Inactivation of gamma-glutamylcysteine synthetase by SAPH-3 disulfide: role of the histaminyl moiety.

Abstract:

:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural analogues of 2a indicate that the histamine moiety plays a significant role in enzyme inactivation. Substitution of methyl groups on the carbon atoms adjacent to both sulfur atoms of the disulfide drastically decreases inhibitory action, probably due to a steric repulsion near the sulfur atom at the enzyme active site.

journal_name

J Pharm Sci

authors

Schor NF,Cheng B,Siuda JF

doi

10.1002/jps.2600800404

subject

Has Abstract

pub_date

1991-04-01 00:00:00

pages

311-2

issue

4

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)48518-1

journal_volume

80

pub_type

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