Microsomes are widely used to study Phase I metabolic reactions, which primarily involve oxidation, reduction, and hydrolysis. This is because liver microsomes are rich in cytochrome P450 enzymes (CYPs) and flavin-containing monooxygenases (FMOs), the main enzymes responsible for Phase I drug metabolism. These enzymes introduce or expose functional groups on drug molecules, often as the first step in their breakdown. Phase II Metabolism: Microsomes can also be used to study certain Phase II metabolic reactions, particularly glucuronidation. This is due to the presence of UDP-glucuronosyltransferases (UGTs) in the microsomal fraction. However, other Phase II enzymes, such as sulfotransferases (SULTs) and glutathione S-transferases (GSTs), are mainly found in the cytosolic fraction, not in microsomes.
Microsomes are a powerful and versatile tool in drug development, enabling rapid and cost-effective evaluation of metabolic stability, metabolite identification, and drug-drug interaction potential—key factors for the safe and effective development of new medicines.
Liver, kidney, lung and intestine subcellular fractions are available from different species, including nonhuman primates Rhesus Monkey, Beagle Dog, Sprague-Dawley Rat, several Mouse strains (e.g. CD-1, Balb/C), Rabbit, Guinea Pig, BAM Minipig, Chicken.
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