Literature summary for 3.2.1.143 extracted from

Koh, D.W.; Coyle, D.L.; Mehta, N.; Ramsinghani, S.; Kim, H.; Slama, J.T.; Jacobson, M.K.
SAR analysis of adenosine diphosphate (hydroxymethyl)pyrrolidinediol inhibition of poly(ADP-ribose) glycohydrolase (2003), J. Med. Chem., 46, 4322-4332.

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-N3-adenosine diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition at 0.290 mM, native protein and 50% inhibition at 0.148 mM, recombinant catalytic fragment	Bos taurus
8-chlorophenylthioadenosine 5'-diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition at 0.12 mM, recombinant catalytic fragment	Bos taurus
8-N3-adenosine diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition at 390 nM, native protein and 50% inhibition at 0.0014 mM, recombinant catalytic fragment	Bos taurus
adenosine diphosphate (hydroxymethyl)pyrrolidine	50% inhibition at 0.019 mM, native protein and 50% inhibition at 0.063 mM, recombinant catalytic fragment	Bos taurus
adenosine diphosphate (hydroxymethyl)pyrrolidine-monoalcohol	50% inhibition at 330nM, native protein and 50% inhibition at 440 nM, recombinant catalytic fragment	Bos taurus
adenosine diphosphate (hydroxymethyl)pyrrolidinediol	i.e. APD-HPD, 50% inhibition at 0.0031 mM, native protein and 50% inhibition at 0.0042 mM, recombinant catalytic fragment	Bos taurus
Ahx	50% inhibition at 0.001 mM, recombinant catalytic fragment	Bos taurus
F3Ahx	50% inhibition at 0.57 mM, recombinant catalytic fragment	Bos taurus
guanosine 5'-diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition above 1 mM, native protein and 50% inhibition at 0.970 mM,+ recombinant catalytic fragment	Bos taurus
additional information	not inhibitory: ADP, pyrrolidine	Bos taurus
N6-benzyladenosine 5'-diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition above 1 mM, recombinant catalytic fragment	Bos taurus
N6-hexyladenosine 5'-diphosphate (hydroxymethyl)pyrrolidinediol	50% inhibition at 0.51 mM, recombinant catalytic fragment	Bos taurus

Organism

Organism	UniProt	Comment	Textmining
Bos taurus	-	native protein and recombinant catalytic fragment	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
thymus	-	Bos taurus	-

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Release 2023.1 (January 2023)