PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 18094991-0 2008 hPEPT1 is responsible for uptake and transport of Gly-Sar in the human bronchial airway epithelial cell-line Calu-3. Glycine 50-53 solute carrier family 15 member 1 Homo sapiens 0-6 18094991-10 2008 Surprisingly, the results indicate that Gly-Sar uptake and transport in Calu-3 cells are hPEPT1-mediated rather than hPEPT2-mediated. Glycine 40-43 solute carrier family 15 member 1 Homo sapiens 89-95 17554807-8 2007 These results indicate that Gly-Pro-Hyp can be partially hydrolyzed by the brush-border membrane-bound aminopeptidase N to remove Gly, and that the resulting Pro-Hyp is, in part, transported into the small intestinal epithelial cells via the H+-coupled PEPT1. Glycine 28-31 solute carrier family 15 member 1 Homo sapiens 253-258 18336632-7 2008 Ethanol reduced maximal transport capacity (I(max)) of hPepT1 for Gly-Sar without affecting Gly-Sar binding affinity (K(0.5) and Hill coefficient). Glycine 66-69 solute carrier family 15 member 1 Homo sapiens 55-61 17944948-4 2007 Bip-Pro inhibited the [(14)C]Gly-Sar uptake via PEPT1 and PEPT2 with exceptional high affinity (K(i) = 24 microm and 3.4 microm, respectively) in a competitive manner. Glycine 29-32 solute carrier family 15 member 1 Homo sapiens 48-53 17407174-7 2007 The affinity of the tripeptides to hPEPT1 was determined by measuring the inhibition of [(14)C]Gly-Sar in mature Caco-2 cell monolayers which resulted in K(i) values ranging from 0.22 to 25 mM or above. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 35-41 17407174-8 2007 Translocation through the intestinal membrane, mediated by hPEPT1, was measured by recording the membrane potential relative to that induced by the known substrate Gly-Sar. Glycine 164-167 solute carrier family 15 member 1 Homo sapiens 59-65 17009102-5 2007 RESULTS: The reverse-charge mutants R282D-hPepT1 and D341R-hPepT1 showed significantly reduced gly-sar uptake, but the double mutant (R282D/D341R-hPepT1) has functionality comparable to that of wild-type hPepT1. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 42-48 17009102-5 2007 RESULTS: The reverse-charge mutants R282D-hPepT1 and D341R-hPepT1 showed significantly reduced gly-sar uptake, but the double mutant (R282D/D341R-hPepT1) has functionality comparable to that of wild-type hPepT1. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 59-65 17009102-5 2007 RESULTS: The reverse-charge mutants R282D-hPepT1 and D341R-hPepT1 showed significantly reduced gly-sar uptake, but the double mutant (R282D/D341R-hPepT1) has functionality comparable to that of wild-type hPepT1. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 59-65 17009102-5 2007 RESULTS: The reverse-charge mutants R282D-hPepT1 and D341R-hPepT1 showed significantly reduced gly-sar uptake, but the double mutant (R282D/D341R-hPepT1) has functionality comparable to that of wild-type hPepT1. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 59-65 17009102-6 2007 Gly-sar uptake by R282C-hPepT1 is reduced, but pre-incubation with 1 mM MTSET, a positively charged cysteine-modifying reagent, restored function to wild-type levels. Glycine 0-3 solute carrier family 15 member 1 Homo sapiens 24-30 17009102-7 2007 Similarly, pre-incubation of D341C-hPepT1 with 10 mM MTSES, a negatively charged cysteine-modifying reagent, increased gly-sar uptake compared to unmodified D341C-hPepT1. Glycine 119-122 solute carrier family 15 member 1 Homo sapiens 35-41 17009102-8 2007 In contrast, MTSET