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Cytochrome P-450 Enzyme System

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Genetic Variation in Cytochrome P450 2R1 and Vitamin D Binding Protein Genes are associated with Vitamin D Deficiency in Adolescents.

International journal for vitamin and nutrition research. Internationale Zeitschrift fur Vitamin- und Ernahrungsforschung. Journal international de vitaminologie et de nutrition
Genome Wide Association Studies (GWAS) have evaluated several genes related to vitamin D synthesis, metabolism and transport. They have proposed a genetic basis for low levels of vitamin D in the blood. The current study aims to investigate the rela...

Computational prediction of cytochrome P450 inhibition and induction.

Drug metabolism and pharmacokinetics
Cytochrome P450 (CYP) enzymes play an important role in the phase I metabolism of many xenobiotics. Most drug-drug interactions (DDIs) associated with CYP are caused by either CYP inhibition or induction. The early detection of potential DDIs is high...

Predicting drug metabolism and pharmacokinetics features of in-house compounds by a hybrid machine-learning model.

Drug metabolism and pharmacokinetics
We constructed machine learning-based pharmacokinetic prediction models with very high performance. The models were trained on 26138 and 16613 compounds involved in metabolic stability and cytochrome P450 inhibition, respectively. Because the compoun...

Mining Toxicity Information from Large Amounts of Toxicity Data.

Journal of medicinal chemistry
Safety is a main reason for drug failures, and therefore, the detection of compound toxicity and potential adverse effects in the early stage of drug development is highly desirable. However, accurate prediction of many toxicity endpoints is extremel...

CYPlebrity: Machine learning models for the prediction of inhibitors of cytochrome P450 enzymes.

Bioorganic & medicinal chemistry
The vast majority of approved drugs are metabolized by the five major cytochrome P450 (CYP) isozymes, 1A2, 2C9, 2C19, 2D6 and 3A4. Inhibition of CYP isozymes can cause drug-drug interactions with severe pharmacological and toxicological consequences....

CYPstrate: A Set of Machine Learning Models for the Accurate Classification of Cytochrome P450 Enzyme Substrates and Non-Substrates.

Molecules (Basel, Switzerland)
The interaction of small organic molecules such as drugs, agrochemicals, and cosmetics with cytochrome P450 enzymes (CYPs) can lead to substantial changes in the bioavailability of active substances and hence consequences with respect to pharmacologi...

Machine Learning-Based Prediction of Drug-Drug Interactions for Histamine Antagonist Using Hybrid Chemical Features.

Cells
The requesting of detailed information on new drugs including drug-drug interactions or targets is often unavailable and resource-intensive in assessing adverse drug events. To shorten the common evaluation process of drug-drug interactions, we prese...

Drug Metabolism: A Half-Century Plus of Progress, Continued Needs, and New Opportunities.

Drug metabolism and disposition: the biological fate of chemicals
The systematic study of drug metabolism began in the 19th Century, but most of what we know now has been learned in the last 50 years. Drug metabolism continues to play a critical role in pharmaceutical development and clinical practice, as well as c...

Using graph neural networks for site-of-metabolism prediction and its applications to ranking promiscuous enzymatic products.

Bioinformatics (Oxford, England)
MOTIVATION: While traditionally utilized for identifying site-specific metabolic activity within a compound to alter its interaction with a metabolizing enzyme, predicting the site-of-metabolism (SOM) is essential in analyzing the promiscuity of enzy...

Prediction of Cytochrome P450 Inhibition Using a Deep Learning Approach and Substructure Pattern Recognition.

Journal of chemical information and modeling
Cytochrome P450 (CYP) is a family of enzymes that are responsible for about 75% of all metabolic reactions. Among them, CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 participate in the metabolism of most drugs and mediate many adverse drug reactions. T...