Page last updated: 2024-08-18

thiophenes and azd3965

thiophenes has been researched along with azd3965 in 29 studies

Research

Studies (29)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's15 (51.72)24.3611
2020's14 (48.28)2.80

Authors

AuthorsStudies
Bishop, PW; Blackhall, F; Critchlow, SE; Dive, C; Fusi, A; Hodgkinson, CL; Kelly, P; Morrow, CJ; Nonaka, D; Polański, R; Priest, L; Smith, PD; Trapani, F; White, A1
Blount, KG; Bola, BM; Chadwick, AL; Critchlow, SE; Michopoulos, F; Smith, PD; Stratford, IJ; Telfer, BA; Williams, KJ1
Cummings, J; Dive, C; Kershaw, S; Morris, K; Tugwood, J1
Alavi, M; Bagryanova, L; Behbahan, IS; Braas, D; Chia, D; Christofk, HR; Critchlow, SE; Dubinett, SM; Espindola Camacho, C; Gardner, BK; Goodglick, L; Graeber, TG; Graham, NA; Gu, W; Hong, CS; Horvath, S; Hurvitz, SA; Krotee, PAL; Kurdistani, SK; Mah, V; Maresh, EL; Mellinghoff, IK1
Liu, Y; Shi, M; Wang, C; Wen, Z; Xie, J; Xue, Y; Zhang, S; Zhao, L; Zhao, Y1
Bacon, CM; Bell, N; Blair, H; Bomken, S; Critchlow, SE; Crossland, R; Keun, HC; Long, A; Miwa, S; Nakjang, S; Noble, RA; Phillips, N; Rand, V; Sikka, A; Televantou, D; Thomas, H; Wedge, SR1
Arunan, V; Beloueche-Babari, M; Casals Galobart, T; Chung, YL; Eykyn, TR; Koniordou, M; Leach, MO; Parkes, HG; Smith, PD; Wantuch, S1
Guan, X; Morris, ME; Ruszaj, D1
Eichner, R; Girardi, E; Hashimoto, M; Superti-Furga, G1
Boyers, A; Chadwick, A; Critchlow, SE; Mehibel, M; Mueller-Klieser, W; Ortiz-Martinez, F; Stratford, IJ; Telfer, BA; Voelxen, N; West, CM; Williams, KJ1
Behrends, V; Bravo-Santano, N; Giskeødegård, GF; Keun, HC; Letek, M1
Guan, X; Morris, ME; Rodriguez-Cruz, V1
Afonso, J; Baltazar, F; Longatto-Filho, A; Marques, H; Pinheiro, C; Pinto, T; Schmitt, F; Simões-Sousa, S1
Bailey, TL; McDonald, PH; Nieto, A1
Guan, X; Morris, ME2
Beloueche-Babari, M; Casals Galobart, T; Delgado-Goni, T; Harker, JA; Leach, MO; Parkes, HG; Tandy, D; Wantuch, S1
Bacon, C; Bowron, A; Greystoke, A; Halford, S; Jenkinson, F; Keun, H; Leech, N; McNeillis, R; Petrides, G; Plummer, R; Siskos, A; Walton, J1
Juvale, K; Puri, S1
Allen, AE; Grant, C; Greenwood, K; Lucas, RJ; Martin, EA; Redfern, WS; Vince, P1
Jiang, X; Lei, J; Wang, N; Xu, H; Yan, C; Yuan, Y; Zhang, S; Zhu, A1
Benes, CH; Boikos, SA; Calbert, ML; Dalton, KM; Dozmorov, M; Egan, RK; Faber, AC; Floros, KV; Glod, J; Greninger, P; Hu, B; Koblinski, J; Kurupi, R; Lochmann, TL; McClanaghan, J; Murchie, E; Puchalapalli, M; Ramamoorthy, S; Shock, L; Stein, GT1
Eliopoulos, E; Papakonstantinou, E; Thireou, T; Vlachakis, D; Vlachoyiannopoulos, PG1
Ademi, H; Chaachouay, H; Gassmann, M; Gerst, D; Gorr, TA; Shinde, DA; Vogel, J1
Li, J; Li, W; Na, N; Ouyang, J; Zhang, S; Zhang, Y1
Bergthaler, A; Bigenzahn, JW; César-Razquin, A; Kartnig, F; Kornauth, C; Lercher, A; Pemovska, T; Srndic, I; Staber, PB; Superti-Furga, G; Valent, P1
Afonso, J; Antunes, B; Baltazar, F; Batista, A; Pinto-Ribeiro, F; Silva, A1
Bailey, T; McDonald, P; Nieto, A1
Bacon, CM; Banerji, U; Chénard-Poirier, M; Dragoni, I; Greystoke, A; Halford, S; Heinzmann, K; Howell, EC; Innes, WA; Keun, HC; Morris, K; Payne, GS; Petrides, G; Plummer, C; Plummer, R; Potter, S; Rata, M; Salisbury, BM; Sloan, P; Veal, GJ; Wedge, SR1

