| http://purl.uniprot.org/citations/22779445 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/22779445 | http://www.w3.org/2000/01/rdf-schema#comment | "The present study, in general, is aimed to uncover the properties of the transport mechanism or mechanisms responsible for the uptake of NP-647 into Caco-2 cells and, in particular, to understand whether it is a substrate for the intestinal oligopeptide transporter, PEPT1 (SLC15A1). NP-647 showed a carrier-mediated, saturable transport with Michaelis-Menten parameters K(m) = 1.2 mM and V(max) = 2.2 μM/min. The effect of pH, sodium ion (Na(+)), glycylsarcosine and amoxicillin (substrates of PEPT1), and sodium azide (Na(+)/K(+)-ATPase inhibitor) on the flux rate of NP-647 was determined. Molecular docking and molecular dynamics simulation studies were carried out to investigate molecular interactions of NP-647 with transporter using homology model of human PEPT1. The permeability coefficient (P(appCaco-2)) of NP-647 (32.5 × 10(-6) cm/s) was found to be four times higher than that of TRH. Results indicate that NP-647 is transported into Caco-2 cells by means of a carrier-mediated, proton-dependent mechanism that is inhibited by Gly-Sar and amoxicillin. In turn, NP-647 also inhibits the uptake of Gly-Sar into Caco-2 cells and, together, this evidence suggests that PEPT1 is involved in the process. Docking and molecular dynamics simulation studies indicate high affinity of NP-647 toward PEPT1 binding site as compared to TRH. High permeability of NP-647 over TRH is attributed to its increased hydrophobicity which increases its affinity toward PEPT1 by interacting with the hydrophobic pocket of the transporter through hydrophobic forces."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.org/dc/terms/identifier | "doi:10.1021/mp200672d"xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Jain R."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Shaikh N."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Bansal A.K."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Tikoo K."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Bagul P."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Khomane K.S."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Meena C.L."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Nandekar P.P."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Pawar Y.B."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Sangamwar A.T."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/author | "Wahlang B."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/date | "2012"xsd:gYear |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/name | "Mol Pharm"xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/pages | "2458-2468"xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/title | "Mechanistic insights into PEPT1-mediated transport of a novel antiepileptic, NP-647."xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://purl.uniprot.org/core/volume | "9"xsd:string |
| http://purl.uniprot.org/citations/22779445 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/22779445 |
| http://purl.uniprot.org/citations/22779445 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/22779445 |
| http://purl.uniprot.org/uniprot/#_B2CQT6-mappedCitation-22779445 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/22779445 |
| http://purl.uniprot.org/uniprot/#_P46059-mappedCitation-22779445 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/22779445 |
| http://purl.uniprot.org/uniprot/#_Q4VAL9-mappedCitation-22779445 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/22779445 |
| http://purl.uniprot.org/uniprot/#_O14496-mappedCitation-22779445 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/22779445 |