ⓘ CYP3A4

                                     

ⓘ CYP3A4

Cytochrome P450 3A4 is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules, such as toxins or drugs, so that they can be removed from the body.

Although many drugs are detoxified by CYP3A4, there are also some medications that are activated by the enzyme. Some substances, such as grapefruit juice and some drugs, interfere in the action of CYP3A4. Therefore, these substances will either strengthen or weaken the action of those drugs that are modified by CYP3A4.

CYP3A4 is a member of a family of cytochrome P450 oxidative enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and most versatile. Like all members of this family, is a hemoprotein, i.e. a protein containing a heme with an iron atom. In humans, the CYP3A4 protein is encoded by the gene CYP3A4. This gene is part of a cluster of cytochrome P-450 genes on chromosome 7q22.1.

                                     
  • The CYP 3 A cluster consists of four genes: CYP3A4 CYP 3 A5, CYP 3 A7, and CYP 3 A43. The region also contains four pseudogenes: CYP 3 A51P, CYP 3 A52P, CYP 3 A54P
  • that CYP 3 A5 is expressed as a 52.5 - kD protein, whereas CYP3A4 migrates as a 52.0 - kD protein. The human CYP 3 A subfamily, CYP3A4 CYP 3 A5, CYP 3 A7 and CYP 3 A43
  • the CYP enzyme inhibition A classical example includes anti - epileptic drugs, such as Phenytoin, which induces CYP 1A2, CYP 2C9, CYP 2C19, and CYP3A4 Effects
  • Leukotriene - B 4 omega - hydroxylase 2 is an enzyme that in humans is encoded by the CYP 4 F 3 gene. CYP 4 F 3 encodes two distinct enzymes, CYP 4 F 3 A and CYP 4 F 3 B, which
  • October 2001 Effects of CYP3A4 inhibition by diltiazem on pharmacokinetics and dynamics of diazepam in relation to CYP 2C19 genotype status Drug Metabolism
  • CYP 3 A7 is an enzyme belonging to the cytochrome P450 family. It is 503 amino acids in size and shares 87 of its sequence with CYP3A4 It carries out
  • known P450 - mediated drug oxidations it and related enzymes CYP1A2 and CYP3A4 are responsible for the breakdown of many toxic environmental chemicals
  • Flockhart DA, Relling MV, Santucci R, Ratain MJ Sep 2004 CYP 2B6, CYP3A4 and CYP 2C19 are responsible for the in vitro N - demethylation of meperidine
  • Metabolism Transport Effects: Substrate of CYP 1A2 minor CYP 2B6 minor CYP 2C9 minor CYP 2E1 minor CYP3A4 major P - glycoprotein ABCB1 Note: Assignment