modification of D341C-hPepT1 (giving a positive charge at position 341) resulted in significant reduction in gly-sar uptake, compared to D341C-hPepT1. Glycine 128-131 solute carrier family 15 member 1 Homo sapiens 41-47 16651734-13 2006 The pH-profile of the transport activity in CHO/hPEPT1 cells treated with DEPC in the presence of 10 mM Gly-Sar also showed a bell-shape similar to that in non-treated CHO/hPEPT1 cells. Glycine 104-107 solute carrier family 15 member 1 Homo sapiens 48-54 16713701-7 2006 However, affinity for and transepithelial transport via hPEPT1 were only seen for Gly-Sar-Sar, AsnPsi[CONCH(3)]PhePsi[CONCH(3)]Trp, and Gly-Sar-Leu. Glycine 82-85 solute carrier family 15 member 1 Homo sapiens 56-62 16713701-7 2006 However, affinity for and transepithelial transport via hPEPT1 were only seen for Gly-Sar-Sar, AsnPsi[CONCH(3)]PhePsi[CONCH(3)]Trp, and Gly-Sar-Leu. Glycine 136-139 solute carrier family 15 member 1 Homo sapiens 56-62 16627568-6 2006 Gly-Sar and the drugs also modified the kinetics of hPEPT1 presteady-state charge movement, by causing a reduction in maximum charge (Qmax) and a shift of the midpoint voltage (V0.5) to more negative potentials. Glycine 0-3 solute carrier family 15 member 1 Homo sapiens 52-58 16627568-8 2006 Based on steady-state and presteady-state analysis of Gly-Sar and cefadroxil transport, we proposed an extension of the 6-state kinetic model for hPEPT1 function that globally accounts for the observed presteady-state and steady-state kinetics of neutral dipeptide and drug transport. Glycine 54-57 solute carrier family 15 member 1 Homo sapiens 146-152 16651734-13 2006 The pH-profile of the transport activity in CHO/hPEPT1 cells treated with DEPC in the presence of 10 mM Gly-Sar also showed a bell-shape similar to that in non-treated CHO/hPEPT1 cells. Glycine 104-107 solute carrier family 15 member 1 Homo sapiens 172-178 16568107-5 2006 In addition, hPepT1 activity was likely to be coupled to a Na+/H+ exchanger, as evidenced by the fact that [14C]Gly-Sar uptake was not affected by the absence of Na+ when cells were incubated at low pH (5.2). Glycine 112-115 solute carrier family 15 member 1 Homo sapiens 13-19 16328452-5 2006 Uptake of the PepT1 substrate glycylsarcosine [(3)H]-Gly-Sar was studied in vitro in the human colon carcinoma cell line Caco2/bbe monolayers as well as in vivo in mice injected with cytokines. Glycine 53-56 solute carrier family 15 member 1 Homo sapiens 14-19 16283203-7 2006 Moreover, PEPT1 mRNA level was positively related to the activity of [(14)C]Gly-Sar uptake (r=0.55). Glycine 76-79 solute carrier family 15 member 1 Homo sapiens 10-15 16283203-9 2006 With this improved model, Gly-Sar transport in clones 1 and 9 was well-predicted, suggesting that our model can simulate Gly-Sar transport in cells expressing PEPT1 at different levels. Glycine 26-29 solute carrier family 15 member 1 Homo sapiens 159-164 16283203-9 2006 With this improved model, Gly-Sar transport in clones 1 and 9 was well-predicted, suggesting that our model can simulate Gly-Sar transport in cells expressing PEPT1 at different levels. Glycine 121-124 solute carrier family 15 member 1 Homo sapiens 159-164 14661916-7 2003 Also, Lys-FITC-OCH3 (100 microM) uptake in HeLa/hPept1 and Caco-2 cells was reduced by 77% and 80%, respectively, in the presence of 1 mM Gly-Sar. Glycine 138-141 solute carrier family 15 member 1 Homo sapiens 48-54 15623827-5 2005 Exposure to 1-5 mmol/L H(2)O(2) for 24 h caused a dose-dependent decrease in Gly-Sar