What is CES1A1?
Summary: CES1A1 is the primary enzyme responsible for the metabolism of methylphenidate (MPH). 1 The Gly143Glu polymorphism reduces enzyme activity, which could result in elevated plasma concentrations of some parent compounds that are substrates of CES1A1.
What does carboxylesterase do?
Carboxylesterases are a multi-gene family of enzymes widely distributed throughout the body of mammals that catalyze the hydrolysis of esters, amides, thioesters, and carbamates. In humans, two carboxylesterases, hCE1 and hCE2, are important pathways of drug metabolism.
Do humans have Carboxylesterase?
In contrast to rodents, humans have no carboxylesterase in blood (Li et al. 2005). CBDP has frequently been used as a specific inhibitor of carboxylesterase. However, we have found that CBDP inhibits both butyrylcholinesterase and carboxylesterase.
What is the optimal pH for the Carboxylesterase?
It is produced as an intracellular protein with a molecular weight of 32 kDa, with optimum pH of 8.5-10.5 and optimum temperature between 35 to 55°C.
What drugs are metabolized by UGT1A4?
The UGT1A4 enzyme mediates the metabolism of important psychotropic medications, including some tricyclic antidepressants, antipsychotics, and mood stabilizers1–20. Therefore, genetic polymorphisms in this gene may have pharmacological importance.
Does caffeine inhibit CYP1A2?
The results of this study revealed a pronounced effect of caffeine on the bioavailability of orally given melatonin, most probably due to inhibition of CYP1A2 activity.
What is a hydrolysis equation?
Thus, if a compound is represented by the formula AB in which A and B are atoms or groups and water is represented by the formula HOH, the hydrolysis reaction may be represented by the reversible chemical equation AB + HOH ⇌ AH + BOH.
Where is esterase found in the body?
In human physiology, esterases are distributed in the liver, erythrocytes, plasma, and the gastrointestinal tract.
What does CES1A1 stand for?
Liver carboxylesterase 1 also known as carboxylesterase 1 (CES1, hCE-1 or CES1A1) is an enzyme that in humans is encoded by the CES1 gene.
What drugs are activated by CES1?
CES1 can activate or deactivate various drugs. CES1 is responsible for the activation of many prodrugs such as angiotensin-converting enzyme (ACE) inhibitors, oseltamivir, and dabigatran.
What is the difference between CES1 and carboxylesterase?
CES1 is present in most tissues with higher levels in the liver and low levels in the gastrointestinal tract. Carboxylesterase 1 is a serine esterase and member of a large multigene carboxylesterase family. It is also part of the alpha/beta fold hydrolase family.
Where is CES1 found in the human body?
CES1 is present in most tissues with higher levels in the liver and low levels in the gastrointestinal tract. Carboxylesterase 1 is a serine esterase and member of a large multigene carboxylesterase family.