PathwaysCompoundsEnzymesVivoUndergo metabolicInactiveInhibitorHyperglycemiaEnzymaticNanoparticlesTumorMoleculesOrallyEnzymeToxicityVitro2020PathwayActivationMutantProcessesConvertCompoundFractionsFattyInteractionsCrucialSuggestsAgentsDrugMolecularFormHighPotentialActivityClinicalResearchersEffectsMethodsTreatmentDrugsRateProjectProfileReleaseSmallAgentMajor
Pathways4
- Additionally, specific genes can be inserted into the virus that then can repair defective metabolic, enzymatic, or synthetic pathways in the host. (medscape.com)
- Laboratories around the world have shown that progesterone and allopregnanolone act through numerous metabolic and physiological pathways that can affect the injury response in many different tissues and organ systems. (weeksmd.com)
- Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. (pharmfair.com)
- This means that the body converts THC-O into THC through the same metabolic pathways used to break down other cannabinoids. (buy-thco.com)
Compounds6
- The prodrug strategy implementation in the last 20 y has led to a steady advancement in the biopharmaceutical, physicochemical and/or pharmacokinetic attributes of the pharmacologically active compounds. (ijpsonline.com)
- Prodrugs have been designed to improve so called drug-like properties of active parent compounds (APC) i.e. to increase solubility or absorption and to reduce first-pass metabolism etc. (helsinki.fi)
- Four commercially available prodrugs (bambuterol, olmesartan medoxomil (OM), candesartan cilexetil (CC) and famciclovir) were used as test compounds. (helsinki.fi)
- Then they screened several cisplatin-containing prodrug compounds, which release the platinum-based molecule when they're broken down, to see if they could inhibit fatty acid oxidation. (acs.org)
- One HHC derivative is HHC-O Acetate, also known as HHC acetate or HHC-O. Throughout the history of medicine, compounds have often had acetate added, making them prodrugs. (kannastar.com)
- Assay idiosyncrasies included the identification of unique compounds, the differential ability to identify known antischistosomal compounds and the concept that compounds of interest might include those that increase metabolic activity above baseline. (biomedcentral.com)
Enzymes5
- Other metabolism of the prodrug and APC (nonproductive metabolism) was studied by comparing incubation with and without cofactors of metabolizing enzymes. (helsinki.fi)
- Nrf2 regulates the transcription of a battery of protective and metabolic enzymes. (diabetesjournals.org)
- Biotin is necessary for the proper functioning of enzymes that transport carboxyl units and fix carbon dioxide, and is required for various metabolic functions, including gluconeogenesis, lipogenesis, fatty acid biosynthesis, propionate metabolism, and catabolism of branched-chain amino acids. (pharmfair.com)
- It is a prodrug that is metabolized by cytochrome P450 (CYP) enzymes CYP2D6 and CYP3A4 to its more potent opioid analgesic metabolites, particularly the O -demethylation product M1. (medscape.com)
- Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms. (msdmanuals.com)
Vivo3
- Prodrugs are derivatives of drug molecules that are pharmacologically inactive but require either chemical or enzymatic transformation to release the active drug in vivo in order to exert a pharmacological effect. (ijpsonline.com)
- Prodrugs are pharmacologically inactive molecules which undergo metabolic bioactivation in vivo to form pharmaceutically active agents. (helsinki.fi)
- On the basis of pharmacokinetic results obtained in rats and mice exposed to chloroform by inhalation, and of enzymatic studies in human tissues in vitro , in vivo metabolic rate constants (VmaxC = 15.7 mg/hour/kg, Km = 0.448 mg/L) were defined for humans (Corley et al. (cdc.gov)
Undergo metabolic1
- They are prodrugs which undergo metabolic conversion to active 3-keto derivatives in the body. (wikipedia.org)
Inactive1
- Some drugs, called prodrugs, are administered in an inactive form, which is metabolized into an active form. (msdmanuals.com)
Inhibitor4
- Much work has linked regimens containing TAF and an integrase inhibitor like DTG to weight gains and metabolic turmoil, especially in black women taking these antiretrovirals as first-line therapy, CHARACTERISE investigators noted. (natap.org)
- David Needham, Professor of Translational Therapeutics in the School of Pharmacy at the University of Nottingham and Professor of Mechanical Engineering and Materials Science at Duke University has been working on developing new, more clinically-effective, formulations of a common metabolic inhibitor (niclosamide) that cuts off the energy of cells and could be modified as a treatment for a number of diseases - including cancer. (nottingham.ac.uk)
- Dabigatran etexilate (DABE) can be an dental prodrug that's rapidly changed into the dynamic thrombin inhibitor, dabigatran (DAB), by serine esterases. (gasyblog.com)
- Multiaction Platinum(IV) Prodrug Containing Thymidylate Synthase Inhibitor and Metabolic Modifier against Triple-Negative Breast Cancer. (bvsalud.org)
Hyperglycemia2
- The aim of this study was to assess whether activation of nrf2 by sulforaphane in human microvascular endothelial cells prevents metabolic dysfunction in hyperglycemia. (diabetesjournals.org)