transport, which was associated with decreased PepT1 transport velocity (V(max)). Glycine 77-80 solute carrier family 15 member 1 Homo sapiens 132-137 15521010-11 2004 Cells overexpressing hPepT1 showed increased Gly-Sar and MDP uptake, whereas decreased uptake was observed after hPepT1 siRNA-inhibition. Glycine 45-48 solute carrier family 15 member 1 Homo sapiens 21-27 14725353-7 2003 RESULTS: At pH 6.0, H57K-, H57R-, H121K-, and H121R-hPepT1 led to a 97%, 90%, 45%, and 75% decrease in [3H]Gly-Sar uptake into HEK293 cells, respectively. Glycine 107-110 solute carrier family 15 member 1 Homo sapiens 52-58 14725353-9 2003 In oocytes expressing H57R-hPepT1, steady-state currents induced by 5 mM Gly-Sar increased with increasing pH (I(max) = 300 nA at pH 8.5), suggesting the binding of protons to H57R. Glycine 73-76 solute carrier family 15 member 1 Homo sapiens 27-33 14725353-11 2003 CONCLUSIONS: H57R-hPepT1 is able to bind protons at a relatively basic pH, resulting in facilitation of transport of Gly-Sar by hPepT1 at higher pH. Glycine 117-120 solute carrier family 15 member 1 Homo sapiens 18-24 14725353-11 2003 CONCLUSIONS: H57R-hPepT1 is able to bind protons at a relatively basic pH, resulting in facilitation of transport of Gly-Sar by hPepT1 at higher pH. Glycine 117-120 solute carrier family 15 member 1 Homo sapiens 128-134 15340850-6 2004 Using the kinetic parameters of PEPT1 and the basolateral peptide transporter, a computational model of Gly-Sar transport in Caco-2 cells was constructed. Glycine 104-107 solute carrier family 15 member 1 Homo sapiens 32-37 15981923-3 2004 In this study, it was first verified that monkey intestine transports a model dipeptide, Gly-Sar, in a proton-dependent manner (0.30 +/- 0.05 pmol cm(-2) s(-1) at pH 6.0 and 0.10 +/- 0.03 pmol cm(-2) s(-1) at pH 7.4) in the absorptive direction, presumably by monkey PEPT1. Glycine 89-92 solute carrier family 15 member 1 Homo sapiens 267-272 15981923-7 2004 Functional comparison of human and monkey peptide transporters expressed in HeLa cells suggested that functionalities of PEPT1 and PEPT2 were largely conserved in terms of Gly-Sar uptake kinetics and inhibitor specificity (for most tested substrates). Glycine 172-175 solute carrier family 15 member 1 Homo sapiens 121-126 15832510-6 2004 The [14C]Gly-Sar uptake in the transfected cells was sodium-independent and pH-dependent, demonstrating enhanced uptake, the rate of which increased significantly from the weakly to strongly expressing hPepT1 MDCK/hPepT1 -V5&His clones as compared to the mock cell line at pH 6.0. Glycine 9-12 solute carrier family 15 member 1 Homo sapiens 202-208 15832510-6 2004 The [14C]Gly-Sar uptake in the transfected cells was sodium-independent and pH-dependent, demonstrating enhanced uptake, the rate of which increased significantly from the weakly to strongly expressing hPepT1 MDCK/hPepT1 -V5&His clones as compared to the mock cell line at pH 6.0. Glycine 9-12 solute carrier family 15 member 1 Homo sapiens 214-220 14532279-3 2003 Out of the remaining 19 transporters, three (F293C-, L296C-, and F297C-hPepT1) showed negligible glycyl-sarcosine (gly-sar) uptake activity and may play an important role in defining the overall hPepT1 structure. Glycine 97-100 solute carrier family 15 member 1 Homo sapiens 71-77 14532279-8 2003 MTSET modification of R282C-hPepT1 resulted in a significant increase in gly-sar uptake. Glycine 73-76 solute carrier family 15 member 1 Homo sapiens 28-34 14661916-5 2003 RESULTS: In HeLa/hPept1 