DETECTION OF INHIBITION OF 5-AMINOIMIDAZOLE-4-CARBOXAMIDE RIBOTIDE TRANSFORMYLASE BY THIOINOSINIC ACID AND AZATHIOPRINE BY A NEW COLORIMETRIC ASSAY

被引：10

作者：

HA, TS ^{[1
]}

MORGAN, SL ^{[1
]}

VAUGHN, WH ^{[1
]}

ETO, I ^{[1
]}

BAGGOTT, JE ^{[1
]}

机构：

[1] UNIV ALABAMA,DEPT NUTR SCI,UAB STN,BOX 501,BIRMINGHAM,AL 35294

来源：

BIOCHEMICAL JOURNAL | 1990年 / 272卷 / 02期

关键词：

D O I：

10.1042/bj2720339

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The colorimetric assay for 5-aminoimidazole-4-carboxamide ribotide (AICAR) transformylase (phosphoribosylaminoimidazolecarboxamide formyltransferase; EC 2.1.2.3) has been extensively modified. The modified assay is based upon the short-term permanganate oxidation of the folate product, tetrahydrofolate (H4folate) to p-aminobenzoyl glutamate (pABG). The modified assay was used to detect the transformylase activity in crude extracts of peripheral-blood mononuclear cells (PBMCs). Azathioprine and its metabolite, thioinosinic acid (tIMP), are competitive inhibitors (with respect to AICAR) of the chicken liver transformylase and the transformylase from PBMCs of the MRL/lpr mouse, an animal model of systemic autoimmune disease. The K(i) values of tIMP and azathioprine for the chicken liver enzyme are 39±4 μM and 120±10 μM, whereas the K(i) values for the enzyme from PBMCs of the MRL/lpr mouse are 110±20 μM and 90±14 μM respectively. The anti-inflammatory drugs ibuprofen and naproxen are also inhibitors of the transformylase.

引用

页码：339 / 342

页数：4

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