Compounds > pyrazines
Page last updated: 2024-08-21

pyrazines and vx-970

pyrazines has been researched along with vx-970 in 39 studies

Research

Studies (39)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's24 (61.54)24.3611
2020's15 (38.46)2.80

Authors

AuthorsStudies
Brunner, TB; Charlton, PA; Cornelissen, B; Fokas, E; Gillies McKenna, W; Hammond, EM; Muschel, RJ; Olcina, MM; Pollard, JR; Prevo, R; Reaper, PM; Vallis, KA1
Boucher, DM; Charlton, P; Charrier, JD; Eustace, B; Furey, B; Golec, J; Gu, Y; Hall, AB; Hare, B; Johnson, MA; Milton, S; Murphy, CE; Newsome, D; Pollard, JR; Reaper, PM; Takemoto, D; Tolman, C; Wang, Y; Wood, M1
Foote, KM; Lau, A; Nissink, JW1
Massey, AJ1
Biskup, E; Gniadecki, R; Naym, DG1
Gershon, TR; Hwang, D; Kabanov, AV; Lang, PY; Nanjangud, GJ; Parker, JS; Shaw, C; Sokolsky-Papkov, M1
Boumelha, AJ; Dobrynin, G; Hammond, EM; Hawkins, MA; Ient, J; Leslie, RE; Leszczynska, KB; Maughan, T; Mukherjee, S; Senra, JM1
Bakkenist, CJ; Beumer, JH; Chu, E; Doyle, A; Iffland, A; Ivy, P; Kiesel, BF; Parise, RA; Scemama, J; Villaruz, L1
Houghton, PJ; Kang, M; Kurmashev, D; Kurmasheva, RT; Reynolds, CP; Smith, MA; Wu, J1
Beleggia, F; Büttner, R; Doerr, F; George, J; Hermann, S; Persigehl, T; Rehkämper, T; Reinhardt, HC; Schmitt, A; Thomas, RK; Walter, V; Weber, JP; Wittersheim, M1
Ding, C; Hao, Y; Liu, M; Qin, Z; Rao, Q; Song, L; Tian, Y; Wang, HW; Wang, J; Wu, Z; Xu, Y1
Frangou, E; Hawkins, M; Holmes, J; Love, S; McGregor, N1
Chen, KN; Dai, L; Dong, B; Fu, H; Kang, XZ; Liang, Z; Shen, LY; Shi, Q; Xiong, HC; Yan, WP; Yang, YB1
Fernandez-Capetillo, O; Lecona, E1
Bindra, RS; Chen, EM; Focarete, ML; Jackson, C; Jiang, Z; Josowitz, AD; Merlettini, A; Noorbakhsh, S; Quijano, AR; Saltzman, WM; Seo, YE; Sundaram, RK1
Boughey, JC; Goetz, MP; Harmsen, WS; Kahila, MM; Kalari, KR; Lou, Z; Mutter, RW; Sarkaria, JN; Tu, X; Wang, L; Yu, J; Yuan, J; Zhou, Q1
Badura, J; Becker, H; Fahrer, J; Heylmann, D; Kaina, B1
Bartfeld, S; Chan, AKW; Chan, AS; Chan, ASY; Chan, D; Cheng, PSW; Clevers, H; Fan, X; Ho, SL; Kwong, DLW; Lam, KO; Law, S; Lee, BCH; Leung, SY; Ma, S; Mak, TW; Man, AHY; Shi, J; Siu, HC; Tsui, WY; Wong, JWH; Yan, HHN; Yue, SSK; Yuen, ST; Zhang, J1
Chiba, T; Kurian, S; Li, S; Song, Y; Wang, Z; Wu, X; Xiang, R1
Aben, N; Avelar, AT; Berns, A; Cozijnsen, M; de Vries, H; Nagel, R; Proost, N; van de Ven, M; van der Vliet, J; Wessels, LFA1
Andrade, AF; Beijersbergen, RL; Bonnefoy, N; Combès, E; Coquel, F; Coquelle, A; Del Rio, M; Desigaud, D; Garambois, V; Gongora, C; Jarlier, M; Martineau, P; Michaud, HA; Moreaux, J; Pasero, P; Tosi, D; Vezzio-Vie, N1
Li, X; Qi, W; Sun, L; Wang, C; Wang, M; Xu, X; Zhao, D1