Reviews

2 review(s) available for thiophenes and azd3965

ArticleYear
Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights.
    European journal of medicinal chemistry, 2020, Aug-01, Volume: 199

    Topics: Antineoplastic Agents; Drug Resistance, Neoplasm; Humans; Monocarboxylic Acid Transporters; Muscle Proteins; Neoplasms; Pyrimidinones; Structure-Activity Relationship; Symporters; Thiophenes; Uracil

2020
In Vivo Anticancer Activity of AZD3965: A Systematic Review.
    Molecules (Basel, Switzerland), 2021, Dec-29, Volume: 27, Issue:1

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Disease Management; Disease Progression; Drug Evaluation, Preclinical; Energy Metabolism; Glycolysis; Humans; Lactic Acid; Monocarboxylic Acid Transporters; Neoplasms; Pyrimidinones; Signal Transduction; Symporters; Thiophenes; Tumor Microenvironment; Warburg Effect, Oncologic; Xenograft Model Antitumor Assays

2021

Trials

1 trial(s) available for thiophenes and azd3965

ArticleYear
A Phase I Dose-escalation Study of AZD3965, an Oral Monocarboxylate Transporter 1 Inhibitor, in Patients with Advanced Cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2023, 04-14, Volume: 29, Issue:8

    Topics: Antineoplastic Agents; Dose-Response Relationship, Drug; Humans; Maximum Tolerated Dose; Neoplasms; Pyrimidinones; Thiophenes

2023

Other Studies

26 other study(ies) available for thiophenes and azd3965

ArticleYear
Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2014, Feb-15, Volume: 20, Issue:4

    Topics: Adult; Aged; Aged, 80 and over; Animals; Antineoplastic Agents; Cell Death; Cell Line, Tumor; Drug Resistance, Neoplasm; Female; Humans; Inhibitory Concentration 50; Kaplan-Meier Estimate; Lactic Acid; Lung Neoplasms; Male; Mice; Mice, Inbred NOD; Mice, SCID; Middle Aged; Monocarboxylic Acid Transporters; Multivariate Analysis; Muscle Proteins; Pyrimidinones; Small Cell Lung Carcinoma; Symporters; Thiophenes; Xenograft Model Antitumor Assays

2014
Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport.
    Molecular cancer therapeutics, 2014, Volume: 13, Issue:12

    Topics: Animals; Biological Transport; Cell Line, Tumor; Cluster Analysis; Disease Models, Animal; Female; Glycolysis; Humans; Lactates; Metabolomics; Monocarboxylic Acid Transporters; Neoplasms; Oxidative Stress; Pyrimidinones; Radiation Tolerance; Symporters; Thiophenes; Tumor Burden; Xenograft Model Antitumor Assays

2014
Optimisation of immunofluorescence methods to determine MCT1 and MCT4 expression in circulating tumour cells.
    BMC cancer, 2015, May-10, Volume: 15

    Topics: Antineoplastic Agents; Cell Line, Tumor; Clinical Trials, Phase I as Topic; Fluorescent Antibody Technique; Healthy Volunteers; Humans; Monocarboxylic Acid Transporters; Muscle Proteins; Neoplastic Cells, Circulating; Pyrimidinones; Small Cell Lung Carcinoma; Symporters; Thiophenes

2015
MCT1 Modulates Cancer Cell Pyruvate Export and Growth of Tumors that Co-express MCT1 and MCT4.
    Cell reports, 2016, Feb-23, Volume: 14, Issue:7

