• The ATP-binding cassette transporters (ABC transporters) are a transport system superfamily that is one of the largest and possibly one of the oldest gene families. (wikipedia.org)
  • ABC transporters are considered to be an ABC superfamily based on the similarities of the sequence and organization of their ATP-binding cassette (ABC) domains, even though the integral membrane proteins appear to have evolved independently several times, and thus comprise different protein families. (wikipedia.org)
  • ABC transporters utilize the energy of ATP binding and hydrolysis to transport various substrates across cellular membranes. (wikipedia.org)
  • The protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. (nih.gov)
  • Among the main mechanisms of this multidrug resistance is the overexpression of ATP-binding cassette (ABC) transporters that mediate drug efflux, and, specifically, ABCB1, ABCG2 and ABCC1 are known to cause cancer chemoresistance. (nature.com)
  • Furthermore, genetic modification of ABC transporters by CRISPR-Cas9 and approaches to re-engineer amino acid sequences to change the direction of transport from efflux to import are briefly discussed. (nature.com)
  • Fig. 2: Structures of three ATP-binding cassette transporters. (nature.com)
  • Fig. 3: Substrate-binding pockets of ATP-binding cassette transporters and the drug transport cycle. (nature.com)
  • Fig. 4: Emerging therapies targeting ATP-binding cassette transporters. (nature.com)
  • mainly involved in uptake, and ABC transporters (ABCs), mainly involved in efflux (e.g. (biorxiv.org)
  • ATP-binding cassette transporters ABCA1 and ABCG1 primarily mediate the efflux of cholesterol from peripheral cells. (diabetesjournals.org)
  • These transporters promote unidirectional cholesterol efflux to lipid-poor apolipoprotein A-I (apoA-I), apoE, or HDL particles, respectively, and are under the transcriptional control of liver X receptors (LXRs), master intracellular sensors that are activated in response to cholesterol biosynthetic intermediates and oxysterols ( 11 , 12 ). (diabetesjournals.org)
  • LXRs also transcriptionally regulate the cholesterol efflux transporters ABCA1 and ABCG1, and deficiency of ABCA1 is associated with decreased body weight ( 18 ), while ABCG1 deficiency protects against diet-induced obesity ( 19 ). (diabetesjournals.org)
  • Two types of transporters are identified in intestine i.e. uptake and efflux transporters. (omicsonline.org)
  • It has been reported that solute carrier (SLC) and the ATP-binding cassette (ABC) transporter super families are the major class of membrane transporters [ 14 , 17 ]. (omicsonline.org)
  • Even though species differences in Mrp2-mediated biliary efflux have previously been reported, agreement on the degree of difference remains to be determined, because the absolute differences of transporters in these models remain unknown. (aspetjournals.org)
  • Several compounds have been shown to inhibit the efflux activity of ABC transporters, thereby increasing intracellular drug accumulation and sensitising cancer cells to therapy. (spandidos-publications.com)
  • The exact biological mechanism(s) by which the BBB limits drug exposure is not clear, but in addition to epithelial tight junctions, enhanced efflux of chemotherapeutic agents out of the CNS space by endothelial cell membrane transporters in brain blood vessels plays a primary role ( 2 ). (jcancer.org)
  • Key drug efflux transporters operational in preserving the BBB are the P-glycoprotein (Pgp) transporter, which belongs to the ATP-binding cassette (ABC) transporter family, and the breast cancer resistance protein (BCRP) ABCG2 ( 4 , 5 ). (jcancer.org)
  • However, for most BBB transporters, it is still difficult to synthesize selective probes and inhibitors to enable specific evaluation of the transport activities of the target transporters, because of the effects of other transporters, including functionally unknown transporters, as well as binding to brain tissues. (aspetjournals.org)
  • ABC (ATP binding cassette) transporters catalyze the transport of a wide variety of molecules across lipid bilayers into or out of cells and organelles. (rug.nl)