Charrier, JD; Davis, C; Durrant, S; Golec, J; Griffiths, M; Kay, D; Knegtel, R; Littlewood, P; MacCormick, S; O'Donnell, M; Pinder, J; Pollard, J; Reaper, P; Storck, P; Twin, H; Virani, A; Young, S1
Bindra, RS; Breslin, H; Burgenske, DM; Ganesa, S; Gilad, O; Jackson, CB; Jia, L; Kalathil, AN; Noorbakhsh, SI; Sarkaria, JN; Sundaram, RK1
Andrs, M; Gorecki, L; Korabecny, J; Rezacova, M1
Algéo, MP; Chaire, V; Italiano, A; Laroche-Clary, A; Le Loarer, F; Malykh, A; Verbeke, S1
Distel, L; Dobler, C; Fietkau, R; Hecht, M; Jost, T1
Falk, M; Hendriks, BS; Jansen, M; Terranova, N1
Arumugaswami, V; Bakowski, MA; Bartenschlager, R; Beck, S; Betz, UAK; Beutler, N; Chatterjee, AK; Damoiseaux, RD; Gabriel, G; Garcia, G; Gomperts, B; Han, B; Kim, H; Kirkpatrick, MG; Kohn, DB; Parcells, MS; Purbey, PK; Purkayastha, A; Ramaiah, A; Riva, L; Rogers, TF; Scumpia, P; Sen, C; Sharma, A; Svendsen, CN; Ulmert, D; Wolff, KC; Yuen, C1
Aladjem, MI; Beck, E; Ceribelli, M; Chen, L; Dahmen, H; Desai, P; Elenbaas, B; Figg, WD; Itkin, Z; Khan, J; Kim, S; Kindrick, JD; Klumpp-Thomas, C; Lee, MJ; Lee, S; McKnight, C; Michael, S; Nichols, S; Peer, CJ; Pommier, Y; Puc, J; Rajapakse, VN; Redon, CE; Schultz, CW; Sciuto, L; Shimellis, H; Steinberg, SM; Sun, Y; Takahashi, N; Thomas, A; Thomas, CJ; Travers, J; Trepel, JB; Varonin, J; Wei, JS; Wilson, KM; Yuno, A; Zenke, FT; Zhang, X; Zhang, Y; Zimmermann, A1
Elloumi, F; Jo, U; Kim, SH; Murai, Y; Pommier, Y; Rajapakse, VN; Saha, LK; Schultz, CW; Senatorov, IS; Takahashi, N; Thomas, A; Zenke, FT; Zimmermann, A1
Bürkel, F; Distel, LV; Faulhaber, EM; Fietkau, R; Hecht, M; Jost, T; Scheper, J; Symank, J1
Abel, L; Baschnagel, AM; Clark, PA; Elnaggar, JH; Kaushik, S; Kimple, RJ; Kromke, AC; Leal, TA; Longhurst, CA; Nickel, KP; Skiba, JH; VanBeek, HJ; Zhao, SG1
Cui, Y; Dreicer, R; Emamekhoo, H; Frankel, PH; Hoimes, C; Kim, WY; Lara, PN; Lyou, Y; Michaelson, D; Milowsky, M; Mortazavi, A; Newman, E; Pal, SK; Parikh, M; Parikh, R; Srinivas, S; Teply, B; Vaishampayan, U; Weng, P; Zhang, T1
Fu, F; Geng, Z; Hu, L; Huang, Q; Li, X; Liu, S; Liu, X; Song, Q; Wang, H; Yin, Q; Zhu, Y1
Cheng, SC; Chowdhury, D; Curtis, J; D'Andrea, AD; da Costa, AABA; Färkkilä, A; Gulhan, D; Hendrickson, AEW; Kochupurakkal, B; Kohn, EC; Kolin, DL; Konstantinopoulos, PA; Lee, EK; Liu, JF; Matulonis, UA; Polak, M; Shapiro, GI; Stover, EH; Tayob, N1
Bindra, RS; Burgenske, DM; Dragojevic, S; Elmquist, WF; Gupta, SK; Kim, M; Mohammad, AS; Sarkaria, JN; Talele, S; Zhang, W1
Classe, JM; Ferron, G; Floquet, A; Freyer, G; Hardy-Bessard, AC; Kurtz, JE; Lécuru, F; Motte-Rouge, T; Pautier, P1
Li, C; Liu, B; Liu, C; Ma, L; Qin, W; Qiu, H; Tu, J; Wang, X; Yuan, X; Zhao, W1

