Global ETD Search
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Showing 1 to 20 of 33 for “"CYPs"”.
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Studies on pro-oxidant cytochrome P450 enzymes as drug discovery tools and the discovery that they also have a dual function as antioxidants
… In this research, specific cytochrome P450s (CYPs) have been overexpressed in baker’s yeast with the following objectives in mind. (i) CYP1A1, CYP1A2, and CYP1B1 are enzymes highly up-regulated in lung cancers that are caused by inhaling or coming into contact with polyaromatic hydrocarbons …
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Genetically engineering a new system for the expression of cytochrome P450 enzymes in insect cells using novel P450 reductases
Human cytochrome P450 enzymes (CYPs) are a superfamily of haem-binding monooxygenase enzymes involved in the metabolism of xenobiotics such as toxins, carcinogens and pharmaceutical drugs as well as in the biosynthesis of cholesterol, vitamins and steroids. In recent years, the area of drug …
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Differential detoxification strategies in closely related herbivore species across a sharp ecotone
… method is the use of cytochrome P450 enzymes (CYPs), many of which are found in the liver. While there has been much study of CYPs in model systems, there has been little research on CYPs in wild systems. The woodrat species Neotoma lepida and N. bryanti live across a sharp ecotone in which …
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Comparative structural analysis of cytochrome P450 family CYP51 in the genus Cryptococcus
… mining, annotation and phylogenetic analysis of CYPs has not been reported. Furthermore, few studies on the structural analysis of CYP51 and its interactions with different azole drugs have been reported. This study is aimed to address these two research gaps. Comprehensive genome-wide CYP …
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Capture and Characterization of Dioxygen Reactive Intermediates in CYP51 Catalysis
The cytochromes P450 (CYPs) are a superfamily of biological catalysts that are ubiquitous throughout the biological domain. CYPs are heme-b containing monooxygenases which oxidize substrates with the help of accessory redox partners. CYP substrates include endogenous compounds required for many …
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Developing novel systems for expression of intracellular membrane-bound human cytochrome P450 enzymes in baker’s yeast
… soluble for excretion from the human body. Human CYPs are also naturally involved in the biosynthesis of vitamins, steroids, fatty acids, lipids and cholesterol. A CYP enzyme requires a CYP reductase (CPR) for it to be active. Both CYPs and CPR are bound to the intracellular endoplasmic reticular …
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Investigation of cytochrome P450s in the biosynthesis of rice phytoalexins
… diterpenoid biosynthesis are cytochromes P450 (CYPs) which catalyze various tailoring reactions on LRD olefins to produce bioactive diterpenoids. Intriguingly, two biosynthetic gene clusters (BGCs), composed of CYPs and upstream cyclases dedicated to LRD production, have been discovered in the …
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Functional characterization and expression of molluscan detoxification enzymes and transporters involved in dietary allelochemical resistance
… identified both allelochemically-responsive CYPs, and constitutively expressed GSTs and transporters in Cyphoma digestive glands. Inhibition of Cyphoma GST activity by gorgonian extracts and selected allelochemicals (i.e., prostaglandins) indicated that gorgonian diets are likely to contain …
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An investigation into the metabolic activation of novel chloromethylindolines by isoforms of cytochrome P450. Targeting drug metabolising enzymes in cancer: analysis of the role and function of selected cytochrome P450 oxidising novel cancer prodrugs
Introduction Cytochromes P450 (CYPs) are the major family of enzymes responsible for detoxification and metabolism of a wide range of both endogenous and xenobiotics chemicals in living organisms. The use of CYPs to activate prodrugs to cytotoxins selectively in tumours has been explored including …
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Effect of Comorbidities on HIV-1 Pathogenesis in Monocytic Cells
… PAHs on the expression of cytochromes P450 (CYPs), oxidative stress, and cytotoxicity. The treated cells were examined for mRNA and protein levels of CYPs (1A1 and 3A4) and antioxidants enzymes (AOEs) superoxide dismutase-1 (SOD1) and catalase. Further, we assessed the levels of reactive …
