PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 9705281-1 1998 We have recently isolated cDNAs from human placenta and rat jejunum encoding the prototypic human and rat equilibrative nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporters hENT1 and rENT1. 4-nitrobenzylthioinosine 120-142 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 185-190 10366666-3 1999 This uptake was decreased by 70-75% in the presence of 1 microM nitrobenzylthioinosine, a concentration that completely inhibits ENT1, and was completely blocked by the addition of 10 microM dipyridamole, a concentration that inhibits both ENT1 and ENT2. 4-nitrobenzylthioinosine 64-86 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 129-133 10366666-3 1999 This uptake was decreased by 70-75% in the presence of 1 microM nitrobenzylthioinosine, a concentration that completely inhibits ENT1, and was completely blocked by the addition of 10 microM dipyridamole, a concentration that inhibits both ENT1 and ENT2. 4-nitrobenzylthioinosine 64-86 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 240-244 10085223-5 1999 Dilazep and dipyridamole inhibited NBMPR binding to hENT1 with IC50 values of 130+/-10 and 380+/-20 nM respectively. 4-nitrobenzylthioinosine 35-40 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 52-57 10085223-8 1999 5+/-1.6 nM, indicating that the replacement of an Asn residue with Gln decreased the affinity of hENT1 for NBMPR. 4-nitrobenzylthioinosine 107-112 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 97-102 9804860-1 1998 The equilibrative nucleoside transporters (ENTs) are a newly recognized family of membrane proteins of which hENT1 is the nitrobenzylmercaptopurine ribonucleoside (NBMPR)-sensitive (es) and hENT2 the NBMPR-insensitive (ei) transporter of human cells. 4-nitrobenzylthioinosine 164-169 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 109-114 9756942-2 1998 These cells express at least three different nucleoside transport systems as follows: a nitrobenzylthioinosine-sensitive equilibrative transport system of the es-type, which appears to be associated with hENT1 expression, and two Na+-dependent transport systems that may correspond to N1 and to the recently characterized N5-type, which is nitrobenzylthioinosine-sensitive and guanosine-preferring. 4-nitrobenzylthioinosine 88-110 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 204-209 9705281-1 1998 We have recently isolated cDNAs from human placenta and rat jejunum encoding the prototypic human and rat equilibrative nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporters hENT1 and rENT1. 4-nitrobenzylthioinosine 144-149 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 185-190 9705281-3 1998 When expressed in Xenopus oocytes, recombinant hENT1 and rENT1 transport both purine and pyrimidine nucleosides, including adenosine, and are inhibited by nanomolar concentrations of NBMPR. 4-nitrobenzylthioinosine 183-188 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 47-52 9353301-3 1997 When expressed in Xenopus oocytes, hENT1 mediated es-type transport activity and was inhibited by coronary vasoactive drugs (dipyridamole and dilazep) that may compete with nucleosides and NBMPR for binding to the substrate binding site. 4-nitrobenzylthioinosine 189-194 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 35-40 26235575-7 2015 The uptake of these agents was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), an inhibitor of equilibrative nucleoside transporters (ENTs), and was also decreased in cells treated with ENT1 small interfering RNA. 4-nitrobenzylthioinosine 44-75 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 192-196 34503974-6 2021 Remdesivir accumulation decreased in the presence of NBMPR by 30% in ENT1 cells (p = 0.0248) and 27% in ENT2 cells (p = 0.0054). 4-nitrobenzylthioinosine 53-58 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 69-73 34503974-7 2021 EIDD-1931 accumulation decreased in the presence of NBMPR by 77% in ENT1 cells (p = 0.0463 ) and by 64% in ENT2 cells (p = 0.0132), supporting computational predictions that both are ENT substrates which may be important for efficacy against COVID-19. 4-nitrobenzylthioinosine 52-57 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 68-72 32393653-4 2020 Inhibition of [3H]uridine uptake by NBMPR was biphasic, with IC50 values of 11.3 nM for ENT1 and 9.6 muM for ENT2. 4-nitrobenzylthioinosine 36-41 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 88-92 32393653-7 2020 The resulting five-fold difference in intrinsic clearance (Jmax/Kt) for ENT1- and ENT2 transport accounted for observed inhibition of [[3H]uridine uptake by 100 nM NBMPR. 