- An insulin-sensitizing agent, such as metformin, is typically used at the start of hyperglycemia treatment in patients with metabolic syndrome. (medscape.com)
Enzymatic1
- These prodrugs subsequently undergo enzymatic or non-enzymatic cleavage to release the active drug moiety (figure 1) [ 12 , 13 ]. (ijpsonline.com)
Nanoparticles2
- The key now is to use drug and prodrug nanoparticles to target these receptors and cut off the energy supply of the cancer cells. (nottingham.ac.uk)
- Chemotherapy-resistant prostate cancers could someday be treated with nanoparticles that encapsulate a cisplatin prodrug, Platin-L. (acs.org)
Tumor2
- Several PET molecular imaging agents could be used for monitoring tumor responses to prodrug activation in gene therapy. (hindawi.com)
- Now, a team of researchers at Kyoto University has developed a prodrug form of curcumin, TBP1901 , that has shown anti-tumor effects without toxicities. (polyphenols-site.com)
Molecules1
Orally1
- We previously described the synthesis of 1-O-octadecyl-2-O-benzyl-glycero-3-phospho-RVn (V2043), an orally bioavailable lipid prodrug of remdesivir nucleoside (RVn, GS-441524) with broad spectrum antiviral activity against viruses with pandemic potential. (cdc.gov)
Enzyme1
- Because metabolic enzyme systems are only partially developed at birth, newborns have difficulty metabolizing certain drugs. (msdmanuals.com)
Toxicity1
- Prodrugs are used typically to maintaining adequate drug stockpiles, will produce up to 36 million courses reduce toxicity caused by functional attempts should be made to optimize per month by year's end if necessary. (cdc.gov)
Vitro4
- In this master's thesis the goal was to establish non-cell-based in vitro methods to study prodrug bioactivation. (helsinki.fi)
- The prodrugs were incubated in liver and intestinal S9 fractions and blood plasma to study in vitro bioactivation of these prodrugs. (helsinki.fi)
- The in vitro incubation used in this study can be used for screening prodrugs. (helsinki.fi)
- LEADS TO Vitro Metabolic Balance. (gasyblog.com)
20202
- On Saturday 10th Oct 2020 Cystinosis Foundation UK ran their first online Cystinosis Symposium, co-hosted by Metabolic Support UK as part of their 2020 Virtual Annual Conference. (cystinosis.org.uk)
- As part of Metabolic Support UK's 2 day virtual conference we are co-hosting a 2 hour interactive 'Cystinosis Symposium' breakout session on Saturday, 10th October 2020, 2-4pm. (cystinosis.org.uk)
Pathway1
- In its original anti-parasitic application, niclosamide has been used for over 60 years, taken as oral tablets, killing tapeworms on contact in the gut by inhibiting their crucial metabolic pathway and shutting down their energy supply. (nottingham.ac.uk)
Activation4
- Metabolic activation of oseltamivir to carboxylic acid. (cdc.gov)
- Drug-DNA adducts as biomarkers for metabolic activation of the nitro-aromatic nitrogen mustard prodrug PR-104A. (harvard.edu)
- Upon metabolic activation by phosphorylation and incorporation into DNA, guadecitabine inhibits DNA Methyltransferase 1 (DNMT1), thereby causing non-specific hypomethylation. (biomedcentral.com)
- Mechanistically, accumulated intracellular PRPP promotes 5\FU prodrug activation and confers enhanced sensitivity to 5\FU on PRPS1 mutant cells. (mdm2-inhibitors.com)
Mutant1
- Therefore, In order to reduce the GCV dose required, we aim to compare the therapeutic efficacy of HSV1-sr39TK, an HSV1-TK mutant with increased GCV prodrug catalytic activity, with wildtype TK in C6 glioma cells. (hindawi.com)
Processes2
- Cancer's though have developed additional strategies to survive and so have very different metabolic processes than normal cells. (nottingham.ac.uk)
- Prodrugs must undergo chemical transformation through metabolic processes before they can become active agents. (kannastar.com)
Convert1
- Suicide gene systems that convert nontoxic systemically delivered prodrugs to active chemotherapeutic agents have been delivered via adenoviral vectors directly into cancer cells. (medscape.com)
Compound1
- To overcome these detractions and develop an improved tier 1 screening system that reduces the cost and time required for new compound evaluation, 490 BioTech proposes to develop a panel of multiple continuously bioluminescent human cell lines that will permit the simultaneous monitoring of each line to ascertain both the individual effects of compound treatment as well as the downstream effects of a compound's biotransformed metabolic breakdown products in real-time. (inknowvation.com)
Fractions1
- The metabolic profile of DABE in HLS9 fractions can be proven in Fig. 2. (gasyblog.com)
Fatty2
- So, Shanta Dhar and colleagues from Sylvester Comprehensive Cancer Center at the University of Miami wanted to develop a therapy that would inhibit fatty acid oxidation in cancer cells by targeting a mitochondrial protein that is vital to the metabolic process, making the cells susceptible to cisplatin. (acs.org)
- The cisplatin prodrug Platin-L, which has a cisplatin molecule bound to a 12-carbon fatty acid on one side and succinate on the other side, had the greatest effect by binding to a key protein required for long chain fatty acid transport, a primary step in this metabolic process. (acs.org)
Interactions1
