Search Results - "Mercer, Susan L."
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Opioid analgesics and P-glycoprotein efflux transporters: a potential systems-level contribution to analgesic tolerance
Published in Current topics in medicinal chemistry (01-05-2011)“…Chronic clinical pain remains poorly treated. Despite attempts to develop novel analgesic agents, opioids remain the standard analgesics of choice in the…”
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2
DARK Classics in Chemical Neuroscience: Morphine
Published in ACS chemical neuroscience (17-10-2018)“…As the major psychoactive agent in opium and direct precursor for heroin, morphine is a historically critical molecule in chemical neuroscience. A structurally…”
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3
DARK Classics in Chemical Neuroscience: Fentanyl
Published in ACS chemical neuroscience (17-10-2018)“…Fentanyl rose to prominence as an alternative analgesic to morphine nearly 50 years ago; today, fentanyl has re-emerged as a dangerous recreational substance…”
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4
Etoposide Quinone Is a Covalent Poison of Human Topoisomerase IIβ
Published in Biochemistry (Easton) (20-05-2014)“…Etoposide is a topoisomerase II poison that is utilized to treat a broad spectrum of human cancers. Despite its wide clinical use, 2–3% of patients treated…”
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5
Two-Mechanism Model for the Interaction of Etoposide Quinone with Topoisomerase IIα
Published in Chemical research in toxicology (19-09-2016)“…Topoisomerase II is an essential nuclear enzyme involved in regulating DNA topology to facilitate replication and cell division. Disruption of topoisomerase II…”
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Opioids and efflux transporters. Part 3: P-glycoprotein substrate activity of 3-hydroxyl addition to meperidine analogs
Published in Bioorganic & medicinal chemistry (15-06-2008)“…Numerous studies have shown that many clinically employed opioid analgesics are substrates for P-glycoprotein (P-gp), suggesting that up-regulation of P-gp may…”
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Impact of cytochrome P450 variation on meperidine N-demethylation to the neurotoxic metabolite normeperidine
Published in Xenobiotica (01-02-2020)“…1. Meperidine is an opioid analgesic that undergoes N-demethylation to form the neurotoxic metabolite normeperidine. Previous studies indicate that meperidine…”
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8
HU-331 Is a Catalytic Inhibitor of Topoisomerase IIα
Published in Chemical research in toxicology (15-12-2014)“…Topoisomerases are essential enzymes that are involved in DNA metabolism. Topoisomerase II generates transient DNA strand breaks that are stabilized by…”
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Synthesis and evaluation of etoposide and podophyllotoxin analogs against topoisomerase IIα and HCT-116 cells
Published in Bioorganic & medicinal chemistry (15-11-2020)“…[Display omitted] •Analogs 2’,6’-dichloropodophyllotoxin (8), 2’-chloroetoposide (9) and 2’-chloro-4’-demethylepipodophyllotoxin (10) displayed variable…”
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HU-331 and Oxidized Cannabidiol Act as Inhibitors of Human Topoisomerase IIα and β
Published in Chemical research in toxicology (19-02-2018)“…Topoisomerase II is a critical enzyme in replication, transcription, and the regulation of chromatin topology. Several anticancer agents target topoisomerases…”
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Etoposide Quinone Is a Redox-Dependent Topoisomerase II Poison
Published in Biochemistry (Easton) (28-06-2011)“…Etoposide is a topoisomerase II poison that is used to treat a variety of human cancers. Unfortunately, 2–3% of patients treated with etoposide develop…”
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12
Catalytic Core of Human Topoisomerase IIα: Insights into Enzyme–DNA Interactions and Drug Mechanism
Published in Biochemistry (Easton) (21-10-2014)“…Coordination between the N-terminal gate and the catalytic core of topoisomerase II allows the proper capture, cleavage, and transport of DNA during the…”
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13
ACS Chemical Neuroscience Molecule Spotlight on Contrave
Published in ACS chemical neuroscience (21-09-2011)“…Contrave is an investigational fixed-dose combination drug of naltrexone and bupropion currently in Phase III clinical trials for the treatment of obesity…”
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14
Etoposide Catechol Is an Oxidizable Topoisomerase II Poison
Published in Chemical research in toxicology (19-08-2013)“…Topoisomerase II regulates DNA topology by generating transient double-stranded breaks. The anticancer drug etoposide targets topoisomerase II and is…”
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15
Drugs of Abuse and Addiction: An integrated approach to teaching
Published in Currents in pharmacy teaching and learning (01-05-2017)“…To describe the design, implementation, and student perceptions of a Drugs of Abuse and Addiction elective course utilizing an integrated teaching model…”
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Opioids and efflux transporters. Part 4: influence of N-substitution on P-glycoprotein substrate activity of noroxymorphone analogues
Published in Bioorganic & medicinal chemistry letters (01-08-2014)“…The efflux transporter protein P-glycoprotein (P-gp) is capable of affecting the central distribution of diverse neurotherapeutics, including opioid…”
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Behavioral effects of gamma-hydroxybutyrate, its precursor gamma-butyrolactone, and GABA(B) receptor agonists: time course and differential antagonism by the GABA(B) receptor antagonist 3-aminopropyl(diethoxymethyl)phosphinic acid (CGP35348)
Published in The Journal of pharmacology and experimental therapeutics (01-09-2009)“…Gamma-hydroxybutyrate (GHB) is used therapeutically and recreationally. The mechanism by which GHB produces its therapeutic and recreational effects is not…”
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ACS Chemical Neuroscience Molecule Spotlight on Qnexa
Published in ACS chemical neuroscience (20-04-2011)“…Qnexa (VI-0521) is an investigational fixed-dose combination drug of phentermine and topiramate currently in Phase III clinical trials for the treatment of…”
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Evaluation of the P-glycoprotein (Abcb1) affinity status of a series of morphine analogs: Comparative study with meperidine analogs to identify opioids with minimal P-glycoprotein interactions
Published in International journal of pharmaceutics (22-06-2009)“…One of the major shortcomings of many commonly used opioids is the fact that they are P-gp substrates, which represents a major obstacle towards effective pain…”
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Cataleptic effects of γ-hydroxybutyrate (GHB), its precursor γ-butyrolactone (GBL), and GABAB receptor agonists in mice : differential antagonism by the GABAB receptor antagonist CGP35348
Published in Psychopharmacologia (01-06-2007)“…Gamma-hydroxybutyrate (GHB) is used to treat narcolepsy but is also abused. GHB has many actions in common with the GABA(B) receptor agonist baclofen. To…”
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