Drug-protein adducts: an industry perspective on minimizing the potential for drug bioactivation in drug discovery and development.
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Nonenzymatic protein acylation as a carbon stress regulated by sirtuin deacylasesReversible targeting of noncatalytic cysteines with chemically tuned electrophilesElectrochemistry-mass spectrometry unveils the formation of reactive triclocarban metabolitesTherapeutic decisions in multiple sclerosis: moving beyond efficacySite-specific arylation of rat glutathione s-transferase A1 and A2 by bromobenzene metabolites in vivoLarge-scale prediction of drug-target relationshipsHigh-throughput metabolic stability studies in drug discovery by orthogonal acceleration time-of-flight (OATOF) with analogue-to-digital signal capture (ADC).Post-acquisition analysis of untargeted accurate mass quadrupole time-of-flight MS(E) data for multiple collision-induced neutral losses and fragment ions of glutathione conjugates.Identification of 17-alpha-ethynylestradiol-modified active site peptides and glutathione conjugates formed during metabolism and inactivation of P450s 2B1 and 2B6.Analysis of protein adduction kinetics by quantitative mass spectrometry: competing adduction reactions of glutathione-S-transferase P1-1 with electrophiles.Protein damage by reactive electrophiles: targets and consequencesBioinformatic analysis of xenobiotic reactive metabolite target proteins and their interacting partners.Metoclopramide is metabolized by CYP2D6 and is a reversible inhibitor, but not inactivator, of CYP2D6Fragmentation of toxicologically relevant drugs in positive-ion liquid chromatography-tandem mass spectrometry.Development of second generation EP2 antagonists with high selectivityStrategies for discovering and derisking covalent, irreversible enzyme inhibitors.High-resolution chromatography/time-of-flight MSE with in silico data mining is an information-rich approach to reactive metabolite screening.Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.Simultaneous screening of glutathione and cyanide adducts using precursor ion and neutral loss scans-dependent product ion spectral acquisition and data mining tools.Application of LC-high-resolution MS with 'intelligent' data mining tools for screening reactive drug metabolites.Improved cytochrome P450 3A4 molecular models accurately predict the Phe215 requirement for raloxifene dehydrogenation selectivity.Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.Profiling the reactive metabolites of xenobiotics using metabolomic technologiesCYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir.Cyclostreptin derivatives specifically target cellular tubulin and further map the paclitaxel site.Detection of reactive metabolites using isotope-labeled glutathione trapping and simultaneous neutral loss and precursor ion scanning with ultra-high-pressure liquid chromatography triple quadruple mass spectrometryIdentification of protein targets of reactive metabolites of tienilic acid in human hepatocytes.Metabolic toxicity screening using electrochemiluminescence arrays coupled with enzyme-DNA biocolloid reactors and liquid chromatography-mass spectrometry.Elucidating mechanisms of drug-induced toxicity.Life and times in biochemical toxicology.Role of metabolism in drug-induced idiosyncratic hepatotoxicity.NMR in pharmacokinetic and pharmacodynamic profiling.Cytochrome P450s and other enzymes in drug metabolism and toxicity.Role of animal models in the study of drug-induced hypersensitivity reactionsThe consequences of lysosomotropism on the design of selective cathepsin K inhibitors.Minimising the potential for metabolic activation in drug discovery.Chemical toxicology: reactive intermediates and their role in pharmacology and toxicology.Addressing metabolic activation as an integral component of drug design.Evaluation of which reactive metabolite, if any, is responsible for a specific idiosyncratic reaction.
P2860
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P2860
Drug-protein adducts: an industry perspective on minimizing the potential for drug bioactivation in drug discovery and development.
description
2004 nî lūn-bûn
@nan
2004年の論文
@ja
2004年論文
@yue
2004年論文
@zh-hant
2004年論文
@zh-hk
2004年論文
@zh-mo
2004年論文
@zh-tw
2004年论文
@wuu
2004年论文
@zh
2004年论文
@zh-cn
name
Drug-protein adducts: an indus ...... rug discovery and development.
@ast
Drug-protein adducts: an indus ...... rug discovery and development.
@en
type
label
Drug-protein adducts: an indus ...... rug discovery and development.
@ast
Drug-protein adducts: an indus ...... rug discovery and development.
@en
prefLabel
Drug-protein adducts: an indus ...... rug discovery and development.
@ast
Drug-protein adducts: an indus ...... rug discovery and development.
@en
P2093
P356
P1476
Drug-protein adducts: an indus ...... rug discovery and development.
@en
P2093
Alan P Watt
David C Evans
Deborah A Nicoll-Griffith
Thomas A Baillie
P356
10.1021/TX034170B
P577
2004-01-01T00:00:00Z