Bradykinin-potentiating peptide

Scheme 13 Solid-Phase Synthesis of [gLys6,(f S)-mPhe7,Ala8]-Bradykinin Potentiating Peptide,.,161...

Nine bradykinin-potentiating peptides (BPP5) were isolated from the Bothropos jararaca venom by Ferreira, Greene and co-workers (82,83). 

Kato, H. and Suzuki, T. 1971. Bradykinin-potentiating peptides from the venom of Agkistrodon halysblomhojfii. Isolation of five bradykinin potentiators and the amino acid sequences of two of them, potentiators B and C. Biochemistry 10, 972—980. 

The teprotide BPP9a (bradykinin-potentiating peptide) 76 and analogous BPP peptides170), which have been isolated from snake venom, are taken up by ACE in competition with the substrate angiotensin I with far greater affinity. 

Norinder, U. (1991). Theoretical Amino Acid Descriptors. Application to Bradykinin Potentiating Peptides. Peptides, 12,1223-1227. 

ACE inhibitor drugs were developed by modelling interaction with the active site of the enzyme of a snake-venom-derived bradykinin-potentiating peptide, and from this the necessary structure of non-peptide inhibitors was inferred. The first such ACE inhibitor used medicinally was caplopril. Later examples in clinical use include cilazapril, enalapril, fosinopril, lisinopril, perindopril, quinapril, ramipril, trandolapril. Several ACE inhibitors are now administered clinically as prodrugs - which have good bioavailability, but are inactive in their own right. They are then converted to the active molecule in vivo, usually by esterases (e.g. enalapril to enalaprilat. and ramipril to ramiprilat). 

Thi ,DPhe BK [Thi ,DPhe ]-bradykinin. bradykinin-potentiating peptide teprotide. bradykinin potentiator B teprotide. BRADYKININ RECEPTOR AGONISTS act at sites recognizing members and derivatives of the bradykinin family of hormone peptides - kinins - of which bradykinin (BK) and kallidin (lysyl-bradykinin Lys-BK KD) are the main mammalian members. The bradykinin family is distinct from the tachykinin family of peptides, though both have profound hypotensive actions and contract many intestinal and other smooth muscles. Historically, it was noted that the former action was relatively slow-developing, hence the name bradykinin. Notable actions of bradykinin and kallidin are to dilate blood vessels and increase their permeability to plasma proteins, and to stimulate sensory nerve C-fibres. These actions are pro-inflammatory, and reflect the fact that the kinin-formation system is activated in inflammation, and enzymes (kallikreins) form the kinins from blood-borne or tissue precursors (kininogens) on injurious insult. 

---