Biochemical Pharmacology 1983-04-15

The inhibition of catechol-O-methyltransferase by 2,3-dihydroxypyridine.

M J Raxworthy, I R Youde, P A Gulliver

Index: Biochem. Pharmacol. 32(8) , 1361-4, (1983)

Full Text: HTML

Abstract

Despite its structural similarity to catechol, 2,3-dihydroxypyridine is not a substrate but a "dead-end" inhibitor of purified pig liver catechol-O-methyltransferase. It inhibits the methylation of 3,4-dihydroxyphenylacetic acid competitively with an inhibitor constant of 15 microM. Against the methyl donor, S-adenosyl-L-methionine, it is an uncompetitive inhibitor (Ki = 85 microM). Clearly, although 2,3-dihydroxypyridine interacts with the catechol-binding site of the enzyme, the presence of a nitrogen in the ring alters its susceptibility to O-methylation.


Related Compounds

Related Articles:

Identifying chelators for metalloprotein inhibitors using a fragment-based approach.

2011-01-27

[J. Med. Chem. 54 , 591-602, (2011)]

Pyrogallol and its analogs can antagonize bacterial quorum sensing in Vibrio harveyi.

2008-03-01

[Bioorg. Med. Chem. Lett. 18 , 1567-72, (2008)]

Connection of metallamacrocycles via dynamic covalent chemistry: a versatile method for the synthesis of molecular cages.

2011-05-11

[J. Am. Chem. Soc. 133(18) , 7106-15, (2011)]

A novel pathway for nicotine degradation by Aspergillus oryzae 112822 isolated from tobacco leaves.

2010-09-01

[Res. Microbiol. 161(7) , 626-33, (2010)]

Effects of mimosine and 2,3-dihydroxypyridine on fiber shedding in Angora goats.

1999-05-01

[J. Anim. Sci. 77(5) , 1224-9, (1999)]

More Articles...