13857a (PDB:5QI3 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13848a (PDB:5QI4 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13987a (PDB:5QI8 ): protein, ligand
- PARP14 macrodomain 3 with fragment N14095a (PDB:5QI9 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13660a (PDB:5QHX ): protein, ligand
- PARP14 macrodomain 3 with fragment N13844a (PDB:5QHY ): protein, ligand
- PARP14 macrodomain 3 with fragment N13767a (PDB:5QHZ ): protein, ligand
- PARP14 macrodomain 3 with fragment N13462a (PDB:5QI2 ): protein, ligand
- PARP14 macrodomain 3 with fragment N14015a (PDB:5QI5 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13888a (PDB:5QI7 ): protein, ligand
- PARP14 macrodomain 3 with fragment N13605a (PDB:5QIA ): protein, ligand