Drug transporters. Medical search. Frequent questions

Used in conjunction with BioReliance technologies, B-CLEAR enables researchers to assess drug disposition and drug interactions within complex, whole-cell liver systems. (prnewswire.com)
The efflux measurements can then facilitate evaluation of biliary clearance, transporter interactions and intracellular concentration. (prnewswire.com)
The ability to accurately predict drug transporter interactions in the liver is a critical part of developing safer and more efficacious therapies," said Paul Brooks , Ph.D., Head of Discovery Research Services at Sigma-Aldrich. (prnewswire.com)
The understanding of the interplay is important in terms of deciphering the change of one eliminatory pathway on compensatory mechanisms in drug disposal, and, ultimately, their importance in drug-drug interactions. (nih.gov)
Drug-drug interactions can lead to changes in systemic exposure (e.g., maximum concentration (Cmax), area under the concentration time curve (AUC), average steady state concentration (Cpss)) potentially resulting in adverse reactions (higher drug exposure) or loss of efficacy (lower drug exposure). (fda.gov)
Thus, these enzymes and systems are often implicated in drug-drug interactions because of their effect on a drug's pharmacokinetics (e.g., drug exposure). (fda.gov)
These examples were evaluated and compiled by FDA as an optional resource for healthcare professionals to consult when reviewing information in the DRUG INTERACTIONS section of the approved U.S. Prescribing Information (PI) in clinical practice. (fda.gov)
This website contains examples of drugs with CYP enzyme-based and transporter-based interactions but does not include drugs with other mechanisms leading to drug interactions (such as certain interactions affecting drug absorption (e.g., chelating agents, resin-based binders, interactions, and drugs that change gut pH), interactions affecting drug plasma protein binding, or pharmacodynamic interactions). (fda.gov)
Researchers from the University of Toronto have created a map of the protein interactions of 19 members of the ATP-binding cassette transporter class in a species of yeast, combining this data with previously-reported ABC transporter interactions into a comprehensive "interactome. (genomeweb.com)
In the group's ABC transporter study, Stagljar and his team used MYTH to map the interactions of all of S. cerevisiae's 19 non-mitochondrial ABC transporters. (genomeweb.com)
They then combined the MYTH screening results with previously reported ABC transporter physical interactions available through the BioGRID database. (genomeweb.com)
The group went on in its recent study to investigate two potentially interesting associations revealed in the yeast ABC transporter interactome map: physical interactions of ABC transporters with one another and the interaction of these molecules with members of the zinc transport system. (genomeweb.com)
These transporters may play important roles in the disposition of aromatic diamidines in humans, as well as resultant drug-drug interactions and toxicity involving diamidine drugs. (aspetjournals.org)
Bhat S, Hasenhuetl PS, Kasture A, El-Kasaby A, Baumann MH, Blough BE, Sucic S, Sandtner W, Freissmuth M (2017) Conformational state interactions pro-vide clues to the pharmacochaperone potential of serotonin transporter partial sub-strates. (springer.com)
To elucidate the molecular mechanisms for the tubular excretion of diuretics, we have elucidated the interactions of human organic anion transporters (hOATs) with diuretics using cells stably expressing hOATs. (aspetjournals.org)
Due to the importance of drug transporters in these processes and the potential drug-drug interactions among drug molecules on these transporters, in vitro transport studies on a standard panel of drug transporters are recommended by the FDA, EMA, and PDMA regulatory agencies to evaluate the potential interactions as substrates and/or inhibitors among the investigational drugs. (alliancepharmaco.com)
Investigating the role of cell membrane proteins has increased over the last decade, as drugdrug interactions and genetic polymorphisms have been found to cause changes in drug pharmacokinetics and dynamics. (helsinki.fi)
The in vitro method developed in this study remains in the research team as a tool to investigate the polymorphisms of the SLCO1B1-gene, the inhibition of the transporter and possible drug interactions. (helsinki.fi)
Recent studies have shown that transporters can mediate drug-drug interactions, and transporter genes are subject to genetic polymorphism which may affect pharmacokinetic parameters of a drug, such as absorption, distribution, and excretion. (helsinki.fi)
Interactions of organophosphate flame retardants with human drug transporters. (bvsalud.org)
The present study investigates in vitro their possible interactions with human drug transporters, which are targets for environmental chemicals and actors of their toxicokinetics . (bvsalud.org)
Understanding drug interactions with the ENTs may inform and facilitate the development of new drugs, including chemotherapeutics and antivirals that require access to sanctuary sites such as the male genital tract. (arizona.edu)
SIGNIFICANCE STATEMENT This study developed computational models of human equilibrative nucleoside transporters (ENTs) to predict drug interactions and validated these models with two compounds in vitro. (arizona.edu)
Drug-drug interactions arise when drugs compete. (msdmanuals.com)
Due to system maintenance, the drug interactions feature you are attempting to access is temporarily unavailable. (medscape.com)
Antiepileptic drugs should be used carefully, with consideration of medication interactions and potential side effects. (medscape.com)