Reviews

4 review(s) available for pyrazines and vx-970

ArticleYear
Drugging ATR: progress in the development of specific inhibitors for the treatment of cancer.
    Future medicinal chemistry, 2015, Volume: 7, Issue:7

    Topics: Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; DNA Damage; Humans; Isoxazoles; Molecular Conformation; Neoplasms; Pyrazines

2015
Targeting ATR in cancer.
    Nature reviews. Cancer, 2018, Volume: 18, Issue:9

    Topics: Ataxia Telangiectasia Mutated Proteins; DNA Damage; Drug Development; Genomic Instability; Humans; Indoles; Isoxazoles; Molecular Targeted Therapy; Morpholines; Neoplasms; Nitroso Compounds; Oxazines; Protein Kinase Inhibitors; Pyrazines; Pyrimidines; Quinolines; Sulfonamides; Sulfoxides

2018
Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy.
    Pharmacology & therapeutics, 2020, Volume: 210

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Drug Discovery; Drug Synergism; Humans; Isoxazoles; Molecular Targeted Therapy; Neoplasms; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Sulfones; Treatment Outcome

2020
Prise en charge médicale de la récidive du cancer épithélial de l'ovaire: Medical management of recurrent epithelial ovarian cancer.
    Bulletin du cancer, 2021, Volume: 108, Issue:9S1

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Immunological; Antineoplastic Combined Chemotherapy Protocols; Azepines; Bevacizumab; Carcinoma, Ovarian Epithelial; Female; Genes, BRCA1; Genes, BRCA2; Humans; Immunoconjugates; Immunotherapy; Isoxazoles; Maintenance Chemotherapy; Maytansine; Neoplasm Recurrence, Local; Ovarian Neoplasms; Platinum Compounds; Poly(ADP-ribose) Polymerase Inhibitors; Pteridines; Pyrazines; Pyrimidines

2021

Trials

3 trial(s) available for pyrazines and vx-970

ArticleYear
Population pharmacokinetics of ATR inhibitor berzosertib in phase I studies for different cancer types.
    Cancer chemotherapy and pharmacology, 2021, Volume: 87, Issue:2

    Topics: Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Dose-Response Relationship, Drug; Female; Humans; Infusions, Intravenous; Inhibitory Concentration 50; Isoxazoles; Male; Middle Aged; Models, Biological; Neoplasms; Protein Kinase Inhibitors; Pyrazines

2021
Effect of Cisplatin and Gemcitabine With or Without Berzosertib in Patients With Advanced Urothelial Carcinoma: A Phase 2 Randomized Clinical Trial.
    JAMA oncology, 2021, Oct-01, Volume: 7, Issue:10

    Topics: Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Transitional Cell; Cisplatin; Deoxycytidine; Gemcitabine; Humans; Isoxazoles; Male; Pyrazines; Treatment Outcome; Urinary Bladder Neoplasms

2021
A Replication stress biomarker is associated with response to gemcitabine versus combined gemcitabine and ATR inhibitor therapy in ovarian cancer.
    Nature communications, 2021, 09-22, Volume: 12, Issue:1

    Topics: Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Biomarkers, Tumor; Deoxycytidine; DNA Replication; Female; Gemcitabine; Humans; Isoxazoles; Mutation; Oncogenes; Ovarian Neoplasms; Progression-Free Survival; Protein Kinase Inhibitors; Pyrazines; Recombinational DNA Repair; Retinoblastoma Binding Proteins

2021

Other Studies

32 other study(ies) available for pyrazines and vx-970

ArticleYear
Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation.
    Cell death & disease, 2012, Dec-06, Volume: 3

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; DNA Damage; Female; Humans; Isoxazoles; Mice; Mice, Inbred BALB C; Pancreatic Neoplasms; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; Pyrazines; Radiation Tolerance; Radiation-Sensitizing Agents

