Sandbox 123456: Difference between revisions
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==Mechanism== | ==Mechanism== | ||
When administered, Posaconazole acts as an antifungal by blocking Lanosterol <scene name='75/756730/Protein_ligand/1'>14-α- demethylase </scene>x, a P-450 dependant fungal enzyme containing heme as a cofactor. Posaconazole binds to the heme cofactor that the enzyme contains, which prevents the fungus from creating ergosterol, an essential component of the fungal cell membrane. Ergosterol performs in fungal cells how cholesterol does in animal cells, making the cell membrane less permeable. Without it, the cells can no longer proliferate and eventually die because the cell membranes become “leaky”, releasing essential organic components from the cell’s interior and preventing it from performing normal cellular functions. In this way, Posaconazole acts both as fungicidal and fungistatic. | When administered, Posaconazole acts as an antifungal by blocking Lanosterol <scene name='75/756730/Protein_ligand/1'>14-α- demethylase </scene>x, a P-450 dependant fungal enzyme containing heme as a cofactor (Groll)(). Posaconazole binds to the heme cofactor that the enzyme contains, which prevents the fungus from creating ergosterol, an essential component of the fungal cell membrane. Ergosterol performs in fungal cells how cholesterol does in animal cells, making the cell membrane less permeable. Without it, the cells can no longer proliferate and eventually die because the cell membranes become “leaky”, releasing essential organic components from the cell’s interior and preventing it from performing normal cellular functions. In this way, Posaconazole acts both as fungicidal and fungistatic. | ||
== Relevance == | == Relevance == | ||
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== References == | == References == | ||
<references/> (need to fix) | <references/> (need to fix) | ||
1. Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS. Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID: 21059682 | 1. Dekkers, B. G. J., Bakker, M., van der Elst, K. C. M., Sturkenboom, M. G. G., Veringa, A., Span, L. F. R., & Alffenaar, J.-W. C. (2016). Therapeutic Drug Monitoring of Posaconazole: an Update. Current Fungal Infection Reports, 10, 51–61. http://doi.org/10.1007/s12281-016-0255-4 | ||
2. Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS. Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID: 21059682 | |||
3. Groll, A. H., & Walsh, T. J. (2005). Posaconazole: clinical pharmacology and potential for management of fungal infections. Expert Review of Anti-infective Therapy, 3(4), 467-487. doi:10.1586/14787210.3.4.467 | |||
4. Nagappan V, Deresinski S: Reviews of anti-infective agents: posaconazole: a broad-spectrum triazole antifungal agent. Clin Infect Dis. 2007 Dec 15;45(12):1610-7. doi: 10.1086/523576. [PubMed:18190324 ] | |||
5. National Center for Biotechnology Information. PubChem Compound Database; CID=468595, https://pubchem.ncbi.nlm.nih.gov/compound/468595 | |||
