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url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url url
  2. Weltenzyklopädie
  3. CYP1A2 - ویکی‌پدیا، دانشنامهٔ آزاد
CYP1A2 - ویکی‌پدیا، دانشنامهٔ آزاد
از ویکی‌پدیا، دانشنامهٔ آزاد
CYP1A2
ساختارهای موجود
PDBجستجوی هم‌ساخت‌شناسی: PDBe RCSB
معین‌کننده‌ها
نام‌های دیگرCYP1A2, CP12, P3-450, P450(PA), cytochrome P450 family 1 subfamily A member 2, Cytochrome P450 1A2, CYPIA2
شناسه‌های بیرونیOMIM: 124060 MGI: 88589 HomoloGene: 68082 GeneCards: CYP1A2
هم‌ساخت‌شناسی
گونه‌هاانسانموش
Entrez

1544

13077

آنسامبل

ENSG00000140505

ENSMUSG00000032310

یونی‌پروت

P05177

P00186

RefSeq (mRNA)

NM_000761

NM_009993

RefSeq (پروتئین)

NP_000752

NP_034123

موقعیت (UCSC)ن/مChr : 57.58 – 57.59 Mb
جستجوی PubMed[۲][۳]
ویکی‌داده
مشاهده/ویرایش انسانمشاهده/ویرایش موش

سیتوکروم پی۴۵۰ ۱ای۲ (به اختصار CYP1A2)، عضوی از سیستم اکسیداز با عملکرد مخلوط سیتوکروم P450 است که در متابولیسم بیگانه‌زیستها در بدن انسان نقش دارد.[۴] در انسان، آنزیم CYP1A2 توسط ژن CYP1A2 کدگذاری می‌شود.[۵]

لیگاندها

در زیر جدولی از منتخب بسترها، القاء کننده‌ها و مهارکننده‌های CYP1A2 آمده‌است.

مهار کننده‌های CYP1A2 را می‌توان بر اساس قدرت آنها طبقه‌بندی کرد، مانند:

  • قوی، که باعث افزایش حداقل ۵ برابری در مقادیر AUC پلاسما یا کاهش بیش از ۸۰٪ در کلیرانس بسترها می‌شود.[۶]
  • متوسط، که باعث افزایش حداقل ۲ برابری در مقادیر AUC پلاسما یا کاهش ۵۰ تا ۸۰ درصدی در کلیرانس بسترها می‌شود.[۶]
  • ضعیف، که باعث افزایش حداقل ۱٫۲۵ برابری اما کمتر از ۲ برابری در مقادیر AUC پلاسما یا کاهش ۲۰–۵۰٪ در کلیرانس بسترها می‌شود.[۶]
بسترها مهارکننده‌ها القاکننده‌ها
قوی:

متوسط

ضعیف

قدرت نامشخص:

القا کننده های متوسط:[۸]

قدرت نامشخص:

همچنین ببینید

منابع

  1. ↑ ۱٫۰ ۱٫۱ ۱٫۲ GRCm38: Ensembl release 89: ENSMUSG00000032310 - Ensembl, May 2017
  2. ↑ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  3. ↑ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ↑ Nelson DR, Zeldin DC, Hoffman SM, Maltais LJ, Wain HM, Nebert DW (Jan 2004). "Comparison of cytochrome P450 (CYP) genes from the mouse and human genomes, including nomenclature recommendations for genes, pseudogenes and alternative-splice variants". Pharmacogenetics. 14 (1): 1–18. doi:10.1097/00008571-200401000-00001. PMID 15128046.
  5. ↑ Jaiswal AK, Nebert DW, McBride OW, Gonzalez FJ (1987). "Human P(3)450: cDNA and complete protein sequence, repetitive Alu sequences in the 3' nontranslated region, and localization of gene to chromosome 15". Journal of Experimental Pathology. 3 (1): 1–17. PMID 3681487.
  6. ↑ ۶٫۰ ۶٫۱ ۶٫۲ Center for Drug Evaluation and Research. "Drug Interactions & Labeling - Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers". www.fda.gov (به انگلیسی). Retrieved 2016-06-01.
  7. ↑ ۷٫۰ ۷٫۱ ۷٫۲ ۷٫۳ Sousa MC, Braga RC, Cintra BA, de Oliveira V, Andrade CH (2013). "In silico metabolism studies of dietary flavonoids by CYP1A2 and CYP2C9". Food Research International. 50: 102–110. doi:10.1016/j.foodres.2012.09.027.
  8. ↑ ۸٫۰۰ ۸٫۰۱ ۸٫۰۲ ۸٫۰۳ ۸٫۰۴ ۸٫۰۵ ۸٫۰۶ ۸٫۰۷ ۸٫۰۸ ۸٫۰۹ ۸٫۱۰ ۸٫۱۱ ۸٫۱۲ ۸٫۱۳ ۸٫۱۴ ۸٫۱۵ ۸٫۱۶ ۸٫۱۷ ۸٫۱۸ ۸٫۱۹ ۸٫۲۰ ۸٫۲۱ "Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers". FDA. 26 May 2021.
  9. ↑ Alkattan, A. , & Alsalameen, E. (2021). Polymorphisms of genes related to phase-I metabolic enzymes affecting the clinical efficacy and safety of clopidogrel treatment. Expert opinion on drug metabolism & toxicology, 10.1080/17425255.2021.1925249. Advance online publication. https://doi.org/10.1080/17425255.2021.1925249
  10. ↑ ۱۰٫۰۰ ۱۰٫۰۱ ۱۰٫۰۲ ۱۰٫۰۳ ۱۰٫۰۴ ۱۰٫۰۵ ۱۰٫۰۶ ۱۰٫۰۷ ۱۰٫۰۸ ۱۰٫۰۹ ۱۰٫۱۰ ۱۰٫۱۱ ۱۰٫۱۲ ۱۰٫۱۳ ۱۰٫۱۴ ۱۰٫۱۵ ۱۰٫۱۶ ۱۰٫۱۷ ۱۰٫۱۸ ۱۰٫۱۹ ۱۰٫۲۰ ۱۰٫۲۱ ۱۰٫۲۲ ۱۰٫۲۳ ۱۰٫۲۴ ۱۰٫۲۵ ۱۰٫۲۶ ۱۰٫۲۷ ۱۰٫۲۸ ۱۰٫۲۹ ۱۰٫۳۰ ۱۰٫۳۱ ۱۰٫۳۲ ۱۰٫۳۳ ۱۰٫۳۴ ۱۰٫۳۵ ۱۰٫۳۶ ۱۰٫۳۷ ۱۰٫۳۸ ۱۰٫۳۹ ۱۰٫۴۰ ۱۰٫۴۱ Flockhart DA (2007). "Drug Interactions Flockhart Table". Indiana University School of Medicine.
  11. ↑ ۱۱٫۰۰ ۱۱٫۰۱ ۱۱٫۰۲ ۱۱٫۰۳ ۱۱٫۰۴ ۱۱٫۰۵ ۱۱٫۰۶ ۱۱٫۰۷ ۱۱٫۰۸ ۱۱٫۰۹ ۱۱٫۱۰ ۱۱٫۱۱ ۱۱٫۱۲ ۱۱٫۱۳ ۱۱٫۱۴ ۱۱٫۱۵ Swedish environmental classification of pharmaceuticals - دارونامه - Facts for prescribers (Fakta för förskrivare). Retrieved July 2011
  12. ↑ Savage RA, Zafar N, Yohannan S, Miller JM (2021). "article-35398". Melatonin. Treasure Island (FL): StatPearls Publishing. PMID 30521244. Retrieved 2021-11-15. Ninety percent of melatonin is metabolized in the liver primarily by the enzyme CYP1A2
  13. ↑ "Erlotinib". Metabolized primarily by CYP3A4 and, to a lesser degree, by CYP1A2 and the extrahepatic isoform CYP1A1
  14. ↑ ۱۴٫۰ ۱۴٫۱ "Verapamil: Drug information. Lexicomp". UpToDate. Retrieved 2019-01-13. Metabolism/Transport Effects: Substrate of CYP1A2 (minor), CYP2B6 (minor), CYP2C9 (minor), CYP2E1 (minor), CYP3A4 (major), P-glycoprotein/ABCB1; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP1A2 (weak), CYP3A4 (moderate), P-glycoprotein/ABCB1
  15. ↑ Dostalek M, Pistovcakova J, Jurica J, Sulcová A, Tomandl J (Sep 2011). "The effect of St John's wort (hypericum perforatum) on cytochrome p450 1a2 activity in perfused rat liver". Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia. 155 (3): 253–7. doi:10.5507/bp.2011.047. PMID 22286810.
  16. ↑ "Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers". U.S. Food and Drug Administration. 2019-02-09.
  17. ↑ Gorski JC, Huang SM, Pinto A, Hamman MA, Hilligoss JK, Zaheer NA, Desai M, Miller M, Hall SD (Jan 2004). "The effect of echinacea (Echinacea purpurea root) on cytochrome P450 activity in vivo". Clinical Pharmacology and Therapeutics. 75 (1): 89–100. doi:10.1016/j.clpt.2003.09.013. PMID 14749695. S2CID 8375888.
  18. ↑ ۱۸٫۰ ۱۸٫۱ ۱۸٫۲ Briguglio M, Hrelia S, Malaguti M, Serpe L, Canaparo R, Dell'Osso B, et al. (December 2018). "Food Bioactive Compounds and Their Interference in Drug Pharmacokinetic/Pharmacodynamic Profiles". Pharmaceutics. 10 (4): 277. doi:10.3390/pharmaceutics10040277. PMC 6321138. PMID 30558213.
  19. ↑ Fuhr U, Klittich K, Staib AH (Apr 1993). "Inhibitory effect of grapefruit juice and its bitter principal, naringenin, on CYP1A2 dependent metabolism of caffeine in man". British Journal of Clinical Pharmacology. 35 (4): 431–6. doi:10.1111/j.1365-2125.1993.tb04162.x. PMC 1381556. PMID 8485024.
  20. ↑ ۲۰٫۰ ۲۰٫۱ ۲۰٫۲ ۲۰٫۳ Sanday, Kate (17 October 2011), "South Asians and Europeans react differently to common drugs", University of Sydney Faculty of Pharmacy News
  21. ↑ Wen X, Wang JS, Neuvonen PJ, Backman JT (Jan 2002). "Isoniazid is a mechanism-based inhibitor of cytochrome P450 1A2, 2A6, 2C19 and 3A4 isoforms in human liver microsomes". Eur J Clin Pharmacol. 57 (11): 799–804. doi:10.1007/s00228-001-0396-3. PMID 11868802. S2CID 19299097.
  22. ↑ Zhao Y, Hellum BH, Liang A, Nilsen OG (June 2015). "Inhibitory Mechanisms of Human CYPs by Three Alkaloids Isolated from Traditional Chinese Herbs". Phytotherapy Research. 29 (6): 825–34. doi:10.1002/ptr.5285. PMID 25640685. S2CID 24002845.

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