4-nitrobenzylthioinosine 164-169 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 72-76 32313990-10 2020 This transporter may be ENT1 because NBMPR counteracted guanosine cytotoxicity in HuT-78 cells with nanomolar efficacy (IC50 of 25-30 nM). 4-nitrobenzylthioinosine 37-42 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 24-28 32635975-6 2020 Ribavirin uptake was inhibited by nucleosides such as adenosine and uridine, and by inhibitors of equilibrative nucleoside transporter 1 (ENT1) such as S-(4-nitrobenzyl)-6-thioinosine and dipyridamole in a concentration-dependent manner. 4-nitrobenzylthioinosine 152-183 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 98-136 31235912-4 2019 Here, we present crystal structures of hENT1 in complex with two chemically distinct AdoRIs: dilazep and S-(4-nitrobenzyl)-6-thioinosine (NBMPR). 4-nitrobenzylthioinosine 105-136 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 39-44 31235912-4 2019 Here, we present crystal structures of hENT1 in complex with two chemically distinct AdoRIs: dilazep and S-(4-nitrobenzyl)-6-thioinosine (NBMPR). 4-nitrobenzylthioinosine 138-143 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 39-44 28292464-7 2017 RESULTS: Overall adenosine transport (i.e., hENT1+hENT2) was semisaturable and partially inhibited by 1 mumol/L, but abolished by 10 mumol/L NBTI in cells non-treated or treated with NH4Cl. 4-nitrobenzylthioinosine 141-145 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 44-49 27480168-6 2016 N48Q-hENT1 protein is found at the plasma membrane in HEK293 cells but at lower levels compared with wt hENT1 based on S-(4-nitrobenzyl)-6-thioinosine (NBTI) binding analysis (wt 3xFLAG-ENT1 Bmax, 41.5+-2.9 pmol/mg protein; N48Q-3xFLAG-ENT1 Bmax, 13.5+-0.45 pmol/mg protein) and immunofluorescence microscopy. 4-nitrobenzylthioinosine 121-150 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 5-10 27480168-6 2016 N48Q-hENT1 protein is found at the plasma membrane in HEK293 cells but at lower levels compared with wt hENT1 based on S-(4-nitrobenzyl)-6-thioinosine (NBTI) binding analysis (wt 3xFLAG-ENT1 Bmax, 41.5+-2.9 pmol/mg protein; N48Q-3xFLAG-ENT1 Bmax, 13.5+-0.45 pmol/mg protein) and immunofluorescence microscopy. 4-nitrobenzylthioinosine 121-150 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 6-10 27480168-6 2016 N48Q-hENT1 protein is found at the plasma membrane in HEK293 cells but at lower levels compared with wt hENT1 based on S-(4-nitrobenzyl)-6-thioinosine (NBTI) binding analysis (wt 3xFLAG-ENT1 Bmax, 41.5+-2.9 pmol/mg protein; N48Q-3xFLAG-ENT1 Bmax, 13.5+-0.45 pmol/mg protein) and immunofluorescence microscopy. 4-nitrobenzylthioinosine 152-156 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 5-10 27480168-6 2016 N48Q-hENT1 protein is found at the plasma membrane in HEK293 cells but at lower levels compared with wt hENT1 based on S-(4-nitrobenzyl)-6-thioinosine (NBTI) binding analysis (wt 3xFLAG-ENT1 Bmax, 41.5+-2.9 pmol/mg protein; N48Q-3xFLAG-ENT1 Bmax, 13.5+-0.45 pmol/mg protein) and immunofluorescence microscopy. 4-nitrobenzylthioinosine 152-156 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 6-10 33980604-6 2021 The presence of the ENT-specific inhibitor, NBMPR, decreased mizoribine accumulation in ENT1 and ENT2 cells (ENT1, ~70% decrease, p = 0.0046; ENT2, ~50% decrease p = 0.0012). 4-nitrobenzylthioinosine 44-49 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 88-92 33980604-6 2021 The presence of the ENT-specific inhibitor, NBMPR, decreased mizoribine accumulation in ENT1 and ENT2 cells (ENT1, ~70% decrease, p = 0.0046; ENT2, ~50% decrease p = 0.0012). 4-nitrobenzylthioinosine 44-49 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 109-113 33980604-7 2021 NBMPR also decreased ribavirin accumulation in ENT1 and ENT2 cells (ENT1: ~50% decrease p = 0.0498; ENT2: ~30% decrease p = 0.0125). 4-nitrobenzylthioinosine 0-5 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 47-51 33980604-7 2021 NBMPR also decreased ribavirin accumulation in ENT1 and ENT2 cells (ENT1: ~50% decrease p = 0.0498; ENT2: ~30% decrease p = 0.0125). 4-nitrobenzylthioinosine 0-5 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 68-72 33426680-3 2021 Nitrobenzylthioinosine (NBMPR) at 0.1 muM inhibits only ENT1, while dipyridamole at 10 muM or NBMPR at 100 muM inhibits both ENT1 and ENT2. 