Concentration-dependent inhibition of mesophilic PETases on poly(ethylene terephthalate) can be eliminated by enzyme engineering.
Sign Up to like & getrecommendations! Published in 2023 at "ChemSusChem"
DOI: 10.1002/cssc.202202277
Abstract: Enzyme-based depolymerization is a viable approach for recycling of poly(ethylene terephthalate) (PET). PETase from Ideonella sakaiensis (IsPETase) is capable of PET hydrolysis under mild conditions but suffers from concentration-dependent inhibition. Here, we report that this inhibition is… read more here.
Keywords: dependent inhibition; inhibition; poly ethylene; ethylene terephthalate ... See more keywords
Kinetic mechanism of time‐dependent inhibition of CYP2D6 by 3,4‐methylenedioxymethamphetamine (MDMA): Functional heterogeneity of the enzyme and the reversibility of its inactivation
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical Pharmacology"
DOI: 10.1016/j.bcp.2018.08.010
Abstract: Graphical abstract Figure. No Caption available. Abstract We investigate the mechanism of time‐dependent inhibition (TDI) of human cytochrome P450 2D6 (CYP2D6) by 3,4‐methylenedioxymethamphetamine (MDMA, ecstasy), one of the most widespread recreational drugs of abuse. In… read more here.
Keywords: dependent inhibition; cyp2d6; time dependent; mechanism ... See more keywords
Substrate and method dependent inhibition of three ABC‐transporters (MDR1, BCRP, and MRP2)
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmaceutical Sciences"
DOI: 10.1016/j.ejps.2017.03.002
Abstract: ABSTRACT Drug transport and drug‐drug interactions (DDI) with human ABC transporters are generally investigated in mammalian cell lines or inverted membrane vesicles from insect cells (Sf9) overexpressing the transporter of interest. In this study, we… read more here.
Keywords: abc transporters; mrp2; inhibition; probe substrates ... See more keywords
Numerical analysis of time-dependent inhibition kinetics: comparison between rat liver microsomes and rat hepatocyte data for mechanistic model fitting
Sign Up to like & getrecommendations! Published in 2017 at "Xenobiotica"
DOI: 10.1080/00498254.2017.1345020
Abstract: Abstract Time-dependent inhibition (TDI) may confound drug interaction predictions. Recently, models were generated for an array of TDI kinetic schemes using numerical analysis of microsomal assays. Additionally, a distinct terminal inactivation step was identified for… read more here.
Keywords: numerical analysis; analysis; model; time dependent ... See more keywords
Group B Wolbachia Strain-Dependent Inhibition of Arboviruses.
Sign Up to like & getrecommendations! Published in 2018 at "DNA and cell biology"
DOI: 10.1089/dna.2017.4025
Abstract: Mosquito-borne viruses, including Zika virus (ZIKV) and dengue virus (DENV), are global threats that continue to infect millions annually. Historically, efforts to combat the spread of these diseases have sought to eradicate the mosquito population.… read more here.
Keywords: group wolbachia; mosquito; strain dependent; wolbachia strain ... See more keywords
A Tale of Two Isoforms: Calcium-Dependent Inhibition of SnRK2 by SnRK-Calcium-Binding Sensor
Sign Up to like & getrecommendations! Published in 2020 at "Plant Physiology"
DOI: 10.1104/pp.19.01554
Abstract: Reacting to the environment requires not only activating signaling cascades but also modulating the activity of individual components in a context- and time-dependent manner. For example, under nonstress conditions, protein phosphatases 2C (PP2C) keep the… read more here.
Keywords: calcium dependent; tale two; two isoforms; isoforms calcium ... See more keywords
NADPH-Independent Inactivation of CYP2B6 and NADPH-Dependent Inactivation of CYP3A4/5 by PBD: Potential Implication for Assessing Covalent Modulators for Time-Dependent Inhibition
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.120.090878
Abstract: Pyrrolo[2,1-c][1,4]benzodiazepine dimer (PBD) has shown broad antitumor properties and potential as a therapeutic agent for cancers. During a routine drug-drug interaction assessment, it was found that PBD is a reversible inhibitor of CYP2C8 (IC50 =… read more here.
Keywords: cyp2b6; inhibition; nadph independent; inactivation ... See more keywords
Cytochrome P450 3A Time-Dependent Inhibition Assays Are Too Sensitive for Identification of Drugs Causing Clinically Significant Drug-Drug Interactions: A Comparison of Human Liver Microsomes and Hepatocytes and Definition of Boundaries for Inactivation Rate Constants
Sign Up to like & getrecommendations! Published in 2020 at "Drug Metabolism and Disposition"
DOI: 10.1124/dmd.121.000356
Abstract: Time-dependent inhibition (TDI) of CYP3A is an important mechanism underlying numerous drug-drug interactions (DDIs), and assays to measure this are done to support early drug research efforts. However, measuring TDI of CYP3A in human liver… read more here.
Keywords: drug; time dependent; dependent inhibition; drug interactions ... See more keywords
Voltage-Dependent Inhibition of Glycine Receptor Channels by Niflumic Acid
Sign Up to like & getrecommendations! Published in 2017 at "Frontiers in Molecular Neuroscience"
DOI: 10.3389/fnmol.2017.00125
Abstract: Niflumic acid (NFA) is a member of the fenamate class of nonsteroidal anti-inflammatory drugs. This compound and its derivatives are used worldwide clinically for the relief of chronic and acute pain. NFA is also a… read more here.
Keywords: inhibition glycine; voltage dependent; niflumic acid; dependent inhibition ... See more keywords
Tricyclic Antidepressant Structure-Related Alterations in Calcium-Dependent Inhibition and Open-Channel Block of NMDA Receptors
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2021.815368
Abstract: N-methyl-D-aspartate receptors (NMDARs) are an essential target for the analgetic action of tricyclic antidepressants (TCAs). Their therapeutic blood concentrations achieve 0.5–1.5 μM, which, however, are insufficient to cause in vitro the open-channel block known as… read more here.
Keywords: dependent inhibition; open channel; channel block;
Coptisine attenuates post‑infectious IBS via Nrf2‑dependent inhibition of the NLPR3 inflammasome.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular medicine reports"
DOI: 10.3892/mmr.2022.12879
Abstract: Inhibition of the activation of the NLR family pyrin domain‑containing 3 (NLRP3) inflammasome has previously been reported to confer protection against post‑infectious irritable bowel syndrome (PI‑IBS). Coptisine, the second most abundant isoquinoline alkaloid in Coptis chinensis,… read more here.
Keywords: dependent inhibition; via nrf2; inhibition; post infectious ... See more keywords