pyrazines has been researched along with indazoles in 36 studies
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 25 (69.44) | 24.3611 |
2020's | 11 (30.56) | 2.80 |
Authors | Studies |
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Kocí, J; Krchnák, V; Oliver, AG | 1 |
Brown, KK; Choudhry, AE; Heerding, DA; Kumar, R; Lai, Z; Lin, H; Luengo, JI; Minthorn, EA; Rhodes, N; Robell, KA; Verma, S; Xie, R; Yamashita, DS; Zeng, J; Zhang, S | 1 |
Arango, BA; Cohen, EE; Perez, CA; Raez, LE; Santos, ES | 1 |
Fuchi, N; Fujii, S; Iura, Y; Kaneko, H; Nishimura, K; Nitta, A; Sekiya, Y; Suyama, K; Takahashi, T; Ueda, H; Yamada, M; Yamaguchi, S | 1 |
Aiello, R; Aspnes, GE; Atkinson, K; Baker, L; Barucci, N; Bian, J; Bourassa, P; Bourbonais, F; Bourbounais, F; D'Aquila, T; Derksen, DR; Filipski, KJ; Guzman-Perez, A; Hamilton, M; Hank, R; Jones, CS; Karki, K; Li, JC; Litchfield, J; MacDougall, M; Patel, L; Pfefferkorn, JA; Rasmusson, T; Robertson, A; Sammons, MF; Song, W; Tu, M; Zeng, D | 1 |
DeVicente, J; Hermann, JC; Jaime-Figueroa, S; Jin, S; Kuglstatter, A; Li, H; Lovey, A; Lynch, SM; Menke, J; Niu, L; Patel, V; Roy, D; Soth, M; Steiner, S; Tivitmahaisoon, P; Vu, MD; Yee, C | 1 |
Burke, RT; Clarke, AS; Currie, KS; Dipaolo, JA; Druker, BJ; Lannutti, BJ; Loriaux, MM; Maciejewski, P; Meadows, S; Mitchell, SA; Spurgeon, SE | 1 |
Barbosa, J; Blomgren, P; Currie, KS; Di Paolo, JA; Gallion, S; Kropf, JE; Lansdon, EB; Lee, T; Macaluso, J; Maciejewski, P; Maclin, D; Mitchell, SA; Rong, H; Rossi, AM; Whitney, JA; Xu, J; Zhao, Z | 1 |
Abella, S; Boxer, M; Hawkins, M; Hu, J; Klein, L; Kolibaba, K; Sharman, J; Wu, M; Yasenchak, C | 1 |
Cebrián, D; de Cabo, R; González-García, I; Gutierrez, VM; Iglesias, G; López, M; Lopez-Guadamillas, E; Martinez, S; Mattison, JA; Mitchell, SJ; Muñoz-Martin, M; Ortega-Molina, A; Pastor, J; Serrano, M; Szarowicz, MD; Vaughan, KL | 1 |
Greenhill, C | 1 |
Chen, K; Gaur, S; Hu, S; Liu, YR; Pan, SL; Tzeng, HE; Wang, Y; Yang, L; Yen, Y | 1 |
Abella-Dominicis, E; Barr, PM; Cheson, BD; Di Paolo, J; Dreiling, LK; Friedberg, JW; Greenwald, DR; Hawkins, MJ; He, J; Hu, J; Joshi, A; Lee, H; Liem, AK; Mclntyre, RE; O'Brien, SM; Reddy, A; Saylors, GB; Spurgeon, SE | 1 |
Cragg, MS; Hou, S; Marshall, AJ; Pauls, SD; Ray, A; Vaughan, AT | 1 |
Choi, JS; Goh, SH; Han, BG; Kim, HS; Kim, JH; Koh, JS; Lee, BI; Lee, J; Lee, SJ; Nam, S; Song, HJ | 1 |
Almejún, MB; Bezares, RF; Borge, M; Cabrejo, M; Colado, A; Dos Santos, P; Elías, EE; Fernández Grecco, H; Gamberale, R; Giordano, M; Podaza, E; Risnik, D; Slavutsky, I; Stanganelli, C | 1 |
Morimoto-Kamata, R; Yui, S | 1 |
Chen, J; Chen, X; Chung, RT; Fuchs, BC; He, L; Holmes, JA; Hong, J; Hu, Q; Jiang, Y; Jin, Q; Li, S; Li, W; Liao, Y; Lidofsky, A; Lin, W; Lin, Z; Liu, Y; Qu, C; Tu, M; Wei, L; Yuan, H; Zheng, D | 1 |
