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Cytochrome P450 1 family: the roles of 1A1, 1A2 and 1B1 in drug metabolism
A selection of talks on Pharmaceutical Sciences
RNA therapeutics: clinical applications and methods of delivery
- Prof. John P. Cooke
- Houston Methodist Research Institute, USA
Overview of nonclinical safety assessment
- Dr. Claudette L. Fuller
- Merck Research Laboratories, USA
Drug-induced liver injury: risk factors and drug development in DILI
- Prof. James H. Lewis
- Georgetown University Medical Center, USA
Drugging conformational states of GPCRs
- Prof. Dr. Peter Kolb
- Philipps-Universität Marburg, Germany
FRED GUENGERICH: Hello, my name is Dr. Fred Guengerich. I'm at Vanderbilt University in Nashville, Tennessee in the United States. And today I'd like to talk to you about cytochrome P450, specifically the cytochrome P450 1 family and the roles of cytochromes P450 1A1, 1A2, and 1B1 in the metabolism of drugs and other things.
So what I'd like to do today is talk about first of all some background on cytochrome P450. Most of my slides will use the abbreviation, P450. Some may use the CYP, which is an acronym for cytochrome P450. And I also talk about the relevance to human health. I am going to give you some background on the P450 family 1 and some important concepts from the literature; particularly in terms of localization and the three-dimensional structures of these enzymes and their relevance to a function. I'm going to talk about more research on these particular P450s, the roles of family 1 P450s in the metabolism of carcinogens. I'll talk about induction and inhibition, the significance of genetic variations, and also a little bit about heterocyclic amines and the possible risk from cancer.
So let's talk generally about cytochrome P450s and drugs and diseases. In the human genome, we know that there are exactly 57 cytochrome P450 genes and proteins. Most of these are involved in the metabolism of steroids and other endogenous compounds, but 15 of these at least are involved in the metabolism of drugs and other xenobiotic chemicals. Xenobiotic is a term that we use to describe compounds, chemicals that is, that are not normally in the body. For instance, drugs, pesticides, things like this would be in this regard.