Table 2 provides definitions of substrates, inhibitors, and inducers for CYP-based metabolism and Table 3 provides definitions of inhibitors and substrates for drug transporter systems. (fda.gov)
The goal of this study is to investigate whether these dicationic drugs are substrates for human organic cation transporters (hOCTs, solute carrier family 22A1-3) and whether hOCTs play a role in their tissue distribution, elimination, and toxicity. (aspetjournals.org)
This is the first finding that dicationic drugs, such as pentamidine and furamidine, are substrates for hOCT1. (aspetjournals.org)
Here, we apply hydrogen-deuterium exchange mass spectrometry to probe the conformational dynamics of human SERT in the absence and presence of known substrates and targeted drugs. (ku.dk)
One molecule of ATP is hydrolyzed to transport substrates across the cell membrane while the second molecule of ATP is hydrolyzed to reset the transporter to its inward-facing conformation. (proteopedia.org)
The overall shift from inward-facing to outward-facing promotes the transport of substrates through the transporter. (proteopedia.org)
After substrates bind in Cavity 1, ATP binds each NBD leading to the transporter shifting from inward-facing to outward-facing. (proteopedia.org)
In many cases, transporters exhibit extremely high Gini coefficients, even when their supposed substrates might be expected to be available to all tissues, indicating a much higher degree of specialisation than is usually assumed. (biorxiv.org)
Perland and Fredriksson, 2017 ) or the pharmaceutical drug substrates of these transporters, and one clue to this may be to understand their differential tissue distribution. (biorxiv.org)
OPFRs also blocked the transporter-dependent membrane passage of endogenous substrates , notably that of hormones . (bvsalud.org)
Identification and prediction of ENT1 and ENT2 substrates allows for the determination of drugs that can penetrate tissues expressing these transporters. (arizona.edu)

Classic MDR is often correlated with the overexpression of three well-studied mammalian ABC transporters: P-glycoprotein (P-gp), Breast Cancer Resistant Protein (BCRP), and Multidrug Resistant Protein 1 (MRP1). (smu.edu)
For ABC transporters, a membrane vesicle assay (for P-gp and BCRP) and MDR1/MDCK bidirectional permeability assay (for P-gp) has been established. (alliancepharmaco.com)
Mechanistically, UroA or UAS03 chemosensitized the 5FUR cancer cells by downregulating the expression and activities of drug transporters (MDR1, BCRP, MRP2 and MRP7) leading to a decrease in the efflux of 5FU. (instem.res.in)
At the end of the fourth week, mRNA expressions of drug efflux transporters (P-glycoprotein and breast cancer resistance protein [BCRP] and MRP2 [multidrug resistance-associated protein-2]) were examined. (innovareacademics.in)
There were increased mRNA expressions of P-glycoprotein, BCRP, and MRP2 after four weeks of treatment with sorafenib, while treatment with quercetin decreased the drug efflux transporters expressions. (innovareacademics.in)
We suggest that decreased expressions of both drug efflux transporters, P-glycoprotein and BCRP, mediated by quercetin ameliorate the efficacy of sorafenib in TNBC. (innovareacademics.in)

Solute carrier organic anion transporter family member 1B3 (SLCO1B3) also known as organic anion-transporting polypeptide 1B3 (OATP1B3) is a protein that in humans is encoded by the SLCO1B3 gene. (wikipedia.org)
The secretion of numerous organic anions, including endogenous metabolites, drugs, and xenobiotics, is an important physiological function of the renal proximal tubule. (aspetjournals.org)
Organic Anion Transporting Polypeptide 2B1 (OATP2B1) is an influx transporter expressed widely throughout the body in tissues such as intestine, liver, brain, placenta and skeletal muscle. (helsinki.fi)
Very lipophilic drugs enter the cell membrane through passive diffusion, but polar or ionized organic compounds can enter the cell membrane only by transporters. (helsinki.fi)