  • Heide van der T., and Poolman, B. (2002) ABC transporters: one, two or four extracytoplasmic substrate-binding sites? (rug.nl)
  • In agreement with the reduced preβ-HDL particles, cholesterol efflux capacity mediated by the transporters ABCA1 and ABCG1 was reduced in AD patients' plasma. (biomedcentral.com)
  • The ATP-binding cassette (ABC) of active transporters comprises a group of proteins that which facilitate efflux of anticancer drugs from cancer cells. (lu.se)
  • Pathogens use siderophores, such as Enterobactin, to scavenge iron that is in complex with high-affinity iron-binding proteins or erythrocytes. (wikipedia.org)
  • Dr. Remaley's laboratory is now focused on how the ABCA1 transporter interacts with other intracellular proteins, as well as with extracellular cholesterol acceptor proteins, such as apoA-I, during the cholesterol efflux process. (nih.gov)
  • However, because of the unknown binding affinity of antibody to MRP2/Mrp2 protein across species and lack of purified MRP2/Mrp2 proteins for calibration, the immunoblotting assay was excluded from the absolute quantification of MRP2/Mrp2 protein for multiple species. (aspetjournals.org)
  • A number of mechanisms involved in the occurrence of MDR have been described, including the overexpression of one or more ATP binding cassette (ABC) transporter proteins that mediate the efflux of many clinically relevant drugs. (spandidos-publications.com)
  • Carbamylation (carbamoylation stricto sensu) of HDL proteins is a non-enzymatic irreversible process mediated by isocyanate, and corresponds to the binding of a carbamoyl moiety (-CONH 2 ) to lysine, resulting in carbamyl-lysine. (biomedcentral.com)
  • Cholesterol efflux from adipocytes is mediated by the cholesterol transport proteins ATP-binding cassette A1 (ABCA1) and ATP-binding cassette G1 (ABCG1). (biomedcentral.com)
  • Multidrug resistance (MDR) proteins related to the ATP-binding cassette family are found in a very wide range of human tumors and result in therapeutic failure. (ebsco.com)
  • ABCA1 is expressed in many organs and is thought to mediate HDL maturation by facilitating the efflux of cellular phospholipids and cholesterol onto apolipoproteins. (jci.org)
  • The central helices of ApoA-I can promote ATP-binding cassette transporter A1 (ABCA1)-mediated lipid efflux. (medlineplus.gov)
  • Amino acid residues 220-231 of the wild-type ApoA-I are required for lipid efflux in vitro and high density lipoprotein formation in vivo. (medlineplus.gov)
  • The ATPase subunits utilize the energy of adenosine triphosphate (ATP) binding and hydrolysis to provide the energy needed for the translocation of substrates across membranes, either for uptake or for export of the substrate. (wikipedia.org)
  • Most of the uptake systems also have an extracytoplasmic receptor, a solute binding protein. (wikipedia.org)
  • D. & E. Uptake systems with two or four covalently linked substrate-binding domains (SBDs). (rug.nl)
  • To characterize factors affecting milciclib pharmacokinetics, we investigated whether milciclib is a substrate of the multidrug effluX and uptake trans- porters ABCB1 (P-gp), ABCG2 (BCRP), and OATP1A/1B, and the drug-metabolizing enzyme CYP3A, using genetically-modified mouse models and Madin-Darby Canine Kidney (MDCK-II) cells. (srcinhibitors.com)
  • APOA4 on prebeta and prebeta-b particles efflux cholesterol from peripheral tissues via ATP-binding cassette transporter A1 (ABCA1) (step 3). (jci.org)
  • We previously reported that hepatobiliary transporter multidrug resistance-associated protein (MRP2/Mrp2) is considered to be the major cause of the interspecies differences detected by efflux of fluorescent substrates in isolated hepatocytes. (aspetjournals.org)
  • The UIC2 monoclonal antibody specifically binds to an extracellular epitope of CD243, which is also known as ATP-binding cassette subfamily B member 1 (ABCB1), Multidrug resistance protein 1 (MDR1), or P-glycoprotein 1. (bdbiosciences.com)
  • The overexpression of efflux pumps such as ABCB1 is one of the mechanisms of MDR. (ebsco.com)
