title: Competitive inhibition of lipolytic enzymes. V. A monolayer study using enantiomeric acylamino analogues of phospholipids as potent competitive inhibitors of porcine pancreatic phospholipase A2.
abstract: For the first time, we have shown that a stereospecific interaction occurs between porcine pancreatic phospholipase A2 and a monomolecular film of amidophospholipid used as inhibitor. Direct binding experiments, using radiolabelled phospholipase A2, showed that 13 times more enzyme was bound to phospholipid films of the L series by comparison with films of the D series. These results were confirmed by indirect binding studies using re-spreading experiments. Kinetic studies of the porcine pancreatic PLA2, using enantiomeric acyl-amino phospholipid analogues, have shown that: (1) inhibitors of the L series are more potent than inhibitors of the D series, (2) inhibitors having a negative charge are more potent than zwitterionic inhibitors, (3) inhibitory power values are greater when evaluated in micellar system than in a the monolayer system, (4) the inhibitory power increases continuously with surface pressure.
authors.affiliation: Centre de Biochimie et de Biologie Moléculaire, C.N.R.S., Marseille, France.
authors.forename: S
authors.initials: S
authors.lastname: Ransac
authors.forename: A M
authors.initials: AM
authors.lastname: Deveer
authors.forename: C
authors.initials: C
authors.lastname: Rivière
authors.forename: A J
authors.initials: AJ
authors.lastname: Slotboom
authors.forename: C
authors.initials: C
authors.lastname: Gancet
authors.forename: R
authors.initials: R
authors.lastname: Verger
authors.forename: G H
authors.initials: GH
authors.lastname: De Haas
mesh_terms: D000818:Animals; D007700:Kinetics; D010179:Pancreas / Q000201:enzymology*; D010741:Phospholipases A / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054467:Phospholipases A2; D010743:Phospholipids / Q000494:pharmacology*; D013379:Substrate Specificity; D013552:Swine
chemical_list: D010743:Phospholipids; D010741:Phospholipases A; D054467:Phospholipases A2