The antiparasitic activity of aromatic diamidine drugs, pentamidine and furamidine, depends on their entry into the pathogenic protozoa via membrane transporters. (aspetjournals.org)
We analyse two comprehensive transcriptome datasets from human tissues and human-derived cell lines in terms of the expression profiles of the SLC and ABC families of membrane transporters. (biorxiv.org)
Development of human membrane transporters: Drug disposition and pharmacogenetics. (msdmanuals.com)

All three substances were also studied for their uptake and releasing properties at dopamine transporters (DAT), norepinephrine transporters (NET) and serotonin transporters (SERT) using in vitro monoamine transporter assays in rat brain synaptosomes and compared to mephedrone. (erowid.org)
Asjad HMM, Kasture A, El-Kasaby A, Sackel M, Hummel T, Freissmuth M, Sucic S (2017) Pharmacochaperoning in a Drosophila model system rescues human dopamine transporter variants associated with infantile/juvenile parkinsonism. (springer.com)
Beerepoot P, Lam VM, Salahpour A (2016) Pharmacological chaperones of the dopamine transporter rescue dopamine transporter deficiency syndrome mutations in heterologous cells. (springer.com)
An at-home olfactory test helps to identify people with an increased risk of having dopamine transporter imaging indicative of early Parkinson's disease, show data from the Parkinson Associated Risk Syndrome study. (news-medical.net)
Striatal dopamine transporter binding, assessed using single-photon emission computed tomography, is strongly correlated with substantia nigra cell counts assessed at postmortem, say the authors of a study. (news-medical.net)
Reduced striatal dopamine transporter availability is already present in patients with Parkinson's disease who go on to develop impulse control disorders, a study shows. (news-medical.net)
Dysfunction of the dopamine transporter has been hypothesized to play a role in the development of TD. (medscape.com)
[ 4 ] Thus, further research is needed to investigate the role of the dopamine transporter in the development and maintenance of TD. (medscape.com)

Nakashima, E 2008, ' Transporter-mediated specific drug therapy during pregnancy ', Drug Metabolism And Pharmacokinetics , vol. 23, no. 5. (elsevierpure.com)
ABCG2 also affects the pharmacokinetics of many drugs and contributes to multidrug resistance . (proteopedia.org)
Since many clinically used drugs are transported by OATP2B1, changes in the function of the transporter due to genetic polymorphism could lead to altered pharmacokinetics or -dynamics of OATP2B1 substrate drugs. (helsinki.fi)
Equilibrativenucleoside transporters (ENTs) participate in the pharmacokinetics and disposition of nucleoside analog drugs. (arizona.edu)
Drug transporters are important regulators of antiretroviral pharmacokinetics. (pitt.edu)
Overview of Pharmacokinetics Pharmacokinetics, sometimes described as what the body does to a drug, refers to the movement of drug into, through, and out of the body-the time course of its absorption, bioavailability, distribution. (msdmanuals.com)
It is important to understand the mechanisms of action and the pharmacokinetics of antiepileptic drugs (AEDs) so that these agents can be used effectively in clinical practice, especially in multidrug regimens (see the image below). (medscape.com)
1,2 The variations in the response to treatment may be due to several factors such as illness, differences in pharmacokinetics and pharmacodynamics of drugs, environmental factors and genetic factors. (bvsalud.org)
The pharmaceutical literature consists of numerous examples of 2-D QSARs, 3-D QSARs and expert systems for modelling the individual components or phases of drug disposition and pharmacokinetics (i.e. absorption, distribution, metabolism and *Corresponding author. (cdc.gov)

These data emphasize the importance of uptake and efflux transporters on hepatic drug metabolism. (aspetjournals.org)
This study aimed to investigate whether quercetin is able to improve the efficacy of sorafenib in triple negative breast cancer cells and explore the possibility of drug efflux transporters modulation by quercetin. (innovareacademics.in)

The isomer N-methoxymephedrone was found to be a weak uptake blocker at DAT, NET and SERT and a fully efficacious substrate-type releasing agent across all three transporters with EC50 values in the low micromolar range. (erowid.org)
The pharmacological correction of folding defects was originally explored in mutants of the serotonin transporter (SERT, SLC6A4), which were created to study the COPII-dependent export from the endoplasmic reticulum. (springer.com)
The serotonin transporter (SERT), a member of the neurotransmitter:sodium symporter family, is responsible for termination of serotonergic signaling by re-uptake of serotonin (5-HT) into the presynaptic neuron. (ku.dk)

