نتایج جستجو برای: hent1

تعداد نتایج: 154  

2013
Amir Avan Francesco Crea Elisa Paolicchi Niccola Funel Victor E Marquez Richard J. Honeywell Romano Danesi Godefridus J. Peters Elisa Giovannetti

Pancreatic ductal adenocarcinoma (PDAC) is characterized by overexpression of Enhancerof Zeste-Homolog-2 (EZH2), which plays a pivotal role in cancer-stem-cell (CSC) selfrenewal through methylation of histone-H3-lysine-27 (H3K27m3). Against this background, EZH2 was identified as an attractive target and we investigated the interaction of the EZH2-inhibitor DZNeP with gemcitabine. EZH2 expressi...

Journal: :International journal of oncology 2015
Wareeporn Wattanawongdon Chariya Hahnvajanawong Nisana Namwat Sirimas Kanchanawat Thidarut Boonmars Patcharee Jearanaikoon Chanwit Leelayuwat Anchalee Techasen Wunchana Seubwai

To establish and characterize the gemcitabine-resistant cholangiocarcinoma (CCA) cell lines, CCA KKU‑M139 and KKU‑M214 cell lines were exposed stepwisely to increasing gemcitabine (GEM). The resultant drug-resistant cell lines, KKU‑M139/GEM and KKU‑M214/GEM, retained the resistant phenotype in drug-free medium at least for 2 months. Sulforhodamine B assay demonstrated that KKU‑M139/GEM and KKU‑...

Journal: :The Journal of pharmacology and experimental therapeutics 2004
James R Hammond Richard G E Archer

Nucleosides such as adenosine, as well as many nucleoside-based drugs, permeate cell membranes via a family of equilibrative nucleoside transporters (ENTs). We assessed the effects of (3-[1-(6,7-diethoxy-2-morpholino-quinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H,3H)-quinazolinedione hydrochloride (KF24345), a novel anti-inflammatory agent that potentiates the actions of adenosine, on the ...

2012
Ozan Kahramanoğullari Gianluca Fantaccini Paola Lecca Daniele Morpurgo Corrado Priami

Gemcitabine (2,2-difluorodeoxycytidine, dFdC) is a prodrug widely used for treating various carcinomas. Gemcitabine exerts its clinical effect by depleting the deoxyribonucleotide pools, and incorporating its triphosphate metabolite (dFdC-TP) into DNA, thereby inhibiting DNA synthesis. This process blocks the cell cycle in the early S phase, eventually resulting in apoptosis. The incorporation ...

Journal: :Molecular cancer therapeutics 2012
Amir Avan Francesco Crea Elisa Paolicchi Niccola Funel Elena Galvani Victor E Marquez Richard J Honeywell Romano Danesi Godefridus J Peters Elisa Giovannetti

Pancreatic ductal adenocarcinoma (PDAC) is characterized by overexpression of enhancer of Zeste homolog-2 (EZH2), which plays a pivotal role in cancer stem cell (CSC) self-renewal through methylation of histone H3 lysine-27 (H3K27me3). Against this background, EZH2 was identified as an attractive target, and we investigated the interaction of the EZH2 inhibitor DZNeP with gemcitabine. EZH2 expr...

Journal: :Molecular pharmacology 2001
T T Lang M Selner J D Young C E Cass

CEM-ARAC leukemia cells with resistance to cytarabine were shown to lack equilibrative transporter (hENT1) expression and activity. Stable transfer of hCNT2 cDNA into CEM-ARAC enabled Na(+)-dependent transport of purine and pyrimidine nucleoside analogs and provided a unique in vitro model for studying hCNT2. Analysis of [(3)H]uridine inhibitory activity by test substances in hCNT2 transfectant...

Journal: :Molecular cancer therapeutics 2008
Stephan A Veltkamp Dick Pluim Maria A J van Eijndhoven Maria J Bolijn Felix H G Ong Rajgopal Govindarajan Jashvant D Unadkat Jos H Beijnen Jan H M Schellens

In a clinical study with oral gemcitabine (2',2'-difluorodeoxycytidine, dFdC), 2',2'-difluorodeoxyuridine (dFdU) was extensively formed and accumulated after multiple oral dosing. Here, we have investigated the in vitro cytotoxicity, cellular uptake, efflux, biotransformation, and nucleic acid incorporation of dFdC and dFdU. Short-term and long-term cytotoxicity assays were used to assess the c...

2015
Marçal Pastor-Anglada Sandra Pérez-Torras

Nucleoside and nucleobase analogs are currently used in the treatment of solid tumors, lymphoproliferative diseases, viral infections such as hepatitis and AIDS, and some inflammatory diseases such as Crohn. Two gene families are implicated in the uptake of nucleosides and nucleoside analogs into cells, SCL28 and SLC29. The former encodes hCNT1, hCNT2, and hCNT3 proteins. They translocate nucle...

2017
Gonzalo Lopez Danielle Braggio Abeba Zewdu Lucia Casadei Kara Batte Hemant Kumar Bid David Koller Peter Yu Obiajulu Hans Iwenofu Anne Strohecker Edwin Choy Dina Lev Raphael Pollock

Leiomyosarcoma (LMS) is a malignant soft tissue sarcoma (STS) with a dismal prognosis following metastatic disease. Chemotherapeutic intervention has demonstrated to have modest clinical efficacy with no curative potential in LMS patients. Previously, we demonstrated pan-HDAC inhibition to have a superior effect in various complex karyotypic sarcomas. In this study, our goal is to evaluate the ...

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