Drug breakdown by oxidation {drug metabolism} is mainly in liver.
Compounds can have an added group {adduct}.
Drug can inhibit or induce another drug {drug-drug interaction}.
Proteins {flavoprotein} can bind FAD or FMN.
Molecules {glutathione} (GSH) can participate in phase II conjugations.
Phase I oxidations, Phase II conjugations, and transport into bile reduce drug in hepatic blood {hepatic first-pass elimination} (HFPE).
Iron compounds {iron-oxene} {iron-oxenoid} can contain free oxygen atoms.
Drug metabolism makes products {metabolite}.
Nitrosoalkanes irreversibly bind to reduced heme intermediates of CYP450 enzymes {metabolite intermediate complexation}.
Compounds or forces can mutate genes {mutagenicity}.
Metabolism percentage {regioselectivity} categorizes sites as major, minor, or unobservable. Rate constant differences among sites cause metabolic-site regioselectivity.
Drugs can affect targets {selectivity, drug} and other sites.
Substrates {agonist} can bind to receptors and cause biologic response.
Substrates {antagonist, chemistry} can bind to receptor but cause no biologic response.
Hydrogen atoms can bind to carbon atoms {acetylation}.
Amino acids can bind to carboxylic-acid groups {amino acid conjugation}, on anti-inflammatory, hypolipidaemic, diuretic, and analgesic drugs.
Enzymes can change drugs to make them toxic {bioactivation}.
Drug metabolism has oxidations and reductions {biotransformation}.
Two charges can exchange {charge-transfer coupling} in reactions.
Molecules can attach small molecule {conjugation, molecule}.
Processes can make rings {cyclization}.
Glucuronic acid allows glucuronide formation {glucuronic acid conjugation}.
Molecules can conjugate with glutathione {glutathione conjugation} to form mercapturic acid.
Atoms {hydrogen bond acceptor} (HBA) can add hydrogen atom.
Atoms {hydrogen bond donor} (HBD) can release hydrogen atom.
Hydrogen atoms can abstract {hydrogen transfer}.
Hydrogen atoms can bind to oxygen atom {hydroxylation}.
Enzymes can change conformation to allow substrate binding {induced fit}.
Drugs can form complexes with receptors and then cause chemical or conformational changes {intrinsic activity, drug}.
Drug metabolism has oxidation or reduction {Phase I enzyme reaction}.
Drug metabolism has conjugation with small molecules {Phase II enzyme reaction}.
Hydrogen atoms removed from molecules {proton abstraction} can make water.
After ATP activates sulfate, sulfotransferase makes sulfate esters {sulfate conjugation}.
nucleophosphate energy compound {guanidine diphosphate} (GDP).
Energy molecules {uridine diphosphate} (UDP) can participate in phase II reactions.
Enzymes {adenylate cyclase} {adenylcyclase} can alter cAMP.
Enzymes {carboxylesterase} can catalyze phase I reactions.
Enzymes {cytochrome P-450} catalyze phase I reactions 3A4, 2D6, 2C9, 1A2, and 2E1.
Enzymes {epoxide hydratase} {epoxide hydrolase} can oxidize olefins and aromatics to make epoxide or oxirane metabolites. It can produce carcinogens.
Enzymes {glucuronyl-transferase} can catalyze phase II reactions, adding glucuronide to drugs.
Enzymes {glutathione-S-transferase}, in liver-cell cytoplasm, can catalyze phase II reactions to conjugate compounds to glutathione.
Enzymes {microsomal flavoprotein mono-oxygenase} can oxidize nitrogen or sulfur organics.
Enzymes {microsomal hydroxylase} can catabolize many compounds, mostly by oxidation, in endoplasmic reticulum.
Enzymes {mixed-function oxidase} (MFO) can catabolize many compounds, mostly by oxidation, in endoplasmic reticulum.
Enzymes {phospholipase A2} can catabolize lipids.
Enzymes {phospholipase C} can catabolize lipids.
Enzymes {protein kinase} can catabolize proteins.
Enzymes {uridine diphosphoglucose transferase} {uridine-diphosphate-glucuronosyl-transferase} (UDP-GT) (UGT) can catalyze phase II reactions, adding glucuronide to drugs.
Chemicals can inhibit drugs {drug inhibition}. Inhibitor has binding constant.
Inhibitor can bind to non-active site {allosteric non-competitive inhibition}.
Drugs {entry inhibitor} can prevent viruses from entering cells.
Drugs {integrase inhibitor} can prevent virus DNA from inserting into host DNA.
Drugs {maturation inhibitor} can block gag-protein protease receptor, so gag protein is not split, and HIV virus coat is not made. PA-457 comes from betulinic acid from Taiwan herb, plane trees, and birch trees.
Metabolized compounds can bind to enzymes {mechanism-based inhibition}.
Drugs {protease inhibitor} can inhibit protease enzymes.
Most-reactive electron {highest occupied molecular orbital} (HOMO) can be in electron-rich nucleophilic molecules.
Most-reactive electron {lowest unoccupied molecular orbital} (LUMO) can be in electron-poor electrophilic molecules.
Total metabolism has rate {absolute metabolism rate}.
Reaction rate typically depends on concentration and temperature {enzyme kinetics}.
Metabolism rate at site has estimated ease {lability}.
Enzymes have binding constants {Michaelis-Menten constant} (Km).
Sites {labile site} can have high metabolism rate and low activation energy.
Sites {moderate site} can have intermediate metabolism rate and activation energy.
Sites {stable site} can have low metabolism rate and high activation energy.
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Description of Outline of Knowledge Database
Date Modified: 2022.0225