Unlike many other transporters, which only work with single compounds, such protein pumps can export a variety of drugs. (acs.org)
One half of a split ubiquitin molecule is attached to an ABC transporter (or another cellular protein of interest) and the other half to its potential interaction targets. (genomeweb.com)
The Innovative Medicines Initiative Consortium RESOLUTE has started to develop tools and produce data sets to de-orphanize transporters in the solute carrier protein (SLC) superfamily, thereby lowering the barrier for the scientific community to explore SLCs as an attractive drug target class. (univie.ac.at)
The ABCG2 multidrug transporter or abc subfamily G member 2 is a membrane protein from the A TP- B inding C assette (ABC) transporter family, specifically the G-subfamily. (proteopedia.org)
In this study the characteristics of the OATP1B1 transporter were reviewed and new in vitro research method to study protein functions was developed. (helsinki.fi)
In January 2019, a study published in Nature Metabolism proved the theory of an NMN transporter: a protein encoded by the gene Slc12a8. (prohealth.com)
The transporters were found to localize at multiple cell types along the cervicovaginal tract, and the protein abundance and localization of transporters were affected by menstrual cycle and hormone/contraceptive use in a mouse model. (pitt.edu)
Structure and function of the MRP2 (ABCC2) protein and its role in drug disposition. (medlineplus.gov)

The B-CLEAR technology enables effective measurement of uptake and efflux into the bile pocket, and the overall integrated effect of transporters and metabolism can also be evaluated. (prnewswire.com)

Until now, the study of the individual role of a transporter in primary hepatocytes and HepaRG cells, which express all of the hepatic transporters, was very difficult. (prnewswire.com)
OPFRs additionally repressed mRNA expressions of some transporters in cultured human hepatic HepaRG cells , especially those of OAT2 and OCT1 in response to TOCP, with IC50 values of 2.3 µM and 2.5 µM, respectively. (bvsalud.org)

Whether a user is interested in uptake transporter knockouts or efflux transporter knockouts, measuring changes in intracellular concentration is the perfect readout to understand their effects," said Dr. Christopher Black , CEO for Qualyst Transporter Solutions. (prnewswire.com)

The group hopes the map, published online this week in Nature Chemical Biology , will be a resource for future applied research, providing insight into these molecules' roles in a variety of cellular processes with implications for drug development and other clinical areas. (genomeweb.com)
We can use the oligomerisation domain as a framework, in order to decorate it with drug molecules. (nanowerk.com)
In the new approach, bacteria can carry hundreds of nanoparticles, each of which can in turn carry hundreds of drug molecules, depending on the size of the nanoparticles. (medgadget.com)
Drug transporters play a key role in the absorption, distribution, metabolism, elimination and toxicity (ADME-Tox) of many drugs by controlling the entry or exit of drug molecules into and out of tissues or organs. (alliancepharmaco.com)

P-gp is the most studied ABC transporter, and the search for P-gp inhibitors as co-therapeutics to combat MDR has had little success after decades of studies. (smu.edu)
P-gp reconstituted into nanodiscs were used to evaluate the potential of our newly discovered drug-like compound to serve as inhibitors of human P-gp ATP hydrolysis activity. (smu.edu)
These structures also illustrated the transporter cycle of ABCG2, the binding locations for inhibitors, and the link between cancer and the ABC transporter family. (proteopedia.org)
The main groups include sodium channel blockers, calcium current inhibitors, gamma-aminobutyric acid (GABA) enhancers, glutamate blockers, carbonic anhydrase inhibitors, hormones, and drugs with unknown mechanisms of action (see the image below). (medscape.com)
Can you explain sodium glucose co-transporter-2 (SGLT-2) inhibitors? (medscape.com)

