Pyridoxal phosphate. 5. 2-Formylethynylphosphonic acid and 2-formylethylphosphonic acid, potent inhibitors of pyridoxal phosphate binding and probes of enzyme topography
- 1 December 1976
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 19 (12) , 1367-1371
- https://doi.org/10.1021/jm00234a003
Abstract
The title compounds (17 and 21) were prepared in good yield by synthesis of the phosphonate diester acetals, deesterification with chloro- or bromotrimethylsilane, hydrolysis of the acetal group and formation of the characterized Ba salts. The 3-C aldehydophosphonic acids (17 and 21) were potent inhibitors (Ki = 2 .times. 10-6) of pyridoxal phosphate (PPal) binding to apoaspartate aminotransferase (AAT) and are believed to span between and bind to the enzymic functional groups which bind the aldehyde and phosphate groups of PPal.This publication has 3 references indexed in Scilit:
- Isolation and Characterization of Multiple Forms of Glutamate-Aspartate Aminotransferase from Pig HeartJournal of Biological Chemistry, 1967
- The action of sulphate and phosphate esters of oestrogens on the reconstitution of two pyridoxal 5-phosphate-dependent enzymesBiochemical Journal, 1962
- GLUTAMIC ASPARTIC TRANSAMINASE .1. ASSAY, PURIFICATION, AND GENERAL PROPERTIES1959