Tankyrase 2 in complex with an inhibitor (OM-1700)

Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.

TANK2,ADP-ribosyltransferase diphtheria toxin-like 6,ARTD6,Poly [ADP-ribose] polymerase 5B,TNKS-2,TRF1-interacting ankyrin-related ADP-ribose polymerase 2,Tankyrase II,Tankyrase-like protein,Tankyrase-related protein

MHHHHHHSSGVDLGTENLYFQSMLNTSGSGTILIDLSPDDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCN
KKLWERYTHRRKEVSEENHNHANERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCP
VHKDRSCYICHRQLLFCRVTLGKSFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYVIYRGEQAYPEYLITYQIMRPEG

Based on gel filtration this runs as a monomer in solution.

Hydrogens have been added in their riding positions

Inhibitor, Complex, Poly-ADP-ribosylation, Enzyme, TRANSFERASE

LNTSGSGTILIDLSPDDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCNKKLWERYTHRRKEVSEENHNHAN
ERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPVHKDRSCYICHRQLLFCRVTLGK
SFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYVIYRGEQAYPEYLITYQIMRPEG