    Topics: Animals; Antineoplastic Agents; Biological Transport; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Citric Acid Cycle; Epithelial Cells; Female; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Glycolysis; Humans; Lung Neoplasms; Mice; Monocarboxylic Acid Transporters; Muscle Proteins; Oxidative Phosphorylation; Pyrimidinones; Pyruvic Acid; Signal Transduction; Symporters; Thiophenes; Tumor Burden; Xenograft Model Antitumor Assays

2016
MACC1 mediates chemotherapy sensitivity of 5-FU and cisplatin via regulating MCT1 expression in gastric cancer.
    Biochemical and biophysical research communications, 2017, 04-08, Volume: 485, Issue:3

    Topics: Antineoplastic Agents; Blotting, Western; Cell Line, Tumor; Cell Survival; Cisplatin; Female; Fluorouracil; Gene Expression Regulation, Neoplastic; Humans; Kaplan-Meier Estimate; Male; Middle Aged; Monocarboxylic Acid Transporters; Multivariate Analysis; Prognosis; Pyrimidinones; Reverse Transcriptase Polymerase Chain Reaction; RNA Interference; Stomach Neoplasms; Symporters; Thiophenes; Trans-Activators; Transcription Factors

2017
Inhibition of monocarboxyate transporter 1 by AZD3965 as a novel therapeutic approach for diffuse large B-cell lymphoma and Burkitt lymphoma.
    Haematologica, 2017, Volume: 102, Issue:7

    Topics: Antineoplastic Agents; Biomarkers; Burkitt Lymphoma; Cell Death; Cell Line, Tumor; Drug Resistance, Neoplasm; Electron Transport Complex I; Energy Metabolism; Humans; Lactic Acid; Lymphoma, Large B-Cell, Diffuse; Mitochondria; Monocarboxylic Acid Transporters; Muscle Proteins; Oxidative Phosphorylation; Pyrimidinones; Symporters; Thiophenes

2017
MCT1 Inhibitor AZD3965 Increases Mitochondrial Metabolism, Facilitating Combination Therapy and Noninvasive Magnetic Resonance Spectroscopy.
    Cancer research, 2017, 11-01, Volume: 77, Issue:21

    Topics: Acrylates; Animals; Antineoplastic Combined Chemotherapy Protocols; Blotting, Western; Cell Line, Tumor; Energy Metabolism; Female; HT29 Cells; Humans; Lactic Acid; Lymphoma; Magnetic Resonance Spectroscopy; Metformin; Mice, SCID; Mitochondria; Monocarboxylic Acid Transporters; Muscle Proteins; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays

2017
Development and validation of a liquid chromatography tandem mass spectrometry assay for AZD3965 in mouse plasma and tumor tissue: Application to pharmacokinetic and breast tumor xenograft studies.
    Journal of pharmaceutical and biomedical analysis, 2018, Jun-05, Volume: 155

    Topics: Acetonitriles; Animals; Atmospheric Pressure; Breast Neoplasms; Cell Line, Tumor; Chromatography, Liquid; Female; Heterografts; Mice; Plasma; Pyrimidines; Pyrimidinones; Reproducibility of Results; Tandem Mass Spectrometry; Thiophenes; Uracil

2018
Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay.
    ACS chemical biology, 2018, 06-15, Volume: 13, Issue:6

    Topics: Biological Assay; Excitatory Amino Acid Transporter 2; Formates; Glutamate Plasma Membrane Transport Proteins; Heating; HEK293 Cells; Humans; Lactic Acid; Ligands; Monocarboxylic Acid Transporters; Protein Binding; Protein Stability; Pyrimidinones; Thiophenes; Uracil

2018
Statin-induced metabolic reprogramming in head and neck cancer: a biomarker for targeting monocarboxylate transporters.
    Scientific reports, 2018, 11-14, Volume: 8, Issue:1

    Topics: Animals; Biomarkers; Head and Neck Neoplasms; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Lactic Acid; Mice; Monocarboxylic Acid Transporters; Oxidative Phosphorylation; Precision Medicine; Prognosis; Pyrimidinones; Thiophenes

2018
Acetaminophen cytotoxicity in HepG2 cells is associated with a decoupling of glycolysis from the TCA cycle, loss of NADPH production, and suppression of anabolism.
    Archives of toxicology, 2019, Volume: 93, Issue:2