4-nitrobenzylthioinosine 0-22 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 56-60 33426680-3 2021 Nitrobenzylthioinosine (NBMPR) at 0.1 muM inhibits only ENT1, while dipyridamole at 10 muM or NBMPR at 100 muM inhibits both ENT1 and ENT2. 4-nitrobenzylthioinosine 24-29 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 56-60 33426680-3 2021 Nitrobenzylthioinosine (NBMPR) at 0.1 muM inhibits only ENT1, while dipyridamole at 10 muM or NBMPR at 100 muM inhibits both ENT1 and ENT2. 4-nitrobenzylthioinosine 94-99 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 125-129 33426680-4 2021 We found that uptake of [3 H]uridine, a typical substrate of ENT1 and ENT2, was decreased to approximately 40% by 0.1 muM NBMPR. 4-nitrobenzylthioinosine 122-127 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 61-65 33105674-8 2020 ENT1-mediated uptake of [3H] uridine was linear over 10 min and inhibited by NBMPR with an IC50 value of 1.35 +- 0.37 nM. 4-nitrobenzylthioinosine 77-82 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-4 32858046-6 2020 The tonic activation of adenosine A2 receptors was dependent on the release of intracellular adenosine through equilibrative nucleoside transporters (ENT1/ENT2): NBTI or dipyridamole reduced (~25%) whereas, when ENTs were blocked, adenosine A2 receptor antagonists failed to reduce and A2 agonists increase parasitic burden. 4-nitrobenzylthioinosine 162-166 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 150-154 32339528-6 2020 Although equilibrative nucleoside transporter 1 (ENT1/SLC29A1) and ENT2/SLC29A2 are also known to be able to transport adenine, [3H]adenine uptake in HepG2 cells was not inhibited by the ENT1/2-specific inhibitor of either dipyridamole or nitrobenzylthioinosine. 4-nitrobenzylthioinosine 239-261 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 49-53 32339528-6 2020 Although equilibrative nucleoside transporter 1 (ENT1/SLC29A1) and ENT2/SLC29A2 are also known to be able to transport adenine, [3H]adenine uptake in HepG2 cells was not inhibited by the ENT1/2-specific inhibitor of either dipyridamole or nitrobenzylthioinosine. 4-nitrobenzylthioinosine 239-261 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 54-61 30254099-2 2018 hENT1, which is potently inhibited by nitrobenzylthioinosine (NBMPR), possesses 11 transmembrane helical domains with an intracellular N-terminus and an extracellular C-terminus. 4-nitrobenzylthioinosine 38-60 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 30254099-2 2018 hENT1, which is potently inhibited by nitrobenzylthioinosine (NBMPR), possesses 11 transmembrane helical domains with an intracellular N-terminus and an extracellular C-terminus. 4-nitrobenzylthioinosine 62-67 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 30214194-5 2018 Materials and methods: S-(4-nitrobenzyl)-6-thioinosine was utilized to inhibit the activity of hENT1 and simulate low hENT1 expression. 4-nitrobenzylthioinosine 23-54 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 95-100 30214194-5 2018 Materials and methods: S-(4-nitrobenzyl)-6-thioinosine was utilized to inhibit the activity of hENT1 and simulate low hENT1 expression. 4-nitrobenzylthioinosine 23-54 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 118-123 27995448-6 2017 Adenosine uptake by hENT1 is competitively inhibited by nitrobenzylmercaptopurine ribonucleoside (NBMPR), nucleosides, deoxynucleosides, and nucleoside-derived anti-cancer and anti-viral drugs. 4-nitrobenzylthioinosine 98-103 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 20-25 26235575-7 2015 The uptake of these agents was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), an inhibitor of equilibrative nucleoside transporters (ENTs), and was also decreased in cells treated with ENT1 small interfering RNA. 4-nitrobenzylthioinosine 77-82 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 192-196 22232287-7 2012 It was found that the primary ribavirin transporter in OR6 cells was ENT1 and that inhibition of ENT1-mediated ribavirin uptake by NBMPR significantly attenuated the antiviral activity of the drug as well as its accumulation in OR6 cells. 4-nitrobenzylthioinosine 131-136 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 97-101 23814180-7 2013 Transport assays using [14C]5-azacytidine demonstrated Na+-independent uptake of the drug into the cells, which was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBTI), a hENT1 inhibitor. 