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1H-NMR and protection studies of interactions between ligands and bovine pancreatic phospholipase A2.

作者信息

Williamson M P, Davis P D, Broadhurst M J, Nixon J S

机构信息

Roche Products Ltd., Welwyn Garden City, U.K.

出版信息

Biochim Biophys Acta. 1989 Jul 27;997(1-2):9-14. doi: 10.1016/0167-4838(89)90129-5.

DOI:10.1016/0167-4838(89)90129-5
PMID:2752056
Abstract

A number of long-chain amines and naphthylamine sulfonates have been studied for their ability to inhibit bovine pancreatic phospholipase A2 (PLA2) and to protect PLA2 against alkylation of the active site histidine by p-bromophenacyl bromide. Their areas of interaction on the enzyme were further delineated using observations of chemical shift changes of assigned aromatic signals in the 1H-NMR spectrum of PLA2, while the bound conformations of two amine inhibitors were revealed using transferred nuclear Overhauser effects. The alkyl amines bind rather non-specifically on the surface of the enzyme, over the active site cleft and the interface recognition site.

摘要

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