isoxazoles has been researched along with pyrazines in 55 studies
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 1 (1.82) | 18.7374 |
1990's | 2 (3.64) | 18.2507 |
2000's | 5 (9.09) | 29.6817 |
2010's | 33 (60.00) | 24.3611 |
2020's | 14 (25.45) | 2.80 |
Authors | Studies |
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Fotsch, C; St Jean, DJ | 1 |
Dannhardt, G; Dominiak, P; Laufer, S | 1 |
Cheney, DL; McGill, W; Murray, TF | 1 |
Kato, A; Kubo, K; Matsuzaki, Y; Okita, K; Terai, S | 1 |
Chaudhry, V; Umapathi, T | 1 |
Adams, AD; Burton, CA; Chin, J; Guo, Q; Huang, S; Lam, MH; Latham, M; Lopez, JC; Lund, EG; Menke, JG; Milot, DP; Mitnaul, LJ; Peterson, LB; Rex-Rabe, SE; Rosa, RL; Sparrow, CP; Tian, JY; Wright, SD | 1 |
Alcázar, J; Alonso, JM; Alvarez, RM; Andrés, JI; Bakker, MH; Biesmans, I; Cid, JM; De Lucas, AI; Drinkenburg, W; Fernández, J; Font, LM; Iturrino, L; Langlois, X; Lenaerts, I; Martínez, S; Megens, AA; Pastor, J; Pullan, S; Steckler, T | 1 |
Howell, MH; von Arnim, AG; Woo, J | 1 |
Hussar, DA | 1 |
Li, Z; Liu, M; Liu, T; Luo, J; Qiu, WW; Tang, J; Xu, J; Yang, F | 1 |
Gobec, S; Hrast, M; Janežič, D; Konc, J; Turk, S; Vehar, B | 1 |
Brunner, TB; Charlton, PA; Cornelissen, B; Fokas, E; Gillies McKenna, W; Hammond, EM; Muschel, RJ; Olcina, MM; Pollard, JR; Prevo, R; Reaper, PM; Vallis, KA | 1 |
Andrulis, M; Bargou, RC; Beilhack, A; Bogen, B; Bumm, T; Chatterjee, M; Einsele, H; Heimberger, T; Riedel, S; Schraud, H; Stühmer, T | 1 |
Hilgenfeld, R; Jochmans, D; Ma, Q; Nascimento, MS; Neyts, J; Rocha-Pereira, J | 1 |
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, M | 1 |
Blacklow, SC; Bradner, JE; Buckley, DL; Fu, H; Huang, Y; Kadam, A; Liu, S; Marineau, JJ; McKeown, MR; Qi, J; Shaw, DL; Xu, X; Zhang, W; Zhang, X; Zhang, Z | 1 |
Bogachkov, Y; Doscas, ME; Kaufman, H; Li, Y; Rao, GS; Ruby, C; Usha, L; Wang, Y; Williams, JW; Williamson, AJ; Xiao, F; Xu, X; Zhou, J | 1 |
Foote, KM; Lau, A; Nissink, JW | 1 |
Altmeyer, R; Gao, Q; Lan, K; Li, G; Wang, Y; Yuan, S; Zou, G | 1 |
Massey, AJ | 1 |
Biskup, E; Gniadecki, R; Naym, DG | 1 |
Gershon, TR; Hwang, D; Kabanov, AV; Lang, PY; Nanjangud, GJ; Parker, JS; Shaw, C; Sokolsky-Papkov, M | 1 |
Boumelha, AJ; Dobrynin, G; Hammond, EM; Hawkins, MA; Ient, J; Leslie, RE; Leszczynska, KB; Maughan, T; Mukherjee, S; Senra, JM | 1 |
Bakkenist, CJ; Beumer, JH; Chu, E; Doyle, A; Iffland, A; Ivy, P; Kiesel, BF; Parise, RA; Scemama, J; Villaruz, L | 1 |
Houghton, PJ; Kang, M; Kurmashev, D; Kurmasheva, RT; Reynolds, CP; Smith, MA; Wu, J | 1 |
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, M | 1 |
Ding, C; Hao, Y; Liu, M; Qin, Z; Rao, Q; Song, L; Tian, Y; Wang, HW; Wang, J; Wu, Z; Xu, Y | 1 |
Frangou, E; Hawkins, M; Holmes, J; Love, S; McGregor, N | 1 |
Abu-Hashem, AA; El-Shazly, M | 1 |
Chen, KN; Dai, L; Dong, B; Fu, H; Kang, XZ; Liang, Z; Shen, LY; Shi, Q; Xiong, HC; Yan, WP; Yang, YB | 1 |
Fernandez-Capetillo, O; Lecona, E | 1 |
Bindra, RS; Chen, EM; Focarete, ML; Jackson, C; Jiang, Z; Josowitz, AD; Merlettini, A; Noorbakhsh, S; Quijano, AR; Saltzman, WM; Seo, YE; Sundaram, RK | 1 |
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, Q | 1 |
Badura, J; Becker, H; Fahrer, J; Heylmann, D; Kaina, B | 1 |
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, J | 1 |