cells, [3H]Gly-Sar uptake was significantly inhibited by Lys-FITC-OCH3 (74%) but not by FITC-Val-OCH3 (22%). Glycine 35-38 solute carrier family 15 member 1 Homo sapiens 17-23 10561591-1 1999 To elucidate the decisive structural factors relevant for dipeptide-carrier interaction, the affinity of short amide and imide derivatives for the intestinal H+/peptide symporter (PEPT1) was investigated by measuring their ability to inhibit Gly-Sar transport in Caco-2 cells. Glycine 242-245 solute carrier family 15 member 1 Homo sapiens 180-185 12788085-7 2003 Y167C-, N171C-, and S174C-hPepT1 showed </=25% Gly-Sar uptake when compared with WT-hPepT1. Glycine 50-53 solute carrier family 15 member 1 Homo sapiens 26-32 11459451-4 2001 The affinities of these conjugates were estimated by their inhibition of the accumulation rate of Gly-Sar, a well-established substrate for PEPT1. Glycine 98-101 solute carrier family 15 member 1 Homo sapiens 140-145 12009949-3 2002 The Gly-Sar uptake via hPEPT1 was significantly inhibited in the polyrotaxane conjugates, and this inhibitory effect was not explained by the sum of interaction between hPEPT1 and alpha-CD-Val-Lys conjugates. Glycine 4-7 solute carrier family 15 member 1 Homo sapiens 23-29 11741253-3 2001 The hPepT1-GFP fusion construct was then transfected into Caco-2 and HeLa cells, and drug inhibition was studied by inhibiting 3H-Gly-Sar uptake. Glycine 130-133 solute carrier family 15 member 1 Homo sapiens 4-10 9893960-4 1999 Kinetic analysis and effects of addition either of uncoupler (protonophore) or by Gly-Sar, one of the good substrates of PEPT1, revealed that fluorescent dipeptides were taken up by passive diffusion. Glycine 82-85 solute carrier family 15 member 1 Homo sapiens 121-126 10213369-7 1999 RESULTS: The utility of the CHO-PEPT1 cell model was demonstrated by determining the uptake kinetics of Gly-Sar, a prototypical dipeptide transporter substrate. Glycine 104-107 solute carrier family 15 member 1 Homo sapiens 32-37 11741208-12 1999 Transport characteristics of Gly-Sar from the basolateral to the apical side in adenovirus-transduced Caco-2 cells are in agreement with those from the apical to the basolateral side, indicating that hPepT1 is also expressed in the basolateral membrane and displays a similar level of transport enhancement after adenovirus mediated hPepT1 gene expression. Glycine 29-32 solute carrier family 15 member 1 Homo sapiens 200-206 9092716-7 1997 Again, Gly-Sar uptake mediated by the human PEPT 1 and PEPT 2 in HeLa cells was found to be inhibited by the anionic cephalosporins with the same order potency as in Caco-2 and SKPT cells. Glycine 7-10 solute carrier family 15 member 1 Homo sapiens 44-50 9735340-4 1998 [3H]Gly-sar uptake in cells transiently transfected with Y167A-hPepT1 was abolished completely, even though the level of Y167A-hPepT1 expression by Western blot analysis and cell surface expression by immunofluorescence microscopy was similar to those of the wild type. Glycine 4-7 solute carrier family 15 member 1 Homo sapiens 63-69 32341465-8 2020 Farnesoid X receptor (FXR) inhibitor glycine-beta-muricholic acid or FXR knockdown reversed the downregulation of PepT1 expression by CDCA and GW4064 (another FXR agonist). Glycine 37-44 solute carrier family 15 member 1 Homo sapiens 114-119 22842481-5 2012 VPY transport and anti-inflammatory activity in Caco-2 cells was reduced in the presence of Gly-Sar, indicating this activity was mediated by PepT1. Glycine 92-95 solute carrier family 15 member 