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Digitale Medien

Design and synthesis of conformationally restricted phospholipids as phospholipase A2 inhibitors (1989)

Magolda, R. L. ; Galbraith, W.

New York, N.Y. : Wiley-Blackwell

Journal of Cellular Biochemistry 40 (1989), S. 371-386

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Details

ISSN: 0730-2312

Schlagwort(e): PLA2 substrate conformation ; modeling ; active-site inhibitors ; phospholipid side chain orientation ; pancreatic PLA2 ; Life and Medical Sciences ; Cell & Developmental Biology

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Biologie , Chemie und Pharmazie , Medizin

Notizen: 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.

Zusätzliches Material: 5 Ill.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1002/jcb.240400313

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