We hold the opposite view and assert that increased secretion should evoke a decrease in metabolism due to the competition between the enzyme and apical efflux transporter for the drug within the cell. (nih.gov)
The conclusion is that the f(met) is the more appropriate index to reflect the extent of metabolism in transporter-enzyme interplay, since the parameter captures drug metabolism in the cell when its contents in the apical, cell, and basolateral compartments or the entire dose is considered to be available for metabolism. (nih.gov)
This parameter for metabolism (f(met)) bears a reciprocal relationship to the secretory intrinsic clearance and is in concordance with the notion that both the enzyme and apical transporter compete for the cellular substrate within. (nih.gov)
The use of an increased MRT to explain increased extents of metabolism upon increased apical excretion is not tenable in these organs or "open systems" since the MRT of drug in the cell is reduced with irreversible loss from biliary excretion or hastened gastrointestinal transit of the secreted drug in the lumen. (nih.gov)
The general conclusion is that a reciprocal relationship exists between the clearances related to enzymes and apical transporters due to their competition for the substrate within the cell, and is a relationship independent of the MRT of drug in the system. (nih.gov)
Transporters in the canalicular domain (apical) of the hepatocyte faclitate removal of drugs or metabolites from the cell interior. (helsinki.fi)

The NBDs in ABCG2 remain in contact with one another even without a bound substrate, providing greater substrate specificity as the entrance to the transporter is not as globular as other ABC transporters like ABCB1 or ABCC1. (proteopedia.org)
Our first discovery, with my colleagues Igor Roninson and Ira Pastan, was that multidrug-resistant cancers overexpressed a gene that encoded an ATP-dependent transporter, termed P-glycoprotein, MDR1 or ABCB1. (sciencewatch.com)
In fact, ABCB1 belongs to a family of 48 human ATP-dependent transporters, of which approximately 50% can confer resistance to one or another drug. (sciencewatch.com)

[2] ABCG2 belongs to the family of 48 transporter proteins called ATP-binding cassette transporters (ABC transporters). (proteopedia.org)

Several reviews and reports present the advantages and limitations of the currently available algorithms and software for in silico modelling of the drug dissolution/bioavailability, oral absorption rate/fraction, volume of distribution, path- ways, affinities or rates of metabolism, renal excretion rate as well as affinity for specific transporters [3-20]. (cdc.gov)

The crystal structure of the multidrug transporter LmrP, shown here as side (left) and top views, reveals a lipid (blue) in the binding pocket along with the substrate (green). (acs.org)

In particular, with some exceptions such as olfactory receptors and genes involved in keratin production, transporter genes are significantly more heterogeneously expressed than are most non-transporter genes. (biorxiv.org)
We hope to determine which multidrug-resistance genes are important in clinical drug resistance, and then design approaches to circumventing or overcoming these forms of drug resistance. (sciencewatch.com)
We set about to develop models of multidrug-resistant cancers in cultured cells and use sophisticated molecular techniques to isolate the genes whose expression conferred resistance to the drugs. (sciencewatch.com)
Although this gene is frequently expressed in drug-resistant cancers, inhibiting it had only minor effects on drug resistance in cancer patients, undoubtedly because there are many other multidrug resistance genes. (sciencewatch.com)
Plus, there are many other genes whose expression can confer drug resistance. (sciencewatch.com)
Pharmacogenetic (PGx) tests are used to help predict an individual's reaction to drugs by interrogating the presence or absence of known genetic variants in genes that encode drug-metabolizing enzymes, drug transporters, drug receptors, or targets of drug action. (cdc.gov)

The Gini index (coefficient) characterises inequalities of distributions, and is used in a novel way to describe the distribution of the expression of each transporter among the different tissues and cell lines. (biorxiv.org)
Similar trends hold true for the expression profiles of transporters in different cell lines, suggesting that cell lines exhibit largely similar transport behaviour to that of tissues. (biorxiv.org)
By contrast, the Gini coefficients for ABC transporters tend to be larger in cell lines than in tissues, implying that some kind of a selection process has taken place. (biorxiv.org)
Drug exposure in the cervicovaginal tissues, colorectal tissue, and immune cells positively correlates with PrEP effectiveness, and there is an urgent need to identify critical physiologic determinants of drug exposure in these relevant tissues and cells, to inform product optimization. (pitt.edu)
This dissertation aims to examine the expression, regulation, and function of drug transporters in human cervicovaginal and colorectal tissues, as well as in the animal models and cell lines utilized in PrEP product testing. (pitt.edu)
Collectively, these studies have shown that antiretroviral drug-related transporters are positively expressed in tissues and cells relevant to HIV-1 sexual transmission, and their expression can be regulated by hormones and cytokines. (pitt.edu)
For example, MRP2 clears certain drugs from organs and tissues, playing a part in drug metabolism. (medlineplus.gov)

