Agudo A, Ribeiro J M, Canales J, Cameselle J C
Unidad de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad de Extremadura, Apartado de Correos 108, E-06080 Badajoz, Spain.
Biotechnol Bioeng. 1998 Jul 5;59(1):62-7. doi: 10.1002/(sici)1097-0290(19980705)59:1<62::aid-bit8>3.0.co;2-r.
Nucleotide alkyl esters are pharmacologically important as potential (ant)agonists of purinoceptors and inhibitors of enzymes. Potato nucleotide pyrophosphatase (PNP) was compared with snake venom phosphodiesterase (SVP) as a catalyst to synthesize nucleotide alkyl esters. In methanol-water mixtures, the methanolysis/hydrolysis ratio of PNP, but not SVP, changed with pH and temperature, being optimal at high pH and low temperature. In a semi-preparative experiment, a crude PNP preparation produced 0.17 mM AMP-O-methyl ester (AMP-OMe) from 1 mM diadenosine 5',5"'-P1,P2-diphosphate (AppA) and 5M methanol, at pH 9 and 0 degrees C. Drawbacks to large-scale use are: low rates inherent to low temperatures, ATP unsuitability as a substrate for alcoholysis, and high cost of AppA. Advantages of PNP vs. SVP are cheapness, non-toxicity, and availability of the enzyme source.
核苷酸烷基酯作为嘌呤受体的潜在(抗)拮抗剂和酶抑制剂在药理学上具有重要意义。将马铃薯核苷酸焦磷酸酶(PNP)与蛇毒磷酸二酯酶(SVP)作为合成核苷酸烷基酯的催化剂进行了比较。在甲醇 - 水混合物中,PNP(而非SVP)的甲醇解/水解比率随pH值和温度变化,在高pH值和低温下最为适宜。在半制备实验中,粗制PNP制剂在pH 9和0℃条件下,由1 mM 5',5'''-P1,P2-二磷酸腺苷(AppA)和5 M甲醇生成了0.17 mM AMP - O - 甲酯(AMP - OMe)。大规模使用的缺点包括:低温固有的低反应速率、ATP不适合作为醇解底物以及AppA成本高昂。与SVP相比,PNP的优点是价格便宜、无毒且酶源易于获取。