Chiba, T; Kurian, S; Li, S; Song, Y; Wang, Z; Wu, X; Xiang, R | 1 |
Aben, N; Avelar, AT; Berns, A; Cozijnsen, M; de Vries, H; Nagel, R; Proost, N; van de Ven, M; van der Vliet, J; Wessels, LFA | 1 |
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, N | 1 |
Li, X; Qi, W; Sun, L; Wang, C; Wang, M; Xu, X; Zhao, D | 1 |
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, S | 1 |
Bindra, RS; Breslin, H; Burgenske, DM; Ganesa, S; Gilad, O; Jackson, CB; Jia, L; Kalathil, AN; Noorbakhsh, SI; Sarkaria, JN; Sundaram, RK | 1 |
Andrs, M; Gorecki, L; Korabecny, J; Rezacova, M | 1 |
Algéo, MP; Chaire, V; Italiano, A; Laroche-Clary, A; Le Loarer, F; Malykh, A; Verbeke, S | 1 |
Distel, L; Dobler, C; Fietkau, R; Hecht, M; Jost, T | 1 |
Falk, M; Hendriks, BS; Jansen, M; Terranova, N | 1 |
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, C | 1 |
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, A | 1 |
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, A | 1 |
Bürkel, F; Distel, LV; Faulhaber, EM; Fietkau, R; Hecht, M; Jost, T; Scheper, J; Symank, J | 1 |
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, SG | 1 |
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, T | 1 |
Fu, F; Geng, Z; Hu, L; Huang, Q; Li, X; Liu, S; Liu, X; Song, Q; Wang, H; Yin, Q; Zhu, Y | 1 |
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, N | 1 |
Bindra, RS; Burgenske, DM; Dragojevic, S; Elmquist, WF; Gupta, SK; Kim, M; Mohammad, AS; Sarkaria, JN; Talele, S; Zhang, W | 1 |
Classe, JM; Ferron, G; Floquet, A; Freyer, G; Hardy-Bessard, AC; Kurtz, JE; Lécuru, F; Motte-Rouge, T; Pautier, P | 1 |
6 review(s) available for isoxazoles and pyrazines
Article | Year |
---|---|
Mitigating heterocycle metabolism in drug discovery.
Topics: Animals; Biotransformation; Databases, Factual; Drug Discovery; Drug Interactions; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds, 4 or More Rings; Humans; Mice; Pharmaceutical Preparations; Rats | 2012 |
Toxic neuropathy.
Topics: Animals; Boronic Acids; Bortezomib; Clinical Trials as Topic; Epothilones; Genetic Therapy; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Isoxazoles; Leflunomide; Neuritis; Neuroprotective Agents; Neurotoxicity Syndromes; Organoplatinum Compounds; Oxaliplatin; Peripheral Nervous System Diseases; Pyrazines; Pyridoxine; Thalidomide | 2005 |
Drugging ATR: progress in the development of specific inhibitors for the treatment of cancer.
Topics: Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; DNA Damage; Humans; Isoxazoles; Molecular Conformation; Neoplasms; Pyrazines | 2015 |
Targeting ATR in cancer.
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.
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.
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 |
3 trial(s) available for isoxazoles and pyrazines
Article | Year |
---|---|
Population pharmacokinetics of ATR inhibitor berzosertib in phase I studies for different cancer types.
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.
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.
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 |
46 other study(ies) available for isoxazoles and pyrazines
Article | Year |
---|---|
[Hypertensive action of 5-(beta-aminoethyl)aminoisoxazoles: synthesis and screening of isoxazolopyrazines and isoxazolodiazepines].