4-nitrobenzylthioinosine 129-160 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 171-176 23814180-7 2013 Transport assays using [14C]5-azacytidine demonstrated Na+-independent uptake of the drug into the cells, which was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBTI), a hENT1 inhibitor. 4-nitrobenzylthioinosine 162-166 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 171-176 22837314-2 2012 A previous study from our laboratory established Cys222 in transmembrane (TM) 6 as the residue responsible for methyl methanethiosulfonate (a membrane-permeable sulfhydryl modifier)-mediated enhancement of the binding of the ENT1 inhibitor nitrobenzylmercaptopurine riboside (NBMPR) in intact cells. 4-nitrobenzylthioinosine 276-281 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 225-229 21791574-2 2011 Given that selective ENT1 inhibitors, such as nitrobenzylmercaptopurine riboside (NBMPR), bind to the N-terminal half of the ENT1 protein, we hypothesized that one or more of the four cysteine residues in this region were contributing to the effects of the sulfhydryl modifiers. 4-nitrobenzylthioinosine 82-87 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 21-25 21965724-9 2011 hENT1-specific inhibitor, nitrobenzylthioinosine, significantly abrogated I3C-induced gemcitabine cytotoxicity, further demonstrating its specificity. 4-nitrobenzylthioinosine 26-48 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 21791574-2 2011 Given that selective ENT1 inhibitors, such as nitrobenzylmercaptopurine riboside (NBMPR), bind to the N-terminal half of the ENT1 protein, we hypothesized that one or more of the four cysteine residues in this region were contributing to the effects of the sulfhydryl modifiers. 4-nitrobenzylthioinosine 82-87 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 125-129 21795683-8 2011 Fluxes of hypoxanthine, thymine, and adenine by hENT1 were saturable and inhibited by NBMPR. 4-nitrobenzylthioinosine 86-91 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 48-53 20728214-8 2010 hEPC-3d cells exhibit hENT1-like adenosine transport (NBTI-sensitive, Na(+)-independent), which is absent in hEPC-14d cells. 4-nitrobenzylthioinosine 54-58 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 22-27 21455275-5 2011 Recombinant tandem histidine-affinity (HAT) and 3xFLAG tagged hENT1 was overexpressed in E. coli, affinity purified, and functionally characterized by nitrobenzylthioinosine (NBTI) binding. 4-nitrobenzylthioinosine 151-173 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 62-67 21455275-5 2011 Recombinant tandem histidine-affinity (HAT) and 3xFLAG tagged hENT1 was overexpressed in E. coli, affinity purified, and functionally characterized by nitrobenzylthioinosine (NBTI) binding. 4-nitrobenzylthioinosine 175-179 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 62-67 19788890-3 2010 Capan-2 cells displayed the lowest levels of (1) extracellular nitrobenzylmercaptopurine ribonucleoside (NBMPR) binding, which represents cell-surface hENT1, (2) FLT and gemcitabine uptake during short (1-45s) and prolonged (1h) periods, and (3) gemcitabine sensitivity. 4-nitrobenzylthioinosine 105-110 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 151-156 19788890-4 2010 Exposure to NBMPR (inhibits only hENT1) or dilazep (inhibits hENT1 and hENT2) reduced FLT and gemcitabine uptake and gemcitabine sensitivity, with dilazep having greater effects than NBMPR. 4-nitrobenzylthioinosine 12-17 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 33-38 19788890-4 2010 Exposure to NBMPR (inhibits only hENT1) or dilazep (inhibits hENT1 and hENT2) reduced FLT and gemcitabine uptake and gemcitabine sensitivity, with dilazep having greater effects than NBMPR. 4-nitrobenzylthioinosine 12-17 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 61-66 18462193-1 2008 hENT1 (human equilibrative nucleoside transporter 1) is inhibited by nanomolar concentrations of various structurally distinct coronary vasodilator drugs, including dipyridamole, dilazep, draflazine, soluflazine and NBMPR (nitrobenzylmercaptopurine ribonucleoside). 4-nitrobenzylthioinosine 216-221 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 19091561-0 2009 CoMFA and CoMSIA 3D-QSAR studies on S(6)-(4-nitrobenzyl)mercaptopurine riboside (NBMPR) analogs as inhibitors of human equilibrative nucleoside transporter 1 (hENT1). 4-nitrobenzylthioinosine 81-86 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 119-157 19091561-0 2009 CoMFA and CoMSIA 3D-QSAR studies on S(6)-(4-nitrobenzyl)mercaptopurine riboside (NBMPR) analogs as inhibitors of human equilibrative nucleoside transporter 1 (hENT1). 