Structural basis and SAR for OD 270, a lead stage 1,2,4-triazole based specific Tankyrase1/2 inhibitor

Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 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

100 mM NaOAc pH 4.5 and 16-26% PEG 3350, VAPOR DIFFUSION, HANGING DROP, temperature 310K

CATALYTIC FRAGMENT, PARP, ADP-RIBOSYLATION, ANK REPEAT, CHROMOSOMAL PROTEIN, GLYCOSYLTRANSFERASE, PHOSPHORYLATION, TELOMERE, TRANSFERASE, TRANSLOCATION, TRANSPORT, WNT-SIGNALLING, TRANSFERASE-TRANSFERASE INHIBITOR complex

LNTSGSGTILIDLSPDDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCNKKLWERYTHRRKEVSEENHNHAN
ERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPVHKDRSCYICHRQLLFCRVTLGK
SFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYVIYRGEQAYPEYLITYQIMRPEG