Hayashi, T; Kittaka, M; Kondo, T; Reichenberger, EJ; Ueki, Y; Yoshimoto, T | 1 |
Alisi, MA; Bettolo, RM; Cazzolla, N; Ceccacci, F; Furlotti, G; Garrone, B; Gasperi, T; La Bella, A; Leonelli, F; Loreto, MA; Magarò, G; Mangano, G; Masini, E; Miceli, M; Migneco, LM; Vitiello, M | 1 |
Assouline, S; Burke, JM; Chen, R; Essell, J; Patel-Donnelly, D; Sharman, J; Shi, W; Shustov, A; Yang, J; Ye, W | 1 |
Andorsky, DJ; Assouline, S; Forero-Torres, A; Jones, V; Klein, LM; Kolibaba, KS; Patel-Donnelly, D; Sharman, JP; Shi, W; Smith, M; Yasenchak, CA; Ye, W | 1 |
Cardona, DM; Cardones, AR; Chao, NJ; Chen, BJ; Di Paolo, JA; Jia, W; Kim, JY; Perez, VL; Poe, JC; Reyes, NJ; Saban, DR; Sarantopoulos, S; Su, H; Sundy, JS | 1 |
Assouline, S; Awan, FT; Hill, B; Patel-Donnelly, D; Rao, AV; Sharman, JP; Thirman, MJ; Ye, W | 1 |
Alexe, G; Armstrong, SA; Blachly, JS; Byrd, JC; Chu, SH; Cremer, A; Ellegast, JM; Frank, ES; Goodale, A; Häupl, B; Mohr, S; Oellerich, T; Piccioni, F; Pikman, Y; Rao, AV; Robichaud, A; Ross, L; Stegmaier, K; Walker, AR | 1 |
Accordi, B; Basso, G; Bresolin, S; Cortese, G; Mariotto, E; Porcù, E; Serafin, V; Veltri, G | 1 |
Bhargava, P; Danilov, AV; Dyer, MJS; Fegan, CD; Herbaux, C; Hillmen, P; Huang, X; Humeniuk, R; Jürgensmeier, JM; Karlin, L; Kio, EA; Mitra, SS; Rule, SA; Walter, HS; Yi, PC; Zhou, Z | 1 |
Bagashev, A; Brown, PA; Loftus, JP; Niswander, LM; Schauf, A; Tannheimer, S; Tasian, SK; Wang, M; Yahiaoui, A | 1 |
Junghanss, C; Kong, W; Murua Escobar, H; Nolte, I; Perez, SV; Ruetgen, B; Sekora, A; Sender, S | 1 |
Jorda, R; Krajčovičová, S; Králová, P; Kryštof, V; Soural, M | 1 |
Bhatnagar, B; Blachly, JS; Blum, WG; Byrd, JC; Crosswell, HE; Lin, TL; Liu, J; Long, L; Mims, AS; Minden, MD; Munugalavadla, V; Oellerich, T; Orwick, S; Pan, Y; Rao, AV; Serve, H; Walker, AR; Zhang, D | 1 |
Bhargava, P; Bouabdallah, K; Cartron, G; Danilov, AV; Davies, AJ; Dyer, MJS; Fegan, C; Hodson, DJ; Huang, X; Humeniuk, R; Jürgensmeier, JM; Li, B; Morschhauser, F; Radford, J; Rajakumaraswamy, N; Rule, SA; Salles, G; Spurgeon, S; Walter, HS; Ysebaert, L | 1 |
Becker, A; Chabanovska, O; Junghanss, C; Murua Escobar, H; Ngezahayo, A; Sekora, A; Sender, S; Villa Perez, S | 1 |
Best, S; Danilov, AV; Goodyear, S; Hashiguchi, T; Kittai, AS; Lam, V; Okada, C; Park, B; Persky, DO; Spurgeon, SE; Thurlow, B | 1 |
Adachi, J; Araki, M; Friboulet, L; Fujita, N; Katayama, K; Katayama, R; Kukimoto-Niino, M; Kutkowska, J; Ma, B; Maruyama, K; Mizuta, H; Nishio, M; Oh-Hara, T; Okada, K; Okuno, Y; Sagae, Y; Sasakura, Y; Shirouzu, M; Simizu, S; Takagi, S; Takemoto, A; Tamai, K; Watanabe, K; Yanagitani, N | 1 |
Best, S; Danilov, AV; Kittai, A; Lam, V; Liu, T; Orand, K; Spurgeon, SE | 1 |
1 review(s) available for pyrazines and indazoles
Article | Year |
---|---|
Novel molecular targeted therapies for refractory thyroid cancer.
Topics: Angiogenesis Inhibitors; Anilides; Antineoplastic Agents; Axitinib; Benzamides; Benzenesulfonates; Benzoquinones; Bibenzyls; Boronic Acids; Bortezomib; Depsipeptides; ErbB Receptors; Gefitinib; Histone Deacetylase Inhibitors; HSP90 Heat-Shock Proteins; Humans; Hydroxamic Acids; Imatinib Mesylate; Imidazoles; Indazoles; Indoles; Lactams, Macrocyclic; Lenalidomide; Niacinamide; Oligonucleotides; Phenylurea Compounds; Piperazines; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-kit; Pyrazines; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Quinolines; Receptor Protein-Tyrosine Kinases; Receptors, Vascular Endothelial Growth Factor; Sorafenib; Sulfonamides; Sunitinib; Thalidomide; Thyroid Neoplasms; Valproic Acid; Vorinostat | 2012 |
9 trial(s) available for pyrazines and indazoles
Article | Year |
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An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia.
Topics: Aged; Aged, 80 and over; Disease-Free Survival; Female; Humans; Indazoles; Intracellular Signaling Peptides and Proteins; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Middle Aged; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazines; Syk Kinase | 2015 |
Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL.
Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Class I Phosphatidylinositol 3-Kinases; Cytokines; Early Termination of Clinical Trials; Female; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Lymphoma, Non-Hodgkin; Male; Middle Aged; Neoplasm Proteins; Pneumonia; Protein Kinase Inhibitors; Purines; Pyrazines; Quinazolinones; Salvage Therapy; Syk Kinase | 2016 |
An Open-label, Phase II Trial of Entospletinib (GS-9973), a Selective Spleen Tyrosine Kinase Inhibitor, in Diffuse Large B-cell Lymphoma.
Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Disease Progression; Drug Administration Schedule; Female; Humans; Indazoles; Lymphoma, Large B-Cell, Diffuse; Male; Middle Aged; Progression-Free Survival; Protein Kinase Inhibitors; Pyrazines; Syk Kinase; Time Factors | 2018 |
An open-label phase 2 trial of entospletinib in indolent non-Hodgkin lymphoma and mantle cell lymphoma.
Topics: Adult; Aged; Aged, 80 and over; Female; Humans; Indazoles; Lymphoma, B-Cell, Marginal Zone; Lymphoma, Follicular; Lymphoma, Mantle-Cell; Male; Middle Aged; Neoplasm Proteins; Pyrazines; Syk Kinase; Waldenstrom Macroglobulinemia | 2019 |
Entospletinib monotherapy in patients with relapsed or refractory chronic lymphocytic leukemia previously treated with B-cell receptor inhibitors: results of a phase 2 study.
Topics: Aged; Aged, 80 and over; Combined Modality Therapy; Drug Resistance, Neoplasm; Female; Humans; Indazoles; Kaplan-Meier Estimate; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Middle Aged; Prognosis; Protein Kinase Inhibitors; Pyrazines; Receptors, Antigen, B-Cell; Recurrence; Retreatment; Treatment Outcome | 2019 |
Phase Ib Study of Tirabrutinib in Combination with Idelalisib or Entospletinib in Previously Treated Chronic Lymphocytic Leukemia.
Topics: Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Drug Resistance, Neoplasm; Female; Follow-Up Studies; Humans; Imidazoles; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Maximum Tolerated Dose; Middle Aged; Neoplasm Recurrence, Local; Prognosis; Purines; Pyrazines; Pyrimidines; Quinazolinones; Salvage Therapy; Tissue Distribution | 2020 |
Entospletinib in Combination with Induction Chemotherapy in Previously Untreated Acute Myeloid Leukemia: Response and Predictive Significance of
Topics: Adult; Cytarabine; Daunorubicin; Female; Gene Expression Regulation, Neoplastic; Homeodomain Proteins; Humans; Indazoles; Induction Chemotherapy; Leukemia, Myeloid, Acute; Male; Middle Aged; Myeloid Ecotropic Viral Integration Site 1 Protein; Pyrazines; Syk Kinase | 2020 |
Phase 1b study of tirabrutinib in combination with idelalisib or entospletinib in previously treated B-cell lymphoma.
Topics: Adult; Aged; Antineoplastic Agents; Female; Humans; Imidazoles; Indazoles; Lymphoma, B-Cell; Male; Middle Aged; Protein Kinase Inhibitors; Purines; Pyrazines; Pyrimidines; Quinazolinones | 2021 |
Proapoptotic and immunomodulatory effects of SYK inhibitor entospletinib in combination with obinutuzumab in patients with chronic lymphocytic leukaemia.
Topics: Antibodies, Monoclonal, Humanized; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Neoplasm Recurrence, Local; Pyrazines; Receptors, Antigen, B-Cell; Syk Kinase | 2022 |
26 other study(ies) available for pyrazines and indazoles
Article | Year |
---|---|
Unprecedented rearrangement of 2-(2-aminoethyl)-1-aryl-3,4-dihydropyrazino[1,2-b]indazole-2-ium 6-oxides to 2,3-dihydro-1H-imidazo[1,2-b]indazoles.
Topics: Catalysis; Imidazoles; Indazoles; Molecular Structure; Oxides; Pyrazines; Structure-Activity Relationship | 2010 |
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Topics: Animals; Cell Line, Tumor; Glycogen Synthase Kinase 3; Glycogen Synthase Kinase 3 beta; Humans; Indazoles; Mice; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Pyridines; Xenograft Model Antitumor Assays | 2010 |
Discovery and structure-activity relationship of 2,6-disubstituted pyrazines, potent and selective inhibitors of protein kinase CK2.
Topics: Animals; Binding Sites; Casein Kinase II; Computer Simulation; Disease Models, Animal; Drug Evaluation, Preclinical; Humans; Indazoles; Injections, Intraperitoneal; Nephritis; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrazines; Rats; Structure-Activity Relationship | 2012 |
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.
Topics: Administration, Oral; Animals; Cell Line, Tumor; Diabetes Mellitus, Type 2; Drug Design; Glucokinase; Glucose Tolerance Test; Half-Life; Humans; Hypoglycemic Agents; Indazoles; Insulin; Kinetics; Protein Binding; Pyrazines; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship | 2012 |
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
Topics: Binding Sites; Crystallography, X-Ray; Drug Design; Hydrophobic and Hydrophilic Interactions; Indazoles; Janus Kinase 1; Janus Kinase 2; Janus Kinase 3; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrazines; Structure-Activity Relationship | 2013 |
A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Drug Synergism; Humans; Indazoles; Intracellular Signaling Peptides and Proteins; Leukemia, Lymphocytic, Chronic, B-Cell; Phosphorylation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Purines; Pyrazines; Quinazolinones; Signal Transduction; Syk Kinase | 2014 |
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Topics: Administration, Oral; Animals; Cells, Cultured; Drug Discovery; Humans; Indazoles; Magnetic Resonance Spectroscopy; Mice; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazines; Rats; Spectrometry, Mass, Electrospray Ionization; Spleen; Structure-Activity Relationship | 2014 |
Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.
Topics: Adiposity; Animals; Histological Techniques; Imidazoles; Immunoblotting; Indazoles; Liver; Macaca mulatta; Mass Spectrometry; Metabolic Syndrome; Mice, Obese; Phosphoinositide-3 Kinase Inhibitors; Pyrazines; Sulfonamides | 2015 |
Obesity: Inhibiting PI3K reduces body weight in obese mice.
Topics: Adiposity; Animals; Imidazoles; Indazoles; Metabolic Syndrome; Phosphoinositide-3 Kinase Inhibitors; Pyrazines; Sulfonamides | 2015 |
The pan-PI3K inhibitor GDC-0941 activates canonical WNT signaling to confer resistance in TNBC cells: resistance reversal with WNT inhibitor.
Topics: Animals; Apoptosis; beta Catenin; Blotting, Western; Cell Proliferation; Drