Selective inhibitors of plasma kallikrein.
Based on a tetrapeptide fragment [Pro387-Ser390] of HK we have developed a series of potent low molecular weight (5-600 Da) inhibitors of PK which are stable to the enzyme. These inhibitors show good selectivity for PK versus tissue kallikrein, thrombin and plasmin. Such inhibitors will help define the role of PK and kinins in human physiology and pathophysiology. They may also find clinical use in the treatment of diseases where kinins are important mediators.
Evans
D M
DM
Ferring Research Institute, University of Southampton Research Centre, Chilworth, UK.
Jones
D M
DM
Pitt
G R
GR
Sueiras-Diaz
J
J
Horton
J
J
Ashworth
D
D
Olsson
H
H
Szelke
M
M
D000595:Amino Acid Sequence; D000596:Amino Acids / Q000032:analysis; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007610:Kallikreins / Q000037:antagonists & inhibitors*; D008969:Molecular Sequence Data
D000596:Amino Acids; D004791:Enzyme Inhibitors; D007610:Kallikreins