The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
CYTOCHROME P-450 3A4: Regulation and Role in Drug Metabolism
Abstract
▪ Abstract Cytochrome P-450 (P-450) 3A4 is the most abundant P-450 expressed in human liver and small intestine. P-450 3A4 contributes to the metabolism of approximately half the drugs in use today, and variations in its catalytic activity are important in issues of bioavailability and drug-drug interactions. The gene is known to be inducible by barbiturates, glucocorticoids, and rifampicin in humans and in isolated hepatocytes, although the mechanism remains unclear. The 5′-untranslated region includes putative basal transcription element, hepatocyte nuclear factor, p53, AP-3, glucocorticoid regulatory element, pregnane X receptor, and estrogen receptor element sequences. Recently, the GRE element has been shown to act in a classic glucocorticoid response. Several issues remain to be resolved regarding the catalytic activity of the P-450 3A4 protein, including rate-limiting steps and the need for cytochrome b 5, divalent cations, and acidic phospholipid systems for optimal activity. Another issue involves the basis of the homotropic and heterotropic cooperativity seen with the enzyme. The in vivo significance of these findings remains to be further established. In addition to more basic studies on P-450 3A4, several areas of practical interest to the pharmaceutical industry require development.
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Shimada, T., Yamazaki, H., Mimura, M., Inui, Y., & Guengerich, F. P. (1994) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)22379-5 · Cited by 2,785
Self-citationYamazaki, H., Johnson, W. W., Ueng, Y.-F., Shimada, T., & Guengerich, F. P. (1996) · Journal of Biological Chemistry · doi:10.1074/jbc.271.44.27438 · Cited by 194
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Dresser, G. K., Spence, J. D., & Bailey, D. G. (2000) · Clinical Pharmacokinetics · doi:10.2165/00003088-200038010-00003 · Cited by 908
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van Rijssen, T. J., van Dijk, E. H. C., Yzer, S., Ohno-Matsui, K., Keunen, J. E. E., Schlingemann, R. O., Sivaprasad, S., Querques, G., Downes, S. M., Fauser, S., et al. (2019) · Progress in Retinal and Eye Research · doi:10.1016/j.preteyeres.2019.07.003 · Cited by 478
Metadata
- Authors
- Guengerich, F. P.
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 1999-04
- Volume
- 39
- Issue
- 1
- Pages
- 1-17
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2127059331
- Cited by
- 1,267
- References
- 2
- FWCI
- 4.14
- Type
- journal article
- Language
- en
- Open access
- closed
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- Guengerich, F. P. (1999). CYTOCHROME P-450 3A4: Regulation and Role in Drug Metabolism. Annual Review of Pharmacology and Toxicology. https://doi.org/10.1146/annurev.pharmtox.39.1.1
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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