Multidrug resistant (MDR) cancers often become resistant to pharmacologically and structurally diverse drugs by overexpressing members of the family of ATP Binding Cassette (ABC) transporters. (smu.edu)
The 2 major transporters are adenosine triphosphate (ATP)-binding cassette (ABC, also referred to as P-glycoprotein) and the solute carrier (SLC) transporters. (msdmanuals.com)

For SLC transporters, an assay platform based on transiently transfected HEK293 cells has been optimized and validated, and can be used for both screening of substrate/inhibitor and K m /IC 50 determination. (alliancepharmaco.com)
These transporters, many of which are sodium-coupled, have been shown to use an elevator mechanism of transport, but exactly how substrate binding is coupled to sodium ion binding and transport is not clear. (elifesciences.org)
Here, we solve the crystal structure at 2.3 Å of a transporter from Neisseria meningitidis (ASBT NM ) in complex with pantoate, a potential substrate of ASBT NM . (elifesciences.org)
The manuscript represents an important contribution to an ongoing discussion about the substrate binding site and mechanism of the Bile Acid Sodium Symporter (BASS) family of transporters. (elifesciences.org)

The field of metabolic and transporter pharmacology is rapidly evolving, thus the examples in Table 1 are a guide and not considered a comprehensive list of all possible drugs and other substances (e.g., foods, including dietary supplements) that fit these categories. (fda.gov)
According to Shomron 7 (2010), this field of the clinical pharmacology studies the contribution of genomes, transcriptomes and proteomes in determining drug-response phenotypes (safety and efficacy). (bvsalud.org)

Though the group did the mapping with ABC transporters from a yeast species - Saccharomyces cerevisiae - many of the proteins are homologous to disease-linked human ABC proteins. (genomeweb.com)
ABC transporters are one of these pharmaceutically very important proteins because they play a role in health and disease, specifically drug resistance," Stagljar explained. (genomeweb.com)
The latter, Stagljar said, is an important area for drug development, because it opens the possibility that you could block ABC transporter activity by blocking associated zinc transport proteins. (genomeweb.com)
The Slc gene, which stands for 'solute carriers', is a super-family of over 395 membrane transport proteins, whose roles range from nutrient transport to drug delivery. (prohealth.com)
Both proteins also influence drug distribution. (elifesciences.org)

The aim of this study was to test for the molecular and functional expression of the non-gastric H + /K + ATPase ATP12A/ATP1AL1 in unstimulated and butyrate-stimulated (1 and 10 mM) human myelomonocytic HL-60 cells, to unravel its potential role as putative apoptosis-counteracting ion transporter as well as to test for the effect of the H + /K + ATPase inhibitor SCH28080 in apoptosis. (karger.com)
A high percentage of the ABC family transporters (19 of the 48) transport chemotherapeutic agents out of cells, making expression levels of ABC transporters a major indicator of cancer treatment prognosis. (proteopedia.org)
2017) Expression and regulation of drug transporters in vertebrate neutrophils. (shef.ac.uk)
Expression of SLC and ABC transporters in human and zebrafish neutrophils. (shef.ac.uk)
The expression of OATP1B1 transporter in HEK293 cells was successful. (helsinki.fi)
The effects of mono (UroA/UAS03/5FU) and combinatorial therapy (UroA/UAS03 + 5FU) on cell proliferation, apoptosis, cell migration and invasion, regulation of epithelial mesenchymal transition (EMT) mediators, expression and activities of drug transporters, and their regulatory transcription factors were examined using molecular, cellular, immunological and flowcytometric methods. (instem.res.in)
Menstrual cycle, exogenous hormones, contraceptives, and proinflammatory cytokines were found to impact transporter expression in mice and/or cell lines. (pitt.edu)

"Synthesis, characterization and monoamine transporter activity of the new psychoactive substance mexedrone and its N-methoxy positional isomer, N-methoxymephedrone" Drug Test Anal . (erowid.org)

OATP1B3 is a 12-transmembrane domain influx transporter. (wikipedia.org)

Anderluh A, Hofmaier T, Klotzsch E, Kudlacek O, Stockner T, Sitte HH, Schütz GJ (2017) Direct PIP2 binding mediates stable oligomer formation of the serotonin transporter. (springer.com)

