Metabolism-resistant bradykinin antagonists: development and applications.
Bradykinin plays many roles in normal and pathological physiology, but rapid enzymatic degradation made elucidation of its functions extremely difficult. Development of effective degradation-resistant antagonists made it possible to delineate these roles and to open the way for development of new drugs to control pathology due to excess production of bradykinin. Presently available peptide bradykinin antagonists are extremely potent, are completely resistant to enzymatic degradation, and are orally available. Non-peptide bradykinin antagonists have also been discovered. Development of bradykinin antagonists as drugs for cancer, inflammation and trauma is anticipated.
Stewart
J M
JM
Department of Biochemistry and Molecular Genetics, University of Colorado School of Medicine, Denver 80262, USA.
Gera
L
L
York
E J
EJ
Chan
D C
DC
Whalley
E J
EJ
Bunn
P A
PA
Vavrek
R J
RJ
D000818:Animals; D001681:Biological Assay; D006801:Humans; D007705:Kinins / Q000378:metabolism*; D010455:Peptides / Q000494:pharmacology; D011956:Receptors, Cell Surface / Q000819:agonists / Q000037:antagonists & inhibitors / Q000145:classification*; D013045:Species Specificity
D007705:Kinins; D010455:Peptides; D011956:Receptors, Cell Surface