Sandbox Reserved 489: Difference between revisions
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==Renin Inhibitors== | ==Renin Inhibitors== | ||
[[Image:Aliskiren.jpg|thumb| | [[Image:Aliskiren.jpg|thumb|400px|alt=text|Aliskiren<ref>PMID:15723979</ref>]] | ||
<Structure load='2v0z' size='400' frame='true' align='left' caption='Asymetric Unit of Renin with Bound Aliskiren' scene='Sandbox_Reserved_489/Asymetricunit2v0z/1' /> | <Structure load='2v0z' size='400' frame='true' align='left' caption='Asymetric Unit of Renin with Bound Aliskiren' scene='Sandbox_Reserved_489/Asymetricunit2v0z/1' /> | ||
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 3rd 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 3rd 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. | ||