- hence, a potential exists for metabolic interactions with other CYP3A substrates. (duke.edu)
Crucial1
- The prodrug approach is rapidly becoming a crucial part in the stratagem of delivery of drugs. (ijpsonline.com)
Suggests1
- Some literature suggests that metformin may help to reverse the pathophysiologic changes of metabolic syndrome. (medscape.com)
Agents2
- One of the most widely used agents in clinical setting is 2-[ 18 F]-fluoro-2-deoxy-D-glucose (FDG) [ 10 , 11 ], which is used as a marker of metabolic activity for glucose. (hindawi.com)
- [ 99 ] each of which may produce favorable metabolic alterations as single agents in patients with metabolic syndrome. (medscape.com)
Drug4
- The prodrug approach using various carriers has evolved as a significant tool in surmounting different obstacles in relation to drug formulation and targeting. (ijpsonline.com)
- Prodrugs have better delivery properties that surpass the parent drug molecule [ 1 ]. (ijpsonline.com)
- Prodrug concept is justified because it enables the active drug to overcome the barrier that would impede it from reaching the site of action to exert the required pharmacological activity. (ijpsonline.com)
- This project aims to understand the metabolic impacts of drug resistance in TB and using this information develop strategies for drastically improving the rate at which antibiotics are able to kill drug-resistant strains. (otago.ac.nz)
Molecular1
- Around 10 % of marketed medicines can be categorized as prodrugs currently, and also that during 2008, 33 % of approved small molecular weight drugs were prodrugs [ 5 - 7 ]. (ijpsonline.com)
Form1
- Atorvastatin lactone is a prodrug form of atorvastatin. (csnpharm.com)
High2
- The high conversion rate of curcumin prodrug TBP1901 to curcumin in bone marrow warrants its clinical application for diseases growing in the marrow like multiple myeloma and leukemia. (polyphenols-site.com)
- The opioid analgesic potency of a given dose of tramadol is influenced by an individual's CYP genetics, with poor metabolizers experiencing little conversion to the active M1 opioid metabolite and individuals with a high metabolic profile, or ultra-metabolizers, experiencing the greatest opioid analgesic effects. (medscape.com)
Potential2
- Recently, improvement in scanner resolution has allowed microPET to become a potential method to monitor metabolic patterns in small animal models. (hindawi.com)
- Further research is needed on the potential metabolic impact of longer-term doxycycline use. (cdc.gov)
Activity1
Clinical2
- Guadecitabine, a dinucleotide prodrug of a decitabine linked via phosphodiester bond to a guanosine, showed promising results in the phase-1 clinical trial, NIBIT-M4 (NCT02608437). (biomedcentral.com)
- METHODS: This review used the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines to search MEDLINE/PubMed for clinical studies published from August 2003 through January 2023 that reported on adverse events with doxycycline use with a focus on side-effects and metabolic effects of long-term use. (cdc.gov)
Researchers1
- The objective of this review is to provide the researchers with a compilation of which carriers would be suitable for prodrug synthesis and what would be their benefits. (ijpsonline.com)
Effects2
- The ENLIGHTEN trials showed the combination provided sustained antipsychotic efficacy with minimal effects on weight, waist circumference, and metabolic parameters. (medscape.com)
- HHC-O is the prodrug version of HHC and therefore has great medicinal effects. (kannastar.com)
Methods1
- Prodrug concentrations were quantified from the incubation samples using liquid chromatography- tandem mass spectrometry (LC-MSMS) methods developed for this study. (helsinki.fi)
Treatment1
Drugs1
- Carrier-linked prodrugs are for drugs with major drawbacks, which are linked to a nontoxic carrier or promoiety through covalent linkage to change or get rid of their undesirable physicochemical properties. (ijpsonline.com)
Rate1
- Studying the rate of prodrug formation alone estimations about clinically relevant bioactivation rates cannot be concluded. (helsinki.fi)
Project1
- We'll have the latest research updates, including the prodrug project that your donations have helped to fund. (cystinosis.org.uk)
Profile1
- Tramadol was originally thought to have a lower risk of constipation, respiratory depression, overdose, and addiction compared with other opioids, but CYP metabolic polymorphisms that will be described later in this review contribute to interesting phenotypic differences in the analgesic and side effect profile. (medscape.com)
Release1
- Serdexmethylphenidate/dexmethylphenidate is a fixed-dose combination of the prodrug of dexmethylphenidate, serdexmethylphenidate, and immediate-release dexmethylphenidate. (medscape.com)
Small1
- The metabolic depletion of DABE in HIMs demonstrated that M2 was the main metabolite in support of a small level of DAB was shaped (Fig. 3A, step one 1). (gasyblog.com)
Agent1
- A bioprecursor prodrug is transformed chemically through hydration (for example, lactones such as some statins), reduction (for example, sulindac, platinum (IV) complexes) or oxidation (for example, dexpanthenol, nabumetone) or metabolically to the active agent [ 5 , 9 - 11 ]. (ijpsonline.com)