This review highlights the "interplay" between enzymes and transporters, essential components of eliminating organs for drug removal. (nih.gov)
Controversy existed on the explanation underlying the interplay between transporters and enzymes in the Caco-2 cell monolayer or cell culture systems, but less so on eliminating organs such as the intestine and liver. (nih.gov)
Cytochrome P-450 (CYP) enzymes are responsible for the metabolism of many drugs, and transporter systems allow for movement of many drugs across cell membranes. (fda.gov)
Table 1 also includes five other substances that interact with CYP enzymes and transporter systems (i.e. (fda.gov)
Drug removal is not only dependent on metabolic enzymes, but also on transporters. (helsinki.fi)
Transporters in the basolateral membrane of the hepatocyte facilitate drug entry and access to drug metabolizing enzymes. (helsinki.fi)

UCSF scientists are studying key drug transporters that play roles in drug absorption and elimination. (ucsf.edu)

This study provided the novel characteristics of gut microbial metabolites to have significant translational implications in drug-resistant cancer therapeutics. (instem.res.in)

However, by using Sigma-Aldrich CompoZr ® Zinc Finger Nuclease (ZFN) technology, HepaRG transporter knockout cell lines have been created empowering more accurate research investigations of liver transporters. (prnewswire.com)
Normally expressed in the liver, the transporter functions to uptake large, non-polar drugs and hormones from the portal vein. (wikipedia.org)
The liver is the major site of drug metabolism and excretion. (helsinki.fi)

Many bacterial cells defend themselves against antibiotics by expelling the drugs using multidrug efflux pumps. (acs.org)
However, no such diamidine transporter has been identified in mammalian cells. (aspetjournals.org)
The proton-coupled folate transporter (PCFT) is ubiquitously expressed in solid tumors to which it delivers antifolates, particularly pemetrexed, into cancer cells. (aspetjournals.org)
The augmentation of intracellular pH, when cells are in a HEPES buffer, should be taken into consideration in studies that encompass all proton-coupled transporter families. (aspetjournals.org)
Human Embryonic Kidney cells (HEK) is a human derived mammalian cell-line that is widely used in the study of OATP1B1 transporter. (helsinki.fi)
HEK293 cells expressing OATP1B1 transporter are well suited for the study of the SLCO1B1-gene. (helsinki.fi)
Oncologists won't be able to cure cancers that have spread unless they can use drugs that specifically kill these cancer cells and spare normal cells. (sciencewatch.com)
Last year's discovery of the " elusive transporter " that efficiently shuttles NMN (nicotinamide mononucleotide) into cells to be converted into NAD (nicotinamide adenine dinucleotide) and used as fuel has opened up new doors - both for anti-aging and health research and quite literally, in the case of NMN entering cells. (prohealth.com)
The research team, led by Shin-ichiro Imai, MD, Ph.D., discovered that Slc12a8 is a specific transporter for NMN, meaning that NR isn't able to enter cells by that pathway. (prohealth.com)
Our cells attempt to maintain a consistent fuel supply by increasing the amounts of the NMN transporter in times of low NAD+, which would then enable NMN to be quickly converted into NAD+. (prohealth.com)
Providing your cells with NMN as well as enhancing the function of its transporter would be an ideal way to increase cellular energy throughout the lifespan. (prohealth.com)

My interest in this problem began in the 1980s when it became clear that there were some very effective anti-cancer drugs, but some cancers didn't respond and others developed resistance. (sciencewatch.com)
SUMMARY Studies done between 1997 and 2003 are reviewed to give an overall picture of antimalarial drug resistance in the Eastern Mediterranean Region of the World Health Organization (WHO). (who.int)
An overview of drug resistance gion. (who.int)
Resis- assessment of in vivo drug response in P. tance to antimalarial drugs has been de- falciparum were developed shortly after scribed for 2 of the 4 species of human the first reports of CQ resistance in this malaria parasites, Plasmodium falciparum species [ 1 ]. (who.int)
Plasmodium falciparum has sequently revised [ 9 ] and have remained developed resistance to nearly all antimalar- basically unchanged since the WHO Scien- ials in current use, although the geographi- tific Group on the Chemotherapy of Malar- cal distribution and prevalence rates of ia and Resistance to Antimalarials in 1972 resistance to individual drugs do vary. (who.int)

The nomenclature system begins with the root symbol Slc, followed by a number that indicates the family, then by a letter designating the sub-family (however, only 'a' is used when the family has not been subdivided), and lastly another number that defines the individual transporter gene. (prohealth.com)

Thank you for sharing this Drug Metabolism & Disposition article. (aspetjournals.org)
Message Body (Your Name) thought you would be interested in this article in Drug Metabolism & Disposition. (aspetjournals.org)
Drug Metabolism and Disposition , 49 (7), 479-489. (arizona.edu)
New insights in the biology of ABC transporters ABCC2 and ABCC3: impact on drug disposition. (medlineplus.gov)

