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  • proteins
  • Here we measured binding and transport of model substrate 1-methyl-4-phenylpyridinium + (MPP + ) by cell-free-expressed fusion proteins of rOCT1 and various rOCT1 mutants with green fluorescent protein that were reconstituted into nanodiscs or proteoliposomes. (aspetjournals.org)
  • Last but not least, some of these transporter proteins can also be envisaged as drug targets, as long as they can show "transceptor" functions, in some cases related to their role as modulators of extracellular adenosine levels, thereby providing a functional link between P1 receptors and transporters. (frontiersin.org)
  • The organic anion transporting polypeptides (OATPs) (gene symbol solute carrier family SLCO ) are a superfamily of transmembrane proteins. (aspetjournals.org)
  • substrate
  • They translocate nucleosides in a Na + coupled manner with high affinity and some substrate selectivity, being hCNT1 and hCNT2 pyrimidine- and purine-preferring, respectively, and hCNT3 a broad selectivity transporter. (frontiersin.org)
  • high-affinity
  • In nanodiscs formed with 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine or cholesterol, phosphatidylserine and phosphatidylcholine two low-affinity MPP + binding sites and one high-affinity MPP + binding site per transporter monomer were determined. (aspetjournals.org)
  • The choline high-affinity transporter is not expressed in the human intestine ( 11 ), and there are no established common loss-of-function variants of PMAT. (diabetesjournals.org)
  • sodium
  • Canagliflozin is an oral antihyperglycemic agent used for the treatment of type 2 diabetes mellitus that blocks the reabsorption of glucose in the proximal renal tubule by inhibiting the sodium glucose co transporter 2. (biomedsearch.com)
  • Cadaverine
  • Initially identified as a lysine decomposition product in organic matter, cadaverine, or 1,5-pentanediamine, is found ubiquitously in the environment. (frontiersin.org)
  • Cadaverine is at the nexus of several biochemical pathways (Figure 1 ). (frontiersin.org)
  • interactions
  • In this article, we provide the recommendations of the International Transporter Consortium on these issues, and present decision trees that are intended to help guide clinical studies on the currently recognized most important drug transporter interactions. (nih.gov)
  • molecule
  • Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions (for example, exclusion and inclusion criteria), as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling. (nih.gov)
  • amino
  • The transgenic Arabidopsis overexpressing L - Amino acid Transporter 1 ( LAT1 ) absorbed more Cad and showed increased Cad sensitivity, suggesting that LAT1 functions as a Cad importer. (springer.com)
  • adverse
  • Pharmacogenomics is the study of the contribution of inheritance to variation in drug response-variation that can range from a loss of the desired therapeutic effect at one end of the spectrum to an adverse drug reaction at the other ( 1 , 2 ). (diabetesjournals.org)
  • tyrosine
  • Chronic myeloid leukemia (CML) results from the balanced translocation of c-ABL from chromosome 9 and BCR on chromosome 22 leading to the formation of BCR-ABL1 chimeric oncoprotein, the product of the BCR-ABL1 hybrid gene, with constitutive tyrosine kinase activity ( 1 , 2 ). (aacrjournals.org)