2012
Potentiation of tumor responses to DNA damaging therapy by the selective ATR inhibitor VX-970.
    Oncotarget, 2014, Jul-30, Volume: 5, Issue:14

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Cisplatin; DNA; DNA Damage; Drug Synergism; Female; Humans; Isoxazoles; Mice; Mice, SCID; Phosphorylation; Protein Kinase Inhibitors; Pyrazines; Random Allocation; Signal Transduction; Xenograft Model Antitumor Assays

2014
Inhibition of ATR-dependent feedback activation of Chk1 sensitises cancer cells to Chk1 inhibitor monotherapy.
    Cancer letters, 2016, 12-01, Volume: 383, Issue:1

    Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Bone Neoplasms; Cell Proliferation; Checkpoint Kinase 1; Colorectal Neoplasms; DNA Damage; DNA-Activated Protein Kinase; Dose-Response Relationship, Drug; Histones; HT29 Cells; Humans; Indoles; Isoxazoles; Molecular Targeted Therapy; Nuclear Proteins; Osteosarcoma; Protein Kinase Inhibitors; Pyrazines; Pyridones; Signal Transduction; Time Factors

2016
Small-molecule inhibitors of Ataxia Telangiectasia and Rad3 related kinase (ATR) sensitize lymphoma cells to UVA radiation.
    Journal of dermatological science, 2016, Volume: 84, Issue:3

    Topics: Ataxia Telangiectasia Mutated Proteins; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cell Survival; Checkpoint Kinase 1; Flow Cytometry; Histones; Humans; Isoxazoles; Lymphoma, T-Cell, Cutaneous; Phosphorylation; Photochemotherapy; Photosensitizing Agents; Pyrazines; Quinolines; Quinuclidines; RNA, Small Interfering; Sulfones; Tumor Cells, Cultured; Ultraviolet Rays

2016
ATR maintains chromosomal integrity during postnatal cerebellar neurogenesis and is required for medulloblastoma formation.
    Development (Cambridge, England), 2016, 11-01, Volume: 143, Issue:21

    Topics: Animals; Animals, Newborn; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Transformation, Neoplastic; Cerebellar Neoplasms; Cerebellum; Chromosomal Instability; Developmental Disabilities; Female; Gene Deletion; Gene Expression Regulation, Developmental; Gene Expression Regulation, Neoplastic; Isoxazoles; Male; Medulloblastoma; Mice; Mice, Inbred C57BL; Mice, Knockout; Nervous System Malformations; Neurogenesis; Neurons; Pyrazines

2016
Preclinical testing of an Atr inhibitor demonstrates improved response to standard therapies for esophageal cancer.
    Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, 2016, Volume: 121, Issue:2

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Chemoradiotherapy; Esophageal Neoplasms; Humans; Isoxazoles; Mice; Pyrazines

2016
LC-MS/MS assay for the quantitation of the ATR kinase inhibitor VX-970 in human plasma.
    Journal of pharmaceutical and biomedical analysis, 2017, Nov-30, Volume: 146

    Topics: Ataxia Telangiectasia Mutated Proteins; Biological Assay; Chromatography, Liquid; Formates; Humans; Isoxazoles; Plasma; Pyrazines; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry

2017
Initial testing (stage 1) of M6620 (formerly VX-970), a novel ATR inhibitor, alone and combined with cisplatin and melphalan, by the Pediatric Preclinical Testing Program.
    Pediatric blood & cancer, 2018, Volume: 65, Issue:2

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Cisplatin; Female; Humans; Isoxazoles; Melphalan; Mice; Mice, SCID; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrazines; Xenograft Model Antitumor Assays

2018
Targeting a non-oncogene addiction to the ATR/CHK1 axis for the treatment of small cell lung cancer.
    Scientific reports, 2017, Nov-14, Volume: 7, Issue:1

    Topics: Adenocarcinoma of Lung; Animals; Antineoplastic Agents; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Benzodiazepinones; cdc25 Phosphatases; Cell Cycle; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; Drug Resistance, Neoplasm; Gene Expression Regulation, Neoplastic; Humans; Isoxazoles; Lung Neoplasms; Male; Mice; Mice, Nude; Molecular Targeted Therapy; Protein Kinase Inhibitors; Proto-Oncogene Proteins p21(ras); Pyrazines; Pyrazoles; RNA, Messenger; Signal Transduction; Small Cell Lung Carcinoma; Xenograft Model Antitumor Assays