4-nitrobenzylthioinosine 81-86 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 159-164 18669604-6 2008 [(3)H]FLT uptake in MCF-7, A549, U251, A498, MIA PaCa-2, and Capan-2 cells was inhibited at least 50% by the hENT1 inhibitor nitrobenzylmercaptopurine ribonucleoside (NBMPR). 4-nitrobenzylthioinosine 167-172 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 109-114 20814156-2 2010 The uptake of uridine, an ENT1 substrate, showed saturation kinetics and was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), a specific ENT1 inhibitor, at both 23 degrees C and ICT. 4-nitrobenzylthioinosine 90-121 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 26-30 20814156-2 2010 The uptake of uridine, an ENT1 substrate, showed saturation kinetics and was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), a specific ENT1 inhibitor, at both 23 degrees C and ICT. 4-nitrobenzylthioinosine 90-121 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 142-146 20814156-2 2010 The uptake of uridine, an ENT1 substrate, showed saturation kinetics and was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), a specific ENT1 inhibitor, at both 23 degrees C and ICT. 4-nitrobenzylthioinosine 123-128 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 26-30 20814156-2 2010 The uptake of uridine, an ENT1 substrate, showed saturation kinetics and was inhibited by S-(4-nitrobenzyl)-6-thioinosine (NBMPR), a specific ENT1 inhibitor, at both 23 degrees C and ICT. 4-nitrobenzylthioinosine 123-128 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 142-146 20814156-5 2010 The trans-stimulated uptake of [3H]uridine at ICT was inhibited by ENT1 inhibitors/substrates such as NBMPR, dipyridamole, adenosine, and ribavirin in a concentration-dependent manner. 4-nitrobenzylthioinosine 102-107 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 67-71 19699178-5 2009 Quantification of GFP-hENT1 (mutant and wildtype) protein at the plasma membrane was conducted using nitrobenzylthioinosine (NBTI) binding. 4-nitrobenzylthioinosine 101-123 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 22-27 19699178-5 2009 Quantification of GFP-hENT1 (mutant and wildtype) protein at the plasma membrane was conducted using nitrobenzylthioinosine (NBTI) binding. 4-nitrobenzylthioinosine 125-129 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 22-27 19116148-5 2009 An EGFP-tagged G24R ENT1 displayed plasma membrane localization even though it was unable to bind [3H]-NBMPR, an ENT1-specific inhibitor. 4-nitrobenzylthioinosine 103-108 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 20-24 18462193-1 2008 hENT1 (human equilibrative nucleoside transporter 1) is inhibited by nanomolar concentrations of various structurally distinct coronary vasodilator drugs, including dipyridamole, dilazep, draflazine, soluflazine and NBMPR (nitrobenzylmercaptopurine ribonucleoside). 4-nitrobenzylthioinosine 216-221 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 13-51 18462193-6 2008 Trp29 mutations increased the IC50 values for hENT1 inhibition by dipyridamole, dilazep, NBMPR, soluflazine and draflazine. 4-nitrobenzylthioinosine 89-94 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 46-51 18289860-0 2008 Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity. 4-nitrobenzylthioinosine 12-17 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 84-122 18289860-0 2008 Constrained NBMPR analogue synthesis, pharmacophore mapping and 3D-QSAR modeling of equilibrative nucleoside transporter 1 (ENT1) inhibitory activity. 4-nitrobenzylthioinosine 12-17 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 124-128 18289860-1 2008 Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. 4-nitrobenzylthioinosine 155-160 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 175-214 18289860-1 2008 Conformationally constrained analogue synthesis was undertaken to aid in pharmacophore mapping and 3D-QSAR analysis of nitrobenzylmercaptopurine riboside (NBMPR) congeners as equilibriative nucleoside transporter 1 (ENT1) inhibitors. 4-nitrobenzylthioinosine 155-160 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 216-220 17881236-2 2007 S(6)-(4-nitrobenzyl)mercaptopurine riboside (NBMPR) is a prototype inhibitor of the human equilibrative nucleoside transporter (hENT1), and is a high affinity ligand with a K(d) of 0.1-1.0 nM. 4-nitrobenzylthioinosine 45-50 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 128-133 17881236-5 2007 Structure-activity relationships (SAR) indicate that increasing the steric bulk at the C(2)-purine position of NBMPR led to a decrease in binding affinity of these ligands at the hENT1. 