Topics: Animals; Azepines; Blood Pressure; Decerebrate State; Heart Rate; Isoxazoles; Male; Pyrazines; Rats; Rats, Inbred Strains; Structure-Activity Relationship | 1991 |
A comparison of the analgesic activities of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP) and 6-chloro-2[1-piperazinyl]pyrazine (MK 212).
Topics: Analgesics; Animals; Bicuculline; Dose-Response Relationship, Drug; Drug Synergism; Drug Tolerance; Isoxazoles; Male; Mice; Morphine; Oxazoles; Pyrazines; Time Factors | 1983 |
Antitumor effect of vesnarinone on human hepatocellular carcinoma cell lines.
Topics: Antineoplastic Agents; Apoptosis; Carcinoma, Hepatocellular; Cell Division; Dose-Response Relationship, Drug; Humans; In Situ Nick-End Labeling; Isoxazoles; Liver Neoplasms; Pyrazines; Quinolines; Tumor Cells, Cultured | 1999 |
Different roles of liver X receptor alpha and beta in lipid metabolism: effects of an alpha-selective and a dual agonist in mice deficient in each subtype.
Topics: 8-Bromo Cyclic Adenosine Monophosphate; Administration, Oral; Animals; ATP Binding Cassette Transporter 1; ATP-Binding Cassette Transporters; Cholesterol; Cholesterol, HDL; Cyclic AMP; DNA-Binding Proteins; Dose-Response Relationship, Drug; Gene Expression Regulation; Isoxazoles; Lipid Metabolism; Liver; Liver X Receptors; Macrophages, Peritoneal; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Structure; Orphan Nuclear Receptors; Phenylurea Compounds; Protein Isoforms; Pyrazines; Receptors, Cytoplasmic and Nuclear; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sterol Regulatory Element Binding Protein 1; Triglycerides | 2006 |
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Topics: Adrenergic alpha-2 Receptor Antagonists; Animals; Antidepressive Agents, Tricyclic; Humans; Isoxazoles; Male; Oxazoles; Pyrazines; Rats; Rats, Wistar; Selective Serotonin Reuptake Inhibitors | 2007 |
Structure-function studies on the active site of the coelenterazine-dependent luciferase from Renilla.
Topics: Aequorin; Amino Acid Sequence; Binding Sites; Catalysis; Computer Simulation; Diethyl Pyrocarbonate; Imidazoles; Isoxazoles; Luciferases, Renilla; Luminescent Measurements; Models, Molecular; Mutagenesis, Site-Directed; Phenylmethylsulfonyl Fluoride; Pyrazines; Structure-Activity Relationship | 2008 |
New drug update: 2007.
Topics: Aged; Amides; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antihypertensive Agents; Antiparkinson Agents; Antipsychotic Agents; Drug Approval; Fumarates; Humans; Hypoglycemic Agents; Isoxazoles; Macular Degeneration; Paliperidone Palmitate; Pyrazines; Pyrimidines; Ranibizumab; Sitagliptin Phosphate; Tetrahydronaphthalenes; Thiophenes; Triazoles; United States | 2008 |
Synthesis and biological evaluation of heterocyclic ring-fused betulinic acid derivatives as novel inhibitors of osteoclast differentiation and bone resorption.
Topics: Acid Phosphatase; Animals; Betulinic Acid; Bone Density Conservation Agents; Bone Resorption; Cathepsin K; Cell Differentiation; Cell Line; Cell Proliferation; Crystallography, X-Ray; Female; Isoenzymes; Isoxazoles; Mice; Mice, Inbred C57BL; Osteoclasts; Ovariectomy; Pentacyclic Triterpenes; Pyrazines; Pyrazoles; Pyrimidines; RANK Ligand; Rats; Structure-Activity Relationship; Tartrate-Resistant Acid Phosphatase; Thiazoles; Triterpenes | 2012 |
Function of the D-alanine:D-alanine ligase lid loop: a molecular modeling and bioactivity study.
Topics: Bacterial Proteins; Benzothiazoles; Enzyme Assays; Escherichia coli Proteins; Isoxazoles; Molecular Dynamics Simulation; Peptide Synthases; Protein Binding; Protein Conformation; Pyrazines; Pyrimidines; Stereoisomerism; Structure-Activity Relationship; Thermus | 2012 |
Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation.
