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Design and synthesis of conformationally restricted phospholipids as phospholipase A2 inhibitors.

作者信息

Magolda R L, Galbraith W

机构信息

Central Research and Development Department, E.I. du Pont de Nemours & Co., Wilmington, Delaware 19880.

出版信息

J Cell Biochem. 1989 Jul;40(3):371-86. doi: 10.1002/jcb.240400313.

DOI:10.1002/jcb.240400313
PMID:2777909
Abstract

The use of conformationally restricted phospholipids 1 and 2 has been employed to understand the conformational preference of phospholipase A2 (PLA2) for substrate phospholipids. Inhibition of porcine pancreatic PLA2 with 1 and 2 indicated a two- to fivefold preference for the distal isomer 2 over the proximal isomer 1. Based upon these studies, both side-chains of the substrate phospholipid appear to occupy the lipid binding domains near the active site with the side-chains further apart most preferred by PLA2.

摘要

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