Lisinopril
From Proteopedia
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| - | < | + | <StructureSection load='' size='340' side='right' caption='Lisinopril, also known as Prinivil' scene='Lisinopril/Lisinopril/1'> |
===Better Known as: Prinivil=== | ===Better Known as: Prinivil=== | ||
* Marketed By: Merck & Co.<br /> | * Marketed By: Merck & Co.<br /> | ||
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Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. | Angiotensin II has been implicated in cardiac, renal and vascular diseases. <ref>PMID:17083068</ref> Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. | ||
Lisinopril binds to the active site of <scene name='Lisinopril/Ace/1'>Angiotensin-Converting Enzyme</scene>, utilizing residues like <scene name='Lisinopril/Lisinopril_bound/1'>His 353, Ala 354 (backbone oxygen), Glue 384, Lys 511, His 513, Tyr 520, Tyr 523 and Glu 162</scene> as well as van der Waals interactions between the phenylpropyl group and Val 518. <ref>PMID:15236580</ref> Binding by Lisinopril actively inhibits ACE-1 binding and conversion of angiotensin 1 into angiotensin II. | Lisinopril binds to the active site of <scene name='Lisinopril/Ace/1'>Angiotensin-Converting Enzyme</scene>, utilizing residues like <scene name='Lisinopril/Lisinopril_bound/1'>His 353, Ala 354 (backbone oxygen), Glue 384, Lys 511, His 513, Tyr 520, Tyr 523 and Glu 162</scene> as well as van der Waals interactions between the phenylpropyl group and Val 518. <ref>PMID:15236580</ref> Binding by Lisinopril actively inhibits ACE-1 binding and conversion of angiotensin 1 into angiotensin II. | ||
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===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%"> | ||
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Pharmacokinetics
For Pharmacokinetic Data References, See: References |
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References
- ↑ Ferrario CM. Role of angiotensin II in cardiovascular disease therapeutic implications of more than a century of research. J Renin Angiotensin Aldosterone Syst. 2006 Mar;7(1):3-14. PMID:17083068
- ↑ Natesh R, Schwager SL, Evans HR, Sturrock ED, Acharya KR. Structural details on the binding of antihypertensive drugs captopril and enalaprilat to human testicular angiotensin I-converting enzyme. Biochemistry. 2004 Jul 13;43(27):8718-24. PMID:15236580 doi:10.1021/bi049480n