2017
Cryo-EM structure of human ATR-ATRIP complex.
    Cell research, 2018, Volume: 28, Issue:2

    Topics: Adaptor Proteins, Signal Transducing; Ataxia Telangiectasia Mutated Proteins; Carrier Proteins; Chromatography, Affinity; Chromatography, Gel; Cryoelectron Microscopy; DNA Damage; DNA-Binding Proteins; Humans; Isoxazoles; Mutation; Nuclear Proteins; Phosphorylation; Protein Binding; Protein Conformation, alpha-Helical; Protein Folding; Protein Kinases; Protein Multimerization; Pyrazines; Signal Transduction; TOR Serine-Threonine Kinases

2018
Challenges in implementing model-based phase I designs in a grant-funded clinical trials unit.
    Trials, 2017, Dec-28, Volume: 18, Issue:1

    Topics: Clinical Trials, Phase I as Topic; Combined Modality Therapy; Esophageal Neoplasms; Humans; Isoxazoles; Maximum Tolerated Dose; Pyrazines; Research Design

2017
The identification of the ATR inhibitor VE-822 as a therapeutic strategy for enhancing cisplatin chemosensitivity in esophageal squamous cell carcinoma.
    Cancer letters, 2018, 09-28, Volume: 432

    Topics: Animals; Antineoplastic Agents; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Carcinoma, Squamous Cell; Cell Cycle; Cell Proliferation; Cisplatin; CRISPR-Cas Systems; Drug Resistance, Neoplasm; Esophageal Neoplasms; Female; Gene Expression Regulation, Neoplastic; Humans; Isoxazoles; Mice; Mice, Inbred BALB C; Mice, Nude; Prognosis; Pyrazines; Signal Transduction; Survival Rate; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2018
Biodegradable PEG-poly(ω-pentadecalactone-co-p-dioxanone) nanoparticles for enhanced and sustained drug delivery to treat brain tumors.
    Biomaterials, 2018, Volume: 178

    Topics: Animals; Biocompatible Materials; Brain Neoplasms; Convection; Drug Delivery Systems; Drug Liberation; Hydrodynamics; Isoxazoles; Male; Nanoparticles; Polyesters; Polyethylene Glycols; Pyrazines; Radiation-Sensitizing Agents; Rats, Inbred F344; Xenograft Model Antitumor Assays

2018
ATR Inhibition Is a Promising Radiosensitizing Strategy for Triple-Negative Breast Cancer.
    Molecular cancer therapeutics, 2018, Volume: 17, Issue:11

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; cdc25 Phosphatases; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; DNA Breaks, Double-Stranded; Drug Resistance, Neoplasm; Female; Homologous Recombination; Humans; Isoxazoles; Mice, Inbred NOD; Mice, SCID; Phosphorylation; Proteolysis; Pyrazines; Radiation-Sensitizing Agents; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays

2018
Sensitivity of CD3/CD28-stimulated versus non-stimulated lymphocytes to ionizing radiation and genotoxic anticancer drugs: key role of ATM in the differential radiation response.
    Cell death & disease, 2018, 10-15, Volume: 9, Issue:11

    Topics: Amino Acid Chloromethyl Ketones; Antibodies; Ataxia Telangiectasia Mutated Proteins; Caspases; CD28 Antigens; CD3 Complex; Cell Proliferation; Chromones; DNA-Activated Protein Kinase; Drug Resistance; Gamma Rays; Gene Expression Regulation; Humans; Isoxazoles; Lymphocyte Activation; Morpholines; MRE11 Homologue Protein; Primary Cell Culture; Pyrazines; Pyrones; Radiation Tolerance; Signal Transduction; T-Lymphocytes, Cytotoxic; T-Lymphocytes, Regulatory; Thiophenes; Thioxanthenes

2018
A Comprehensive Human Gastric Cancer Organoid Biobank Captures Tumor Subtype Heterogeneity and Enables Therapeutic Screening.
    Cell stem cell, 2018, 12-06, Volume: 23, Issue:6