1 Homo sapiens 142-147 27719884-7 2017 BBPs were the main peptidases involved in the PepT1 transport and the maximum hydrolysis rate was 11.4muM Gly/min. Glycine 106-109 solute carrier family 15 member 1 Homo sapiens 46-51 27547863-5 2016 Transport uptake of Glycylsarcosine (Gly-sar) by the hPepT1-N562Q variant, but not by other single mutants, was moderately impaired. Glycine 20-23 solute carrier family 15 member 1 Homo sapiens 53-59 27547863-8 2016 Kinetic studies indicated that the Vmax values for Gly-sar transport by low activity mutants were decreased compared to those of wild-type, which suggested that the cell surface expression and/or turnover rate of hPepT1 mutants was impaired; Km values were unchanged in most cases. Glycine 51-54 solute carrier family 15 member 1 Homo sapiens 213-219 25178856-4 2014 Inhibition experiments were carried out using Gly-Sar, a typical PepT1 substrate, to confirm the PepT1-mediated transport mechanism of TRH analogs. Glycine 46-49 solute carrier family 15 member 1 Homo sapiens 65-70 25178856-4 2014 Inhibition experiments were carried out using Gly-Sar, a typical PepT1 substrate, to confirm the PepT1-mediated transport mechanism of TRH analogs. Glycine 46-49 solute carrier family 15 member 1 Homo sapiens 97-102 29580877-15 2018 This approach allowed the successful confirmation of the binding of Gly-Sar at the mM range and revealed for the first time the KD of the antiviral prodrug valacyclovir to the PepT1 homolog at around 50 muM. Glycine 68-71 solute carrier family 15 member 1 Homo sapiens 176-181 26924013-6 2016 Cell experiments also showed that the designed tripeptide and Gly-Sar were transported across Caco-2 cell via PepT1, whereas the tetra- and pentapeptides were transported through the paracellular tight-junction pathway. Glycine 62-65 solute carrier family 15 member 1 Homo sapiens 110-115 25178856-7 2014 Further, the significant inhibition of the uptake of Gly-Sar by TRH analogs confirmed the PepT1-mediated transport mechanism. Glycine 53-56 solute carrier family 15 member 1 Homo sapiens 90-95 23962042-9 2013 The uptake of the hSGLT1 substrate [(14)C]-alpha-methyl-D-glycopyranoside and the hPepT1 substrate [(14)C]-Gly-Sar in Caco-2 cells was also decreased in the presence of 0.3 mM sertraline. Glycine 107-110 solute carrier family 15 member 1 Homo sapiens 82-88 22779445-7 2012 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. Glycine 44-47 solute carrier family 15 member 1 Homo sapiens 113-118 21280612-4 2011 The uptake of glycylsarcosine (Gly-Sar, a typical substrate of PepT1) by Caco-2 cells could be inhibited by compound 4a in a concentration-dependent manner. Glycine 31-34 solute carrier family 15 member 1 Homo sapiens 63-68 21529830-8 2011 K(m), V(max), and % gly-sar transported by PepT1 were calculated and compared. Glycine 20-23 solute carrier family 15 member 1 Homo sapiens 43-48 21529830-9 2011 RESULTS: K(m), V(max), and % gly-sar transported by PepT1 varied from 0.7 to 2.4 mM, 8.4 to 21.0 nmol/mg protein/10 min, and 69% to 87%, respectively. Glycine 29-32 solute carrier family 15 member 1 Homo sapiens 52-57 21703856-5 2011 The six investigated compounds were all defined as high affinity ligands (K(i)-values <0.5 mM) for hPEPT1 by measuring the concentration dependent inhibition of apical [(14)C]Gly-Sar uptake in Caco-2 cells. Glycine 178-181 solute carrier family 15 member 1 Homo sapiens 102-108 21262302-6 2011 And JBP485 uptake was also significantly inhibited by glycylsarcosine (Gly-Sar, a typical