Renin: Difference between revisions
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<StructureSection load='2ren' size='450' side='right' scene='' caption=''> | <StructureSection load='2ren' size='450' side='right' scene='' caption=''> | ||
[[Image:ColoredRenin.png|left|thumb|300px|alt=text|Renin]] | [[Image:ColoredRenin.png|left|thumb|300px|alt=text|Renin]] | ||
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'''Renin''', also known as angiotensinogenase, is an aspartyl protease and belongs to the protein family peptidase A1. Aspartyl proteases are endopeptidases that typically use two aspartate residues in the active site to specifically cleave peptide substrates using an acid-base hydrolysis mechanism. Mature renin circulates in the blood stream and contains 340 amino acid residues and has a mass of approximately 37 kDa. The function of renin is to cleave angiotensinogen to produce angiotensin I. | '''Renin''', also known as angiotensinogenase, is an aspartyl protease and belongs to the protein family peptidase A1. Aspartyl proteases are endopeptidases that typically use two aspartate residues in the active site to specifically cleave peptide substrates using an acid-base hydrolysis mechanism. Mature renin circulates in the blood stream and contains 340 amino acid residues and has a mass of approximately 37 kDa. The function of renin is to cleave angiotensinogen to produce angiotensin I. | ||
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==Renin Inhibitors== | ==Renin Inhibitors== | ||
[[Image:Aliskiren.jpg|thumb|400px|alt=text|Aliskiren<ref>PMID:15723979</ref>]] | [[Image:Aliskiren.jpg|thumb|400px|alt=text|Aliskiren<ref>PMID:15723979</ref>]] | ||
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<scene name='Sandbox_Reserved_489/Asymetricunit2v0z/1'>Renin with Bound Aliskiren</scene> ([[2v0z]]). | <scene name='Sandbox_Reserved_489/Asymetricunit2v0z/1'>Renin with Bound Aliskiren</scene> ([[2v0z]]). | ||
There are three generations of renin inhibitors. The first two generation molecules were peptide molecules. These peptide molecules were not specific or effective as renin inhibitors. Aliskiren, part of the 3<sup>rd</sup> generation, is a nonpeptide renin inhibitor. Small molecule nonpeptide inhibitors such as aliskiren have good pharmokenetics and are very specific for renin and not other protein peptidases. Advancements in crystallography and molecular modeling allowed the discovery of aliskiren. Aliskiren inhibits renin activity. Since renin is the rate limiting step of the RAS renin inhibition is a successful method to lower blood pressure. | There are three generations of renin inhibitors. The first two generation molecules were peptide molecules. These peptide molecules were not specific or effective as renin inhibitors. Aliskiren, part of the 3<sup>rd</sup> generation, is a nonpeptide renin inhibitor. Small molecule nonpeptide inhibitors such as aliskiren have good pharmokenetics and are very specific for renin and not other protein peptidases. Advancements in crystallography and molecular modeling allowed the discovery of aliskiren. Aliskiren inhibits renin activity. Since renin is the rate limiting step of the RAS renin inhibition is a successful method to lower blood pressure. | ||