CHEM2052 Tutorial Example4: Difference between revisions

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== '''Chem2052: Example 4 - Renin''' ==
== '''Chem2052: Example 4 - Renin''' ==


The spinning structure you initially view on this page is a protease called Renin. Renin is an '''aspartyl protease''', which cleaves a particular peptide called angiotensinogen.
The spinning structure you initially view on this page is a protease called '''Renin''' (also known as '''angiotensinase'''). Renin is an '''aspartyl protease''', which cleaves a particular peptide called angiotensinogen. Although this enzyme functions as a monomer the crystal structure obtained is a dimer and this is what you can see here. In the following representations one of the sub-units has been removed to represent the protein in its natural state.


== '''Background''' ==
== '''Background''' ==


In later lecture we will look a little more closely at '''Renin''' (also known as '''angiotensinase'''). This enzyme is involved in a biological pathway leading to elevation of blood pressure, which can be beneficial in many ways. However if this process has become overactive, hypertension (high blood pressure) can result. Hypertension leads to cardiovascular disease which is the leading cause of death globally. The World Health Organisation states "An estimated 17.3 million people died from cardiovascular disease in 2008, representing 30% of all global deaths" see the following web page if you want to know more: [http://www.who.int/mediacentre/factsheets/fs317/en/ Cardiovascular disease facts WHO].
In later lecture we will look a little more closely at '''Renin'''. This enzyme is involved in a biological pathway leading to elevation of blood pressure, which can be beneficial in many ways. However if this process has become overactive, hypertension (high blood pressure) can result. Hypertension leads to cardiovascular disease which is the leading cause of death globally. The World Health Organisation states "An estimated 17.3 million people died from cardiovascular disease in 2008, representing 30% of all global deaths" see the following web page if you want to know more: [http://www.who.int/mediacentre/factsheets/fs317/en/ Cardiovascular disease facts WHO].


Since the 1970s scientists have been trying to modulate the action of renin by blocking the active site of the enzyme and preventing its function, hence lowering blood pressure. Aliskerin is the only renin inhibitor in clinical use today [http://en.wikipedia.org/wiki/Renin_inhibitor Renin information Site]. However there is still interest in developing new, improved inhibitors. This question looks at a renin inhibitor identified through research at Pfizer.<ref>PMID:17574423</ref>
Since the 1970s scientists have been trying to modulate the action of renin by blocking the active site of the enzyme and preventing its function, hence lowering blood pressure. Aliskerin is the only renin inhibitor in clinical use today [http://en.wikipedia.org/wiki/Renin_inhibitor Renin information Site]. However there is still interest in developing new, improved inhibitors. This question looks at a renin inhibitor identified through research at Pfizer.<ref>PMID:17574423</ref>