substrate for PEPT1 transporters), JBP923 (a derivative of JBP485), and cephalexin (CEX, a beta-lactam antibiotic and a known substrate of PEPT1) in Caco-2 cells. Glycine 71-74 solute carrier family 15 member 1 Homo sapiens 104-109 22369721-6 2012 The Michaelis-Menten constant (K(m)) values of Gly-Sar uptake by the hPEPT1 and hPEPT2-expressing transfectants were 1.03 mM and 0.0965 mM, respectively, and the K(m) values of JBP485 uptake were 1.33 mM for PEPT1 and 0.144 mM for PEPT2. Glycine 47-50 solute carrier family 15 member 1 Homo sapiens 69-75 22369721-6 2012 The Michaelis-Menten constant (K(m)) values of Gly-Sar uptake by the hPEPT1 and hPEPT2-expressing transfectants were 1.03 mM and 0.0965 mM, respectively, and the K(m) values of JBP485 uptake were 1.33 mM for PEPT1 and 0.144 mM for PEPT2. Glycine 47-50 solute carrier family 15 member 1 Homo sapiens 70-75 22369721-8 2012 Maximal uptake of Gly-Sar were detected at pH 5.8 (for PEPT1) and pH 6.5 (for PEPT2), suggesting that both HeLa-hPEPT1 and HeLa-hPEPT2 were H(+) dependent transporters. Glycine 18-21 solute carrier family 15 member 1 Homo sapiens 55-60 22369721-8 2012 Maximal uptake of Gly-Sar were detected at pH 5.8 (for PEPT1) and pH 6.5 (for PEPT2), suggesting that both HeLa-hPEPT1 and HeLa-hPEPT2 were H(+) dependent transporters. Glycine 18-21 solute carrier family 15 member 1 Homo sapiens 112-118 22369721-9 2012 Stably transfected HeLa-hPEPT1/HeLa-hPEPT2 cells were constructed successfully, and the functions of hPEPT1/hPEPT2 were identified using their substrates, JBP485 and Gly-Sar. Glycine 166-169 solute carrier family 15 member 1 Homo sapiens 101-107 20449699-8 2010 Affinities for hPEPT1 of relevant tripeptides were determined by competition studies with [14C]Gly-Sar in MDCK/hPEPT1 cells. Glycine 95-98 solute carrier family 15 member 1 Homo sapiens 15-21 20726987-6 2010 KEY RESULTS: Ibuprofen concentration dependently inhibited hPEPT1-mediated uptake of Gly-Sar in MDCK/hPEPT1 cells (K(i)(app) = 0.4 mM) but uptake of ibuprofen in Caco-2 cells and MDCK/hPEPT1 cells was not inhibited by hPEPT1 substrates. Glycine 85-88 solute carrier family 15 member 1 Homo sapiens 59-65 20726987-6 2010 KEY RESULTS: Ibuprofen concentration dependently inhibited hPEPT1-mediated uptake of Gly-Sar in MDCK/hPEPT1 cells (K(i)(app) = 0.4 mM) but uptake of ibuprofen in Caco-2 cells and MDCK/hPEPT1 cells was not inhibited by hPEPT1 substrates. Glycine 85-88 solute carrier family 15 member 1 Homo sapiens 101-107 20726987-6 2010 KEY RESULTS: Ibuprofen concentration dependently inhibited hPEPT1-mediated uptake of Gly-Sar in MDCK/hPEPT1 cells (K(i)(app) = 0.4 mM) but uptake of ibuprofen in Caco-2 cells and MDCK/hPEPT1 cells was not inhibited by hPEPT1 substrates. Glycine 85-88 solute carrier family 15 member 1 Homo sapiens 101-107 20726987-6 2010 KEY RESULTS: Ibuprofen concentration dependently inhibited hPEPT1-mediated uptake of Gly-Sar in MDCK/hPEPT1 cells (K(i)(app) = 0.4 mM) but uptake of ibuprofen in Caco-2 cells and MDCK/hPEPT1 cells was not inhibited by hPEPT1 substrates. Glycine 85-88 solute carrier family 15 member 1 Homo sapiens 101-107 21147219-6 2011 The K(i)-values of H-X(aa)-Ser-OH dipeptides for hPEPT1 in MDCK/hPEPT1 cells ranged from 0.14 mM (logIC(50)=-0.85 +- 0.06) for H-Tyr-Ser-OH to 0.89 mM (logIC(50)=-0.09 +- 0.02) for H-Gly-Ser-OH, as measured in a competition assay with [(14)C]Gly-Sar. Glycine 183-186 solute carrier family 15 member 1 Homo sapiens 49-55 20929265-5 2010 2a-d did not induce inward