Nontargeted Identification of Reactive Metabolite Protein Adducts.
Sign Up to like & getrecommendations! Published in 2017 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.6b04604
Abstract: Metabolic bioactivation of many different chemicals results in the formation of highly reactive compounds (chemically reactive metabolites, CRMs) that can lead to toxicity via binding to macromolecular targets (e.g., proteins or DNA). There is a… read more here.
Keywords: protein; reactive metabolite; nontargeted identification; identification reactive ... See more keywords
Designing Around Structural Alerts in Drug Discovery.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00917
Abstract: Cumulative research over several decades has implicated the involvement of reactive metabolites in many idiosyncratic adverse drug reactions (IADRs). Consequently, "avoidance" strategies have been inserted into drug discovery paradigms, which include the exclusion of structural… read more here.
Keywords: structural alerts; reactive metabolite; drug; designing around ... See more keywords
Reactive metabolite production is a targetable liability of glycolytic metabolism in lung cancer
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DOI: 10.1038/s41467-019-13419-4
Abstract: Increased glucose uptake and metabolism is a prominent phenotype of most cancers, but efforts to clinically target this metabolic alteration have been challenging. Here, we present evidence that lactoylglutathione (LGSH), a byproduct of methylglyoxal detoxification,… read more here.
Keywords: metabolism; metabolite production; reactive metabolite; lung cancer ... See more keywords
Peripheral biomarkers of oxidative stress in dogs with acute pancreatitis
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Veterinary Internal Medicine"
DOI: 10.1111/jvim.16535
Abstract: Abstract Background Oxidative stress is considered a pathomechanism of acute pancreatitis (AP), but no studies have extensively characterized oxidant status in dogs with naturally‐occurring AP. Hypothesis or Objectives Evaluate measures of oxidant status in dogs… read more here.
Keywords: reactive metabolite; oxidative stress; range; severity ... See more keywords
Regorafenib and reactive metabolite of sunitinib activate inflammasomes: Implications for multi tyrosine kinase inhibitor-Iiduced immune related adverse events.
Sign Up to like & getrecommendations! Published in 2022 at "Die Pharmazie"
DOI: 10.1691/ph.2022.1955
Abstract: Multi-targeted tyrosine kinase inhibitors have been developed for the treatment of various cancers, but they are associated with a significant incidence of idiosyncratic drug reactions (IDRs). There is compelling evidence that most IDRs are immune… read more here.
Keywords: reactive metabolite; sunitinib; activate inflammasomes; tyrosine kinase ... See more keywords