4-nitrobenzylthioinosine 111-116 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 179-184 17409283-6 2007 Equilibrium binding of [(3)H]nitrobenzylmercaptopurine ribonucleoside (NBMPR), a high-affinity inhibitor of hENT1, to brush-border membrane vesicles from cortex confirmed the presence of hENT1 on apical surfaces of proximal tubules. 4-nitrobenzylthioinosine 71-76 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 108-113 17695509-4 2007 A [3H] gemcitabine cellular uptake assay was performed to examine the inhibition of hENT1 by nitrobenzylmercaptoprine ribonucleoside (NBMPR). 4-nitrobenzylthioinosine 134-139 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 84-89 17695509-7 2007 In the PSN1 cells, [3H] gemcitabine uptake via hENT1 was significantly inhibited by NBMPR, and 5-FU sensitivity was significantly increased when the cells were pretreated with NBMPR. 4-nitrobenzylthioinosine 84-89 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 47-52 17379602-2 2007 Human equilibrative nucleoside transporter 1 (hENT1) is inhibited by nanomolar concentrations of structurally diverse compounds, including dipyridamole, dilazep, nitrobenzylmercaptopurine ribonucleoside (NBMPR), draflazine, and soluflazine. 4-nitrobenzylthioinosine 204-209 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 6-44 17379602-2 2007 Human equilibrative nucleoside transporter 1 (hENT1) is inhibited by nanomolar concentrations of structurally diverse compounds, including dipyridamole, dilazep, nitrobenzylmercaptopurine ribonucleoside (NBMPR), draflazine, and soluflazine. 4-nitrobenzylthioinosine 204-209 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 46-51 17167068-7 2007 However, ADP responses were significantly enhanced in the presence of the ENT1 nucleoside transporter inhibitors dipyridamole and NBTI and were significantly inhibited by adenosine deaminase, indicating a role for extracellular adenosine. 4-nitrobenzylthioinosine 130-134 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 74-78 15905191-5 2005 Inhibition of SLC29A1 by nitrobenzylmercaptopurine ribonucleoside (NBMPR) caused a 33% to 45% reduction of TGN in ALL cells in vitro (P < .006), consistent with the gene expression findings. 4-nitrobenzylthioinosine 67-72 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 14-21 16617163-6 2006 During prolonged drug exposures of CEM cells with hENT1 activity, araC was more cytotoxic than TaraC, whereas coexposures with nitrobenzylthioinosine (to pharmacologically block hENT1) yielded identical cytotoxicities for araC and TaraC. 4-nitrobenzylthioinosine 127-149 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 178-183 15634027-1 2005 4-nitrobenzylthioinosine (NBTI, 1) is a well-known inhibitor for the nucleoside transport protein ENT1. 4-nitrobenzylthioinosine 0-24 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 98-102 15634027-1 2005 4-nitrobenzylthioinosine (NBTI, 1) is a well-known inhibitor for the nucleoside transport protein ENT1. 4-nitrobenzylthioinosine 26-30 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 98-102 11814344-11 2002 This is the first identification and characterization of a critical amino acid residue of hENT1 that is important in both nucleoside transporter function and sensitivity to inhibition by NBMPR. 4-nitrobenzylthioinosine 187-192 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 90-95 15481982-1 2004 4-Nitrobenzylthioinosine (NBTI, 1) is a well-known inhibitor for the nucleoside transport protein ENT1. 4-nitrobenzylthioinosine 0-24 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 98-102 15481982-1 2004 4-Nitrobenzylthioinosine (NBTI, 1) is a well-known inhibitor for the nucleoside transport protein ENT1. 4-nitrobenzylthioinosine 26-30 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 98-102 15471562-4 2004 In a highly gemcitabine-sensitive cell line, NCI-H23, the sensitivity to gemcitabine was inhibited by nitrobenzylmercaptopurine ribonucleoside (NBMPR), an inhibitor of hENT1, without significant modulation of hENT1 expression. 4-nitrobenzylthioinosine 144-149 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 168-173 15471562-4 2004 In a highly gemcitabine-sensitive cell line, NCI-H23, the sensitivity to gemcitabine was inhibited by nitrobenzylmercaptopurine ribonucleoside (NBMPR), an inhibitor of hENT1, without significant modulation of hENT1 expression. 