    Topics: Aminopyridines; Antineoplastic Agents; Benzimidazoles; Benzofurans; Biological Specimen Banks; Cell Proliferation; Drug Screening Assays, Antitumor; Female; Humans; Isoxazoles; Male; Naphthoquinones; Organoids; Precision Medicine; Pyrazines; Stomach Neoplasms

2018
DNA polymerase θ (POLQ) is important for repair of DNA double-strand breaks caused by fork collapse.
    The Journal of biological chemistry, 2019, 03-15, Volume: 294, Issue:11

    Topics: Camptothecin; Cells, Cultured; DNA Breaks, Double-Stranded; DNA Polymerase theta; DNA Repair; DNA Replication; DNA-Directed DNA Polymerase; Dose-Response Relationship, Drug; Humans; Isoxazoles; Protein Kinase Inhibitors; Pyrazines; Structure-Activity Relationship; Topoisomerase Inhibitors

2019
Inhibition of the Replication Stress Response Is a Synthetic Vulnerability in SCLC That Acts Synergistically in Combination with Cisplatin.
    Molecular cancer therapeutics, 2019, Volume: 18, Issue:4

    Topics: A549 Cells; Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Survival; Checkpoint Kinase 1; Cisplatin; CRISPR-Associated Protein 9; DNA Damage; Drug Synergism; Etoposide; Humans; Isoxazoles; Lung Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Protein Kinase Inhibitors; Pyrazines; Small Cell Lung Carcinoma; Tumor Burden; Xenograft Model Antitumor Assays

2019
Inhibition of Ataxia-Telangiectasia Mutated and RAD3-Related (
    Cancer research, 2019, 06-01, Volume: 79, Issue:11

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Checkpoint Kinase 2; Colorectal Neoplasms; DNA Breaks, Double-Stranded; Drug Resistance, Neoplasm; Female; Humans; Isoxazoles; Mice, Inbred C57BL; Oxaliplatin; Pyrazines; T-Lymphocytes; Xenograft Model Antitumor Assays

2019
Inhibition of Wee1 sensitizes AML cells to ATR inhibitor VE-822-induced DNA damage and apoptosis.
    Biochemical pharmacology, 2019, Volume: 164

    Topics: Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; DNA Damage; Dose-Response Relationship, Drug; Humans; Isoxazoles; Leukemia, Myeloid, Acute; Protein-Tyrosine Kinases; Pyrazines; U937 Cells

2019
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR
    Journal of medicinal chemistry, 2019, 06-13, Volume: 62, Issue:11

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Line; Drug Design; Isoxazoles; Male; Models, Molecular; Protein Conformation; Protein Kinase Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley

2019
Temozolomide Sensitizes MGMT-Deficient Tumor Cells to ATR Inhibitors.
    Cancer research, 2019, 09-01, Volume: 79, Issue:17

    Topics: Animals; Antineoplastic Agents, Alkylating; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; DNA Breaks, Double-Stranded; DNA Damage; DNA Modification Methylases; DNA Repair Enzymes; Drug Synergism; Female; Humans; Isoxazoles; Mice, Nude; Pyrazines; Temozolomide; Tumor Suppressor Proteins; Xenograft Model Antitumor Assays

2019
ATR Inhibition Broadly Sensitizes Soft-Tissue Sarcoma Cells to Chemotherapy Independent of Alternative Lengthening Telomere (ALT) Status.
    Scientific reports, 2020, 05-04, Volume: 10, Issue:1

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; DNA Damage; Female; Humans; Isoxazoles; Mice; Mice, Knockout; Neoplasm Proteins; Pyrazines; S Phase Cell Cycle Checkpoints; Sarcoma; Telomere Homeostasis; Xenograft Model Antitumor Assays

2020
Senescence Induction by Combined Ionizing Radiation and DNA Damage Response Inhibitors in Head and Neck Squamous Cell Carcinoma Cells.
    Cells, 2020, 09-01, Volume: 9, Issue:9

    Topics: Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Cycle; Cell Line, Tumor; Cellular Senescence; DNA Damage; Fibroblasts; Head and Neck Neoplasms; Humans; Isoxazoles; Male; Protein Kinase Inhibitors; Pyrazines; Pyridines; Quinolines; Radiation, Ionizing; Signal Transduction; Squamous Cell Carcinoma of Head and Neck; TOR Serine-Threonine Kinases; Triazoles

