Inhibition of angiotensin converting enzyme and potentiation of bradykinin by retro-inverso analogues of short peptides and sequences related to angiotensin I and bradykinin
作者:Adriana K. Carmona、Luiz Juliano
DOI:10.1016/0006-2952(96)00047-0
日期:1996.4
pharmacological evidence indicating that, in addition to the inhibition of angiotensin converting enzyme (ACE; EC 3.4.15.1), the potentiation of bradykinin (BK) responses may also involve the BK receptor or some binding site in the structures involved in the contractile response to this peptide. Dipeptides such as Val-Trp and some of its analogues as well as tripeptide homologues, including total and partial retro-inverso
有药理学证据表明,除了抑制血管紧张素转化酶(ACE; EC 3.4.15.1),缓激肽(BK)反应的增强作用还可能涉及BK受体或参与收缩的结构中的某些结合位点对这种肽的反应。合成了二肽(如Val-Trp及其一些类似物)以及三肽同源物(包括全部和部分逆反肽),并测定了它们抑制纯化的豚鼠血浆ACE以及增强BK对分离物的作用的能力。回肠相同的物种。含有P2-P1,P1-P'1和P'1-P'2反向酰胺键的肽可抑制ACE,对水解具有抵抗力,并且取决于氨基酸组成,其中一些增强了对BK的收缩反应,而另一些则没有。Des- [Arg1] -BK,在高于10(-5)M的浓度下具有固有活性,与非常相似的血管紧张素I(AI)类似物[Cys5-Cys10]-血管紧张素I-(5-10)-没有可检测的收缩活性的酰胺能够抑制ACE并增强BK。与这些肽相反,Bothrops jararaca毒液的BPP5a和BPP9a以及Agkistrodon