  • ABCA1 regulates the formation of nascent high-density lipoprotein (HDL) via cholesterol efflux to lipid free apolipoprotein A-1, whereas ABCG1 mediates cholesterol transport to the HDL fraction [ 13 ]. (biomedcentral.com)
  • The UIC2 antibody reportedly inhibited the efflux of CD243 substrates from MDR cells and increased the cytotoxicity of certain CD243-transported drugs. (bdbiosciences.com)
  • The transport, metabolism and efflux of terfenadine and its metabolites were investigated in TC7 monolayers. (nih.gov)
  • Ketoconazole increased the AP-BL transport terfenadine dramatically by inhibiting both terfenadine metabolism and Pgp efflux. (nih.gov)
  • Xenobiotics and their metabolites are generally eliminated and detoxified by phase I and phase II enzymatic metabolism, by phase III transporter-mediated drug efflux to bile, or by both mechanisms. (aspetjournals.org)
  • ATP-Binding Cassette Transporter Family C Protein 10 Participates in the Synthesis and Efflux of Hexosylceramides in Liver Cells. (nih.gov)
  • 71 Clusterin is a small heat shock glycoprotein overexpressed in most of the solid tumors, which promotes apoptosis by binding to various molecules such as BAX (BCL2-associated X protein) 72 and signal transducer and activator of transcription (STAT)−1. (oncologynurseadvisor.com)
  • 3 The tandem CBS domain 4 , which is linked to the nucleotide binding protein, plays a pivotal role in the regulation. (rug.nl)
  • CD243 acts as an ATP-dependent efflux pump for a large variety of lipophilic molecules and drugs. (bdbiosciences.com)
  • However, these drugs have little effect on brain metastasis due to the combined effects of poor penetration of the blood-brain barrier and their removal from the central nervous system (CNS) by the p-glycoprotein (Pgp) drug efflux pump. (jcancer.org)
  • Because BAAA is usually equally fluorescent compared to its turned-over carboxylate product, CSCs are identified based on their ability to retain the BAAA product relative to the unactivated probe using efflux pump inhibitors. (bioskinrevive.com)
  • While LXR-deficient mice are leaner than littermate controls and are protected against diet-induced obesity, the mechanisms that control fat loss in these mice are still a matter of debate and could involve either reduced lipogenesis, enhanced lipid oxidation and lipolysis, or reduced cholesterol efflux pathways ( 14 ). (diabetesjournals.org)
  • Furthermore, we determined the major components of GLSP triterpenes, including Ganoderic acid A, Ganoderic acid B, Ganoderic acid C6, Ganoderic acid G, and Ganodermanontriol, and found that these triterpenes promoted ABCA1/G1-mediated cholesterol efflux and inhibited inflammation in macrophage, and inactivated RUNX2-mediated osteogenesis in VSMC. (thno.org)
  • Unlike lapatinib, TAK-285 is not a substrate for Pgp efflux. (jcancer.org)
  • C. auris exhibited higher thermotolerance, virulence in a mouse infection model, and ATP-dependent drug efflux activity than C. haemulonii . (cdc.gov)
  • A fourth mechanism suggests that cytotoxic drugs are removed from the source using efflux pumps, and the last mechanism is microtubule alterations that affect cytotoxic drug attachment to cancer cells. (oncologynurseadvisor.com)
  • Genetic variation in the ATP binding cassette transporter ABCC10 is associated with neutropenia for docetaxel in Japanese lung cancer patients cohort. (nih.gov)
  • Overall, these processes allow the regeneration of NAD + required for ATP production through glycolysis. (hindawi.com)
  • The production process underwent stringent testing and validation to assure that it generates a high-quality conjugate with consistent performance and specific binding activity. (bdbiosciences.com)
  • This efflux activity has been suggested to lead to resistance to the drugs used in chemotherapy. (bdbiosciences.com)
  • Another focus of Dr. Remaley's work is on the main cholesterol efflux transporter from cells, namely the ATP-binding cassette transporter 1 (ABCA1). (nih.gov)
  • Inhibition studies indicated that the efflux was mediated by Pgp. (nih.gov)
  • Cholesterol mobilization involves adipose tissue ATP-binding cassette transporter A1 (ABCA1), which has recently been shown to contribute to HDL biogenesis in vivo ( 9 , 10 ). (diabetesjournals.org)