4-nitrobenzylthioinosine 144-149 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 209-214 14759222-0 2004 Mutation of leucine-92 selectively reduces the apparent affinity of inosine, guanosine, NBMPR [S6-(4-nitrobenzyl)-mercaptopurine riboside] and dilazep for the human equilibrative nucleoside transporter, hENT1. 4-nitrobenzylthioinosine 88-93 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 203-208 14759222-3 2004 This growth was prevented when inhibitors of hENT1 [e.g. NBMPR [S6-(4-nitrobenzyl)-mercaptopurine riboside], dilazep or dipyridamole] were included in the media. 4-nitrobenzylthioinosine 57-62 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 45-50 14759222-12 2004 We have identified for the first time an amino acid residue (Leu92) of hENT1 that, when mutated, selectively alters the affinity of hENT1 to transport the nucleosides inosine and guanosine and its sensitivity to the inhibitors NBMPR and dilazep. 4-nitrobenzylthioinosine 227-232 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 71-76 14759222-12 2004 We have identified for the first time an amino acid residue (Leu92) of hENT1 that, when mutated, selectively alters the affinity of hENT1 to transport the nucleosides inosine and guanosine and its sensitivity to the inhibitors NBMPR and dilazep. 4-nitrobenzylthioinosine 227-232 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 132-137 15149181-1 2004 A bifunctional biotinylated photoaffinity label for the nitrobenzylmercaptopurine riboside (NBMPR)-sensitive (es) nucleoside transporter (ENT1) has been synthesized and evaluated. 4-nitrobenzylthioinosine 92-97 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 138-142 14607828-8 2004 The mitochondrial toxicity of FIAU to Madin-Darby canine kidney cells was enhanced by hENT1-YFP, even when hENT1 activity on the plasma membrane was selectively blocked by 10 nm nitrobenzylthioinosine. 4-nitrobenzylthioinosine 178-200 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 107-112 12538831-2 2003 These compounds competed with the binding of nitrobenzylthioinosine (NBMPR) to K562 cells, consistent with inhibition of the NBMPR-sensitive equilibrative transporter (ENT1). 4-nitrobenzylthioinosine 45-67 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 168-172 12077112-3 2002 Consistent with the effects of these compounds on the nitrobenzylthioinosine (NBMPR)-sensitive equilibrative nucleoside transporter (ENT1), incubation with SB203580 or SB203580-iodo eliminated the binding of [3H]NBMPR to K562 cells or membranes isolated from human erythrocytes. 4-nitrobenzylthioinosine 54-76 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 133-137 12077112-3 2002 Consistent with the effects of these compounds on the nitrobenzylthioinosine (NBMPR)-sensitive equilibrative nucleoside transporter (ENT1), incubation with SB203580 or SB203580-iodo eliminated the binding of [3H]NBMPR to K562 cells or membranes isolated from human erythrocytes. 4-nitrobenzylthioinosine 78-83 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 133-137 12006583-2 2002 The human (h) and rat (r) equilibrative (Na(+)-independent) nucleoside transporters (ENTs) hENT1, rENT1, hENT2, and rENT2 belong to a family of integral membrane proteins with 11 transmembrane domains (TMs) and are distinguished functionally by differences in sensitivity to inhibition by nitrobenzylthioinosine and coronary vasoactive drugs. 4-nitrobenzylthioinosine 289-311 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 91-96 12062437-2 2002 We show that acute stimulation of protein kinase C (PKC) causes a rapid increase in S-(4-nitrobenzyl)-6-thioinosine-sensitive (human equilibrative nucleoside transporter 1, hENT1) nucleoside uptake, in human cultured cells, which is not due to increased metabolism and which can be blocked by PKC inhibitors. 4-nitrobenzylthioinosine 84-115 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 133-171 12062437-2 2002 We show that acute stimulation of protein kinase C (PKC) causes a rapid increase in S-(4-nitrobenzyl)-6-thioinosine-sensitive (human equilibrative nucleoside transporter 1, hENT1) nucleoside uptake, in human cultured cells, which is not due to increased metabolism and which can be blocked by PKC inhibitors. 4-nitrobenzylthioinosine 84-115 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 173-178 11814344-0 2002 A single glycine mutation in the equilibrative nucleoside transporter gene, hENT1, alters nucleoside transport activity and sensitivity to nitrobenzylthioinosine. 