We previously used high-throughput in silico ligand docking studies and identified drug-like compounds that reversed MDR in human cancers cell lines. (smu.edu)
A smaller panel of transporters were positively detected in three epithelial cell lines (End1/E6E7, Ect1/E6E7, VK2/E6E7) derived from human endocervix, ectocervix, vagina, and a T cell line (PM1). (pitt.edu)

WASHINGTON -- Another ileal bile acid transporter inhibitor has demonstrated in a phase III trial the ability to reduce pruritus and serum bile acids for kids with progressive familial intrahepatic cholestasis (PFIC). (medpagetoday.com)
Odevixibat (Bylvay), also an ileal bile acid transporter inhibitor, was approved in July 2021 to treat PFIC-related pruritus in children ages 3 months and up. (medpagetoday.com)

As an ABC Transporter , ABCG2 exhibits ATPase activity and uses the energy of ATP hydrolysis to facilitate transport. (proteopedia.org)

These computational and in vitro models can inform compound selection in the drug discovery and development process, thereby reducing time and expense of identification and optimization of ENT-interacting compounds. (arizona.edu)

We showed [in the paper] for the first time this interaction between some ABC transporters of the PDR subfamily and zinc transporters," Stagljar said. (genomeweb.com)

The abuse of synthetic psychoactive substances known as "designer drugs," or "new psychoactive substances" (NPS), is increasing at an alarming rate. (jneurosci.org)
Psychoactive "bath salts" first appeared in the recreational drug marketplace of the United States during late 2010. (jneurosci.org)

Although dedicated studies in large cohorts of patients are needed to confirm this observation, we speculate that patients carrying procholestatic hepatobiliary transporter variants may benefit from vaccination against hepatitis A. (elsevier.es)

LmrP is a great model to understand how transporters of the major facilitator superfamily (MFS) work," Govaerts says. (acs.org)

Keep reading to learn more about the elusive transporter and its various roles in the body. (prohealth.com)

OATP1B3 has also been identified as a transporter aberrantly expressed in prostate cancer and implicated in prostate cancer progression. (wikipedia.org)

Tubular secretion of acetazolamide was demonstrated to be important for the elimination of this drug in the study using the isolated rat perfused kidney ( Taft and Sweeney, 1995 ). (aspetjournals.org)
Additionally, the NMN transporter, Slc12a8, may have a relationship with the pathogenesis of autoimmune-related skin conditions and kidney function. (prohealth.com)
What about this new class of drugs that involves the kidney? (medscape.com)
We have glucose transporters in the kidney and so the kidney is very good at reabsorbing glucose. (medscape.com)

Medically reviewed by Drugs.com on Feb 8, 2023. (drugs.com)
Medically reviewed by Drugs.com on May 5, 2023. (drugs.com)

Microbial metabolite restricts 5-fluorouracil-resistant colonic tumor progression by sensitizing drug transporters via regulation of FOXO3-FOXM1 axis. (instem.res.in)

This broad association "suggests that [ABC transporters] involvement in cellular function is more complex than previously demonstrated," the authors wrote. (genomeweb.com)
Before cellular metabolism can occur, a drug must first enter the hepatocyte. (helsinki.fi)

Anatomy21

Organisms13

Diseases1

Chemicals and Drugs157

Analytical, Diagnostic and Therapeutic Techniques and Equipment16

Phenomena and Processes44

Disciplines and Occupations3

Information Science4

Interactions26

Substrates11

BCRP6

Organic4

Membrane transporters3

Dopamine8

Pharmacokinetics9

Efflux transporters2

SERT3

Protein8

Uptake and efflux1

Hepatic2

Interested in uptake1

Molecules4

Inhibitors5

Apical6

ABCB13

Family of 481

Specific transporters1

Multidrug transporter1

Genes6

Tissues7

Cassette2

Substrate4

Pharmacology2

Proteins5

Expression7

Monoamine1

Influx transporter1

Serotonin transporter1

Enzymes6

Absorption1

Metabolites1

Liver3

Cells11

Resistance5

Gene1

Disposition4

Human2

Bile2

ABCG21

Compounds1

Subfamily1

Psychoactive2

Variants1

Superfamily1

Roles1

OATP1B31

Kidney4

20232

Regulation1

Cellular2