CYP3A4: Difference between revisions
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== Overview == | == Overview == | ||
'''Cytochrome P450 3A4''' (CYP3A4) is in the heme-thiolate monooxygenase enzyme family meaning the protein contains a heme group with an iron atom. Enzymes in Cytochrome P450 are oxidizing enzymes and CYP3A4 works in the body oxidizing foreign molecules such as toxins and drugs<ref name="a">PMID:16389357</ref><ref name="b">PMID:15603755</ref>. It appears almost half of the marketed pharmaceutical drugs are metabolized by CYP3A4 [http://www.pharmacytimes.com/publications/issue/2008/2008-09/2008-09-8687] All Cytochrome P450 are essential enzymes for metabolism and the enzyme CYP3A4 is the most important. [http://www.medsafe.govt.nz/profs/PUArticles/March2014DrugMetabolismCytochromeP4503A4.htm] Primarily found in the liver and intestine, CYP3A4 is localized in the endoplasmic reticulum membrane [http://www.uniprot.org/uniprot/P08684] and are present in all eukaryotic organisms as well as some prokaryotes<ref name="c">PMID: 15352783</ref>. While CYP3A4's role in drug metabolism are numerous, they are often aiding deactivation through facilitated excretion from the system or by direct inactivation. [https://en.wikipedia.org/wiki/CYP3A4#Tissue_distribution] | '''Cytochrome P450 3A4''' (CYP3A4) is in the heme-thiolate monooxygenase enzyme family meaning the protein contains a heme group with an iron atom. Enzymes in [[Cytochrome P450]] are oxidizing enzymes and CYP3A4 works in the body oxidizing foreign molecules such as toxins and drugs<ref name="a">PMID:16389357</ref><ref name="b">PMID:15603755</ref>. It appears almost half of the marketed pharmaceutical drugs are metabolized by CYP3A4 [http://www.pharmacytimes.com/publications/issue/2008/2008-09/2008-09-8687] All Cytochrome P450 are essential enzymes for metabolism and the enzyme CYP3A4 is the most important. [http://www.medsafe.govt.nz/profs/PUArticles/March2014DrugMetabolismCytochromeP4503A4.htm] Primarily found in the liver and intestine, CYP3A4 is localized in the endoplasmic reticulum membrane [http://www.uniprot.org/uniprot/P08684] and are present in all eukaryotic organisms as well as some prokaryotes<ref name="c">PMID: 15352783</ref>. While CYP3A4's role in drug metabolism are numerous, they are often aiding deactivation through facilitated excretion from the system or by direct inactivation. [https://en.wikipedia.org/wiki/CYP3A4#Tissue_distribution] | ||
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The gene encoding CYP3A4 is located on chromosome 7 in the human genome<ref name="e">PMID: 1391968</ref> and it has been found that there are significant variants of the protein correlating to race <ref name="f"> PMID: 11714865</ref>. This finding is relevant due to the proteins altered ability to react with substrates such as testosterone <ref name="g">PMID: 11714865</ref>. | The gene encoding CYP3A4 is located on chromosome 7 in the human genome<ref name="e">PMID: 1391968</ref> and it has been found that there are significant variants of the protein correlating to race <ref name="f"> PMID: 11714865</ref>. This finding is relevant due to the proteins altered ability to react with substrates such as testosterone <ref name="g">PMID: 11714865</ref>. | ||
The | The <scene name='72/728174/N_to_c_terminus/1'>alpha helices</scene> can be seen colored in rainbow succession from the N to C terminus. The protein pocket, where the reactions are catalyzed, more specifically, the <scene name='72/728174/Heme_binding_site/1'>heme binding site</scene> contains twenty-two residues [http://www.rcsb.org/pdb/explore/remediatedSequence.do?structureId=4NY4] but the main interaction is with a Cysteine at position 442, which coordinates with iron. [http://www.uniprot.org/uniprot/P08684]. | ||
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[[Image:First-pass metabolism.jpg]] | [[Image:First-pass metabolism.jpg]] | ||
</StructureSection> | </StructureSection> | ||
<b>References</b><br> | |||
<references/> | |||
[[Category:Topic Page]] | |||