currents, indicating that they are not transported, but the stereoisomers with an L-configuration at the N-terminal valine (2a and 2b) potently inhibited transport of the hPEPT1 substrate glycylsarcosine (Gly-Sar). Glycine 232-235 solute carrier family 15 member 1 Homo sapiens 198-204 20558765-6 2010 We found that uptake of glycine-sarcosine, a specific substrate of PepT1, in intestinal epithelial Caco2-BBE cells was inhibited by Tri-DAP in a dose-dependent manner. Glycine 24-31 solute carrier family 15 member 1 Homo sapiens 67-72 20307658-3 2010 Growth of AsPC-1 cells was inhibited by these two peptides and a typical PEPT1/SLC15A1 substrate Gly-Sar. Glycine 97-100 solute carrier family 15 member 1 Homo sapiens 73-78 20307658-3 2010 Growth of AsPC-1 cells was inhibited by these two peptides and a typical PEPT1/SLC15A1 substrate Gly-Sar. Glycine 97-100 solute carrier family 15 member 1 Homo sapiens 79-86 19685173-5 2009 RESULTS: E595C- and G594C-hPEPT1 showed negligible Gly-Sar uptake. Glycine 51-54 solute carrier family 15 member 1 Homo sapiens 26-32 20128809-6 2010 KEY RESULTS: ALA inhibited SLC36A1-mediated L-[(3)H]Pro and SLC15A1-mediated [(14)C]Gly-Sar uptake in Caco-2 cell monolayers with IC(50) values of 11.3 and 2.1 mM respectively. Glycine 84-87 solute carrier family 15 member 1 Homo sapiens 60-67 27713232-2 2009 The [14C]Gly-Sar uptake via PEPT1 was inhibited by Zn2+ and Cu2+ treatment in a concentration-dependent manner (Ki values 107 +- 23 and 19 +- 5 muM, respectively). Glycine 9-12 solute carrier family 15 member 1 Homo sapiens 28-33 27713232-3 2009 Kinetic analysis showed that the Kt of Gly-Sar uptake was increased 2-fold in the presence of zinc sulphate (150 muM) whereas the Vmax value were not affected suggesting that zinc ions inhibited Gly-Sar uptake by PEPT1 in a competitively manner. Glycine 39-42 solute carrier family 15 member 1 Homo sapiens 213-218 19201665-5 2009 The validated method was successfully employed in the study of Gly-Sar uptake inhibition in Caco-2 cells by valcytarabine, a potential substrate of the peptide transporter 1 (PEPT1). Glycine 63-66 solute carrier family 15 member 1 Homo sapiens 152-173 18781650-6 2009 Ser(Reb)-Gly exhibited significantly increased uptake by PEPT1-expressing cells in comparison with that by mock cells. Glycine 9-12 solute carrier family 15 member 1 Homo sapiens 57-62 18781650-7 2009 The permeability of Ser(Reb)-Gly across a Caco-2 cell monolayer was significantly higher than that of rebamipide itself, and the transport was decreased in the presence of PEPT1 substrates. Glycine 29-32 solute carrier family 15 member 1 Homo sapiens 172-177 19201665-5 2009 The validated method was successfully employed in the study of Gly-Sar uptake inhibition in Caco-2 cells by valcytarabine, a potential substrate of the peptide transporter 1 (PEPT1). Glycine 63-66 solute carrier family 15 member 1 Homo sapiens 175-180 18782614-6 2008 MDR1 and PepT1 function was investigated using talinolol and Gly-Sar transport, respectively. Glycine 61-64 solute carrier family 15 member 1 Homo sapiens 9-14 18782614-12 2008 PepT1 mRNA levels showed significant correlation to the uptake ratio and net active uptake of Gly-Sar. Glycine 94-97 solute carrier family 15 member 1 Homo sapiens 0-5 19115956-5 2009 Glycylsarcosine (gly-sar, a typical substrate of PepT1) uptake by Caco-2 cells can be inhibited by 2 in a concentration-dependent manner, and IC(50) for 2 was 2.18 +/- 0.12 mM. Glycine 17-20 solute carrier family 15 member 1 Homo sapiens 49-54