UGT2B7

Overview

UGT2B7 (UDP-glucuronosyltransferase 2B7) is an important enzyme in the human body that belongs to the UDP-glucuronosyltransferase family. This enzyme is primarily involved in the process of glucuronidation, a major phase II metabolic pathway that facilitates the elimination of lipophilic substances by converting them into more water-soluble compounds. UGT2B7 is encoded by the UGT2B7 gene located on chromosome 4q13.

Function

UGT2B7 plays a crucial role in the metabolism of a wide range of endogenous and exogenous compounds. It is responsible for the glucuronidation of various drugs, hormones, and xenobiotics. Some of the notable substrates of UGT2B7 include:

• Morphine
• Ibuprofen
• Valproic acid
• Zidovudine

The enzyme is also involved in the metabolism of steroid hormones such as testosterone and estradiol, as well as bile acids.

Clinical Significance

The activity of UGT2B7 can significantly affect the pharmacokinetics and pharmacodynamics of drugs. Variations in the UGT2B7 gene, such as single nucleotide polymorphisms (SNPs), can lead to differences in enzyme activity among individuals, influencing drug efficacy and toxicity. For example, altered UGT2B7 activity can affect the clearance of morphine, impacting its analgesic effects and side effects.

UGT2B7 is also implicated in drug-drug interactions. Inhibitors or inducers of UGT2B7 can alter the metabolism of its substrates, leading to potential therapeutic failures or adverse drug reactions.

Expression

UGT2B7 is predominantly expressed in the liver, but it is also found in other tissues such as the kidney, intestine, and brain. The expression levels of UGT2B7 can be influenced by various factors, including genetic factors, diet, and environmental exposures.

Research and Developments

Ongoing research is focused on understanding the genetic variations of UGT2B7 and their implications in personalized medicine. Studies are also exploring the role of UGT2B7 in the metabolism of new therapeutic agents and its potential as a target for drug development.

Also see

• UDP-glucuronosyltransferase
• Glucuronidation
• Phase II metabolism
• Pharmacogenomics
• Drug metabolism

References

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