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 |
The heat shock transcription factor 1 as a potential new therapeutic target in multiple myeloma.
Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Blotting, Western; Boronic Acids; Bortezomib; Cells, Cultured; Diterpenes; DNA-Binding Proteins; Down-Regulation; Epoxy Compounds; Female; Gene Knockdown Techniques; Heat Shock Transcription Factors; Heat-Shock Proteins; Humans; Immunohistochemistry; Isoxazoles; Mice; Mice, Inbred BALB C; Multiple Myeloma; Neoplasm Transplantation; Phenanthrenes; Plasma Cells; Proteasome Endopeptidase Complex; Pyrazines; Resorcinols; RNA, Small Interfering; Transcription Factors; Transplantation, Heterologous | 2013 |
The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon.
Topics: Amides; Antiviral Agents; Cell Line; Cysteine Endopeptidases; Cytidine; Drug Combinations; Drug Synergism; Hepatocytes; Humans; Isoxazoles; Molecular Docking Simulation; Norwalk virus; Papain; Phenylalanine; Pyrazines; Pyrrolidinones; Replicon; RNA-Dependent RNA Polymerase; Valine; Viral Proteins; Virus Replication | 2014 |
Potentiation of tumor responses to DNA damaging therapy by the selective ATR inhibitor VX-970.
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 |
Biased multicomponent reactions to develop novel bromodomain inhibitors.
Topics: Alkanesulfonic Acids; Azepines; Cell Cycle Proteins; Cell Line, Tumor; Crystallography, X-Ray; Fluorocarbons; Gene Expression Regulation; Humans; Imidazoles; Inhibitory Concentration 50; Isoxazoles; Ligands; Models, Molecular; Nuclear Proteins; Pyrazines; Pyridines; Small Molecule Libraries; Structure-Activity Relationship; Transcription Factors | 2014 |
Inhibition of p70 S6 kinase (S6K1) activity by A77 1726 and its effect on cell proliferation and cell cycle progress.
Topics: Aniline Compounds; Butadienes; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chromones; Crotonates; Feedback, Physiological; Gene Knockdown Techniques; Humans; Hydroxybutyrates; Imidazoles; Isoxazoles; Leflunomide; MAP Kinase Signaling System; Morpholines; Nitriles; Phosphatidylinositol 3-Kinases; Protein Kinase Inhibitors; Pyrazines; Receptor, IGF Type 1; Ribosomal Protein S6 Kinases, 70-kDa; Toluidines | 2014 |
In Vitro Assessment of Combinations of Enterovirus Inhibitors against Enterovirus 71.
Topics: Amides; Amino Acid Sequence; Animals; Antiviral Agents; Binding Sites; Cell Line, Tumor; Chlorocebus aethiops; Drug Combinations; Drug Resistance, Viral; Drug Synergism; Enterovirus A, Human; Humans; Indoles; Isoxazoles; Itraconazole; Molecular Docking Simulation; Mutation; Myoblasts; Phenols; Phenylalanine; Protein Binding; Protein Interaction Domains and Motifs; Protein Structure, Secondary; Pyrazines; Pyrrolidinones; Sequence Alignment; Sequence Homology, Amino Acid; Suramin; Valine; Vero Cells; Viral Nonstructural Proteins; Virus Replication | 2016 |
Inhibition of ATR-dependent feedback activation of Chk1 sensitises cancer cells to Chk1 inhibitor monotherapy.
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.
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.
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.
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.
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.
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.
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.
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.
Topics: Clinical Trials, Phase I as Topic; Combined Modality Therapy; Esophageal Neoplasms; Humans; Isoxazoles; Maximum Tolerated Dose; Pyrazines; Research Design | 2017 |
Synthesis of New Isoxazole-, Pyridazine-, Pyrimidopyrazines and Their Anti-Inflammatory and Analgesic Activity.
Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Drug Evaluation, Preclinical; Female; Isoxazoles; Male; Mice; Molecular Structure; Pyrazines; Pyridazines; Pyrimidines; Rats, Sprague-Dawley | 2018 |
The identification of the ATR inhibitor VE-822 as a therapeutic strategy for enhancing cisplatin chemosensitivity in esophageal squamous cell carcinoma.
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.
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.
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.
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.
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.
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.
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 (
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.
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
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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 |