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Functional characterization and expression of molluscan detoxification enzymes and transporters involved in dietary allelochemical resistance
… identified both allelochemically-responsive CYPs, and constitutively expressed GSTs and transporters in Cyphoma digestive glands. Inhibition of Cyphoma GST activity by gorgonian extracts and selected allelochemicals (i.e., prostaglandins) indicated that gorgonian diets are likely to contain …
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Functional effects of cytochrome P450 variants on drug metabolism and adverse drug reactions: developing and extending high throughput P450 protein technology platforms
Cytochrome P450 (CYPs) are a superfamily of heme containing enzymes that catalyse a diverse range of biological reactions. They are responsible for over 80% of primary metabolism of currently available drugs and are therefore central to its medical importance. Investigating the effects of these …
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The Effects of Ethanol and Nicotine on Hepatic and Brain CYP2 Family Enzymes in African Green Monkeys
Cytochromes P450 (CYPs) metabolize a vast array of xenobiotics, including many drugs and toxins. Induction or downregulation of the CYPs can have important consequences such as changes in drug efficacy and altered susceptibility to toxicity. Our study investigated the independent and combined …
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Studying the Specificity of hPXR Antagonists Using a Panel of Cell-based Assays
… metabolism and transportation. Induction of CYPs contributes to adverse drug-drug interactions. Non-toxic, PXR-specific antagonists will be valuable in attenuating the adverse drug-drug interaction which is the cause of many treatment failures in clinic. However, few hPXR antagonists were …
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In vitro metabolism studies to inform physiologically-based pharmacokinetic modelling of mefloquine, ritonavir and proguanil
… by CYP2D6 and CYP3A. These determined fm,CYPs were then used, along with available data from literature, to develop PBPK models for mefloquine, proguanil and cycloguanil as a metabolite of proguanil using a middle-out approach with the use of Simcyp modelling software. These models were …
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A NOVEL ROLE FOR CYTOCHROME P450 G 35 (CYP4G35) IN ODOR PROCESSING IN AEDES AEGYPTI MOSQUITOES
… enzymes, such as esterases and cytochrome P450s (CYPs), have been hypothesized to function as odor-degrading enzymes; however, none is yet functionally characterized. Most insects have 1 or 2 CYP4G genes, an insect-specific class of CYPs. The Dipteran insect genomes have two genes. Similar to …
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Enzymology of lipid metabolism by CYP2J2 as controlled by multiple-ligand binding events
… the CYP pathway and how it is regulated. The CYPs responsible for producing EETs metabolize other PUFAs, lipids, and drugs. Complex substrate-substrate interactions have been observed with drug-metabolizing CYPs and is thought to mediate some of the known drug-drug interactions. Therefore, the …
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Prediction of CYP3A4 metabolic activity from whole genome RNA-seq data with feature selection machine learning methods
… one of the isozyme of the cytochromes P450 (CYPs), contributes significantly to drug clearance and drug-drug interactions. The goals of this project are to identify hepatically-expressed genes that are associated with CYP3A4 metabolic activity in human liver tissue and to predict CYP3A4 …
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Osmotic balance and establishment of polarity in C. elegans embryo require cytochrome P450 CYP31A
… on a class of proteins: the cytochrome P450s (CYPs), which are involved in lipid production in many organisms. We have used C. elegans, a classical genetic model system, to investigate lipid metabolism because this nematode offers several technical advantages that render it suitable for our …
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BIOACTIVATION OF NATURAL DIETARY PRODRUGS BY SPECIFIC CYTOCHROME P450 ENZYMES
Tumour specific cytochrome P450 enzymes (CYPs) have recently been established as a novel target in anticancer drug discovery. The enzymes are used to activate nontoxic prodrugs with latent activity. Thus, the combination of tumour specific CYPs as ‘rescue enzymes’ with a suitable substrate provides …
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