4-nitrobenzylthioinosine 139-161 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 76-81 11814344-1 2002 The human equilibrative nucleoside transporter, hENT1, which is sensitive to inhibition by nitrobenzylthioinosine (NBMPR), is expressed in a wide variety of tissues. 4-nitrobenzylthioinosine 91-113 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 48-53 11814344-1 2002 The human equilibrative nucleoside transporter, hENT1, which is sensitive to inhibition by nitrobenzylthioinosine (NBMPR), is expressed in a wide variety of tissues. 4-nitrobenzylthioinosine 115-120 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 48-53 15037197-0 2004 Glycine 154 of the equilibrative nucleoside transporter, hENT1, is important for nucleoside transport and for conferring sensitivity to the inhibitors nitrobenzylthioinosine, dipyridamole, and dilazep. 4-nitrobenzylthioinosine 151-173 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 57-62 15037197-4 2004 hENT1 and hENT2 differ in their affinity for nucleoside substrates and in their sensitivity to inhibitors, such as nitrobenzylthioinosine (NBMPR). 4-nitrobenzylthioinosine 115-137 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 15037197-4 2004 hENT1 and hENT2 differ in their affinity for nucleoside substrates and in their sensitivity to inhibitors, such as nitrobenzylthioinosine (NBMPR). 4-nitrobenzylthioinosine 139-144 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 0-5 15037197-8 2004 Since NBMPR competitively inhibits nucleoside transporter activity, we hypothesized that G154 may also play a role in the transport of natural nucleosides and in the inhibition by other hENT1 inhibitors, dipyridamole (DP), and dilazep (DZ). 4-nitrobenzylthioinosine 6-11 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 186-191 12820662-5 2003 Whole-cell current measurements showed that application of extracellular nitrobenzylmercaptopurine ribonucleoside (NBMPR), a selective inhibitor of hENT1-mediated transport, had similar effects on whole-cell currents as the application of exogenous adenosine. 4-nitrobenzylthioinosine 115-120 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 148-153 11139404-1 2001 The human and rat equilibrative nucleoside transporter proteins hENT1, rENT1, hENT2 and rENT2 belong to a family of integral membrane proteins with 11 potential transmembrane segments (TMs), and are distinguished functionally by differences in transport of nucleobases and sensitivity to inhibition by nitrobenzylthioinosine (NBMPR) and vasoactive drugs. 4-nitrobenzylthioinosine 302-324 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 64-69 11584005-0 2001 Topology of a human equilibrative, nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporter (hENT1) implicated in the cellular uptake of adenosine and anti-cancer drugs. 4-nitrobenzylthioinosine 35-57 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 100-105 11584005-0 2001 Topology of a human equilibrative, nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporter (hENT1) implicated in the cellular uptake of adenosine and anti-cancer drugs. 4-nitrobenzylthioinosine 59-64 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 100-105 11801546-4 2002 The presence of NBMPR reduced the cytotoxic effects of 5"-deoxy-5-fluorouridine, indicating that hENT1 also enabled cellular uptake of this capecitabine metabolite by breast cancer cells. 4-nitrobenzylthioinosine 16-21 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 97-102 11139404-1 2001 The human and rat equilibrative nucleoside transporter proteins hENT1, rENT1, hENT2 and rENT2 belong to a family of integral membrane proteins with 11 potential transmembrane segments (TMs), and are distinguished functionally by differences in transport of nucleobases and sensitivity to inhibition by nitrobenzylthioinosine (NBMPR) and vasoactive drugs. 4-nitrobenzylthioinosine 326-331 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 64-69 11085929-1 2000 Mammalian cells express at least two subtypes of equilibrative nucleoside transporters, i.e. ENT1 and ENT2, which can be distinguished functionally by their sensitivity and resistance respectively to inhibition by nitrobenzylthioinosine. 4-nitrobenzylthioinosine 214-236 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 93-97 10722669-5 2000 With hENT1 being more sensitive, there is a 7000-fold and 71-fold difference in sensitivity to nitrobenzylthioinosine (NBMPR) (IC(50), 0.4 +/- 0.1 nM versus 2.8 +/- 0.3 microM) and dipyridamole (IC(50), 5.0 +/- 0.9 nM versus 356 +/- 13 nM), respectively. 4-nitrobenzylthioinosine 95-117 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 5-10