2020
Antiviral drug screen identifies DNA-damage response inhibitor as potent blocker of SARS-CoV-2 replication.
    Cell reports, 2021, 04-06, Volume: 35, Issue:1

    Topics: A549 Cells; Animals; Antiviral Agents; Chlorocebus aethiops; COVID-19; COVID-19 Drug Treatment; DNA Damage; Drug Evaluation, Preclinical; HEK293 Cells; HeLa Cells; Humans; Isoxazoles; MAP Kinase Signaling System; Middle East Respiratory Syndrome Coronavirus; Pyrazines; SARS-CoV-2; Vero Cells; Virus Replication

2021
Therapeutic targeting of ATR yields durable regressions in small cell lung cancers with high replication stress.
    Cancer cell, 2021, 04-12, Volume: 39, Issue:4

    Topics: Aged; Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; DNA Replication; DNA Topoisomerases, Type I; Genomic Instability; Humans; Isoxazoles; Lung Neoplasms; Middle Aged; Neoplasm Recurrence, Local; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Small Cell Lung Carcinoma

2021
Novel and Highly Potent ATR Inhibitor M4344 Kills Cancer Cells With Replication Stress, and Enhances the Chemotherapeutic Activity of Widely Used DNA Damaging Agents.
    Molecular cancer therapeutics, 2021, Volume: 20, Issue:8

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Proliferation; Deoxycytidine; DNA Replication; Female; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Irinotecan; Isoxazoles; Lung Neoplasms; Mice; Mice, Nude; Morpholines; Pyrazines; Pyrazoles; Small Cell Lung Carcinoma; Topotecan; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2021
Kinase Inhibitors of DNA-PK, ATM and ATR in Combination with Ionizing Radiation Can Increase Tumor Cell Death in HNSCC Cells While Sparing Normal Tissue Cells.
    Genes, 2021, 06-17, Volume: 12, Issue:6

    Topics: Ataxia Telangiectasia Mutated Proteins; Carcinoma, Squamous Cell; Cell Death; Cell Line, Tumor; Cells, Cultured; DNA Repair; DNA-Activated Protein Kinase; Head and Neck Neoplasms; Humans; Isoxazoles; Protein Kinase Inhibitors; Pyrazines; Pyridines; Quinolines; Triazoles; X-Rays

2021
ATR Inhibitor M6620 (VX-970) Enhances the Effect of Radiation in Non-Small Cell Lung Cancer Brain Metastasis Patient-Derived Xenografts.
    Molecular cancer therapeutics, 2021, Volume: 20, Issue:11

    Topics: Animals; Carcinoma, Non-Small-Cell Lung; Female; Heterografts; Humans; Isoxazoles; Lung Neoplasms; Mice; Mice, Nude; Neoplasm Metastasis; Pyrazines; Treatment Outcome

2021
VE-822, a novel DNA Holliday junction stabilizer, inhibits homologous recombination repair and triggers DNA damage response in osteogenic sarcomas.
    Biochemical pharmacology, 2021, Volume: 193

    Topics: Antineoplastic Agents; Cell Line, Tumor; DNA; DNA Damage; DNA Repair; Doxorubicin; Humans; Isoxazoles; Osteosarcoma; Pyrazines; Recombination, Genetic

2021
Brain Distribution of Berzosertib: An Ataxia Telangiectasia and Rad3-Related Protein Inhibitor for the Treatment of Glioblastoma.
    The Journal of pharmacology and experimental therapeutics, 2021, Volume: 379, Issue:3

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Brain; Cell Line, Tumor; Female; Glioblastoma; HEK293 Cells; Humans; Infusion Pumps; Isoxazoles; Male; Mice; Mice, Knockout; Mice, Nude; Pyrazines; Xenograft Model Antitumor Assays

2021
Combining radiation and the ATR inhibitor berzosertib activates STING signaling and enhances immunotherapy via inhibiting SHP1 function in colorectal cancer.
    Cancer communications (London, England), 2023, Volume: 43, Issue:4

    Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Colorectal Neoplasms; Humans; Immunotherapy; Mice; Pyrazines; Tumor Microenvironment

2023