    Topics: Acetaminophen; Cell Survival; Citric Acid Cycle; Drug Synergism; Glutathione; Glycolysis; Hep G2 Cells; Humans; Lactates; Metabolism; Monocarboxylic Acid Transporters; NADP; Pyrimidinones; Symporters; Thiophenes; Toxicity Tests

2019
Cellular Uptake of MCT1 Inhibitors AR-C155858 and AZD3965 and Their Effects on MCT-Mediated Transport of L-Lactate in Murine 4T1 Breast Tumor Cancer Cells.
    The AAPS journal, 2019, 01-07, Volume: 21, Issue:2

    Topics: Animals; Breast Neoplasms; Cell Line, Tumor; Coumaric Acids; Drug Screening Assays, Antitumor; Female; Humans; Hydrogen-Ion Concentration; Lactic Acid; Mice; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Uracil

2019
Clinical significance of metabolism-related biomarkers in non-Hodgkin lymphoma - MCT1 as potential target in diffuse large B cell lymphoma.
    Cellular oncology (Dordrecht), 2019, Volume: 42, Issue:3

    Topics: Adult; Aged; Aged, 80 and over; Biomarkers, Tumor; Cell Line, Tumor; Cell Survival; Female; Glycolysis; Humans; Kaplan-Meier Estimate; Lymphoma, Large B-Cell, Diffuse; Lymphoma, Non-Hodgkin; Male; Middle Aged; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Young Adult

2019
A Nonradioactive High-Throughput Screening-Compatible Cell-Based Assay to Identify Inhibitors of the Monocarboxylate Transporter Protein 1.
    Assay and drug development technologies, 2019, Volume: 17, Issue:6

    Topics: Animals; Cell Survival; Cells, Cultured; HEK293 Cells; High-Throughput Screening Assays; Humans; Mice; Molecular Structure; Monocarboxylic Acid Transporters; Pyrimidinones; Pyruvates; Symporters; Thiophenes

2019
Pharmacokinetics of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Mice: Potential Enterohepatic Circulation and Target-Mediated Disposition.
    Pharmaceutical research, 2019, Dec-10, Volume: 37, Issue:1

    Topics: Administration, Oral; Animals; Chromatography, High Pressure Liquid; Delayed-Action Preparations; Drug Delivery Systems; Enterohepatic Circulation; Female; Glucuronides; Humans; Mice; Mice, Inbred BALB C; Pyrimidinones; Tandem Mass Spectrometry; Thiophenes; Tissue Distribution

2019
Monocarboxylate transporter 1 blockade with AZD3965 inhibits lipid biosynthesis and increases tumour immune cell infiltration.
    British journal of cancer, 2020, Volume: 122, Issue:6

    Topics: Animals; Cell Culture Techniques; Cell Line; Cell Line, Tumor; Disease Models, Animal; Female; Humans; Lipid Metabolism; Mice; Monocarboxylic Acid Transporters; Pyrimidinones; Thiophenes

2020
A case of malignant hyperlactaemic acidosis appearing upon treatment with the mono-carboxylase transporter 1 inhibitor AZD3965.
    British journal of cancer, 2020, Volume: 122, Issue:8

    Topics: Acidosis, Lactic; Humans; Hyperlactatemia; Male; Melanoma; Middle Aged; Monocarboxylic Acid Transporters; Positron-Emission Tomography; Pyrimidinones; Symporters; Thiophenes

2020
In Vitro and In Vivo Efficacy of AZD3965 and Alpha-Cyano-4-Hydroxycinnamic Acid in the Murine 4T1 Breast Tumor Model.
    The AAPS journal, 2020, 06-11, Volume: 22, Issue:4

    Topics: Animals; Breast Neoplasms; Cell Line, Tumor; Coumaric Acids; Dose-Response Relationship, Drug; Female; Lung Neoplasms; Mice; Mice, Inbred BALB C; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes; Treatment Outcome; Tumor Burden; Xenograft Model Antitumor Assays

2020
Effects of a monocarboxylate transport 1 inhibitor, AZD3965, on retinal and visual function in the rat.
    British journal of pharmacology, 2020, Volume: 177, Issue:20

    Topics: Animals; Electroretinography; Pyrimidinones; Rats; Rats, Long-Evans; Rats, Wistar; Retina; Thiophenes

2020
Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates.
    Cell, 2021, 01-21, Volume: 184, Issue:2

    Topics: Amino Acid Sequence; Animals; Antineoplastic Agents; Basigin; Binding Sites; Cryoelectron Microscopy; Humans; Ligands; Models, Molecular; Monocarboxylic Acid Transporters; Mutant Proteins; Protons; Pyrimidinones; Rats; Structural Homology, Protein; Substrate Specificity; Symporters; Thiophenes

2021
Catastrophic ATP loss underlies a metabolic combination therapy tailored for
    Proceedings of the National Academy of Sciences of the United States of America, 2021, 03-30, Volume: 118, Issue:13

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Basigin; Cell Line, Tumor; Cell Proliferation; Electron Transport Complex I; Gene Amplification; Humans; Mice; Mitochondria; Monocarboxylic Acid Transporters; N-Myc Proto-Oncogene Protein; Neuroblastoma; Phenformin; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays

2021
A Holistic Evolutionary and 3D Pharmacophore Modelling Study Provides Insights into the Metabolism, Function, and Substrate Selectivity of the Human Monocarboxylate Transporter 4 (hMCT4).
    International journal of molecular sciences, 2021, Mar-13, Volume: 22, Issue:6

    Topics: Animals; Antineoplastic Agents; Binding Sites; Biological Transport; Drug Design; Glycolysis; Humans; Lactic Acid; Molecular Docking Simulation; Monocarboxylic Acid Transporters; Muscle Proteins; Phloretin; Phylogeny; Protein Binding; Protein Conformation, alpha-Helical; Protein Interaction Domains and Motifs; Protein Isoforms; Pyrimidinones; Quercetin; Reserpine; Structural Homology, Protein; Substrate Specificity; Thiophenes; Uracil

2021
Targeting neovascularization and respiration of tumor grafts grown on chick embryo chorioallantoic membranes.
    PloS one, 2021, Volume: 16, Issue:5

    Topics: Angiogenesis Inhibitors; Animals; Cell Line, Tumor; Chick Embryo; Chorioallantoic Membrane; Dogs; Humans; Mice; Monocarboxylic Acid Transporters; Neoplasm Proteins; Neoplasms, Experimental; Neovascularization, Pathologic; Oxygen Consumption; Pyrimidinones; Symporters; Thiophenes; Xenograft Model Antitumor Assays

2021
Multifunctional Spiky Topological Nanocapsules for the Discrimination and Differential Inhibition of Inflammation and Cancer.
    ACS applied materials & interfaces, 2021, Jun-09, Volume: 13, Issue:22

    Topics: Animals; Apoptosis; Carcinoma, Hepatocellular; Cell Movement; Cell Proliferation; Drug Liberation; Female; Humans; Inflammation; Liver Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; MicroRNAs; Monocarboxylic Acid Transporters; Nanocapsules; Pyrimidinones; Symporters; Thiophenes; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2021
Metabolic drug survey highlights cancer cell dependencies and vulnerabilities.
    Nature communications, 2021, 12-14, Volume: 12, Issue:1

    Topics: Biomarkers, Tumor; Cell Survival; Cluster Analysis; Fatty Acids; Genotype; Humans; Leukemia, Myeloid; Monocarboxylic Acid Transporters; Phenotype; Phosphatidylinositol 3-Kinase; Phosphoinositide-3 Kinase Inhibitors; Pyrimidinones; Pyrrolidines; Signal Transduction; Small Molecule Libraries; Symporters; Systems Analysis; Thiophenes; Triazoles; Tumor Cells, Cultured

2021
Inhibition of the Monocarboxylate Transporter 1 (MCT1) Promotes 3T3-L1 Adipocyte Proliferation and Enhances Insulin Sensitivity.
    International journal of molecular sciences, 2022, Feb-08, Volume: 23, Issue:3

    Topics: 3T3-L1 Cells; Adipocytes; Animals; CDC2 Protein Kinase; Cell Cycle; Cell Proliferation; Down-Regulation; Glucose; Insulin Resistance; Mice; Models, Biological; Monocarboxylic Acid Transporters; Pyrimidinones; Symporters; Thiophenes

2022