Ace inhibitors - activators of kinin receptors

Kugaevskaya E.V.1 , Elisseeva Yu.E.1

1. Institute of Biomedical Chemistry, Russian Academy of Medical Sciences (RAMS)
Section: Review
DOI: 10.18097/PBMC20115703282      PubMed Id: 21863742
Year: 2011  Volume: 57  Issue: 3  Pages: 282-299
Angiotensin converting enzyme (ACE) inhibitors are widely used for treatment of cardiovascular diseases. The effects of ACE inhibitors on the human bradykinin receptors were investigated. The mode of action of ACE inhibitors is considered. There is evidence that ACE inhibitors exert effects on the vascular system that cannot be attributed simply to the inhibition of ACE activity and accumulation of locally produced bradykinin. ACE inhibitors augment bradykinin effects on receptors indirectly by inducing cross-talk between ACE and the B2 receptor when enzyme and receptor molecules are sterically close, possibly forming a heterodimer. ACE inhibitors activate B1 receptors directly and independently of ACE via the zink-binding consensus sequence HEXXH, which is present in B1, but not in B2 receptor. Particular structure of B2 and B1 are represented, as well as receptor amino acids coupled with the G-proteins. Activation of kinin receptors by ACE inhibitors leads to clinically beneficial effects of ACE inhibitors.
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Keywords: kinin receptors, angiotensin converting enzyme inhibitors, cardiovascular protection

Kugaevskaya, E. V., Elisseeva, Yu. E. (2011). Ace inhibitors - activators of kinin receptors. Biomeditsinskaya Khimiya, 57(3), 282-299.
This paper is also available as the English translation: 10.1134/S1990750810040013
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