Title : Critical roles of residues 36 and 40 in the phenol and tertiary amine aglycone substrate selectivities of UDP-glucuronosyltransferases 1A3 and 1A4.

Pub. Date : 2007 Oct

PMID : 17636046






2 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 UGT1A3 glucuronidates the planar phenols 1-naphthol (1-NP) and 4-methylumbelliferone (4-MU), whereas UGT1A4 converts the tertiary amines lamotrigine (LTG) and trifluoperazine (TFP) to quaternary ammonium glucuronides. Amines UDP glucuronosyltransferase family 1 member A4 Homo sapiens
2 Thus, residues 36 and 40 of UGT1A3 and UGT1A4 are pivotal for the respective selectivities of these enzymes toward planar phenols and tertiary amines, although other regions of the proteins influence binding affinity and/or turnover. Amines UDP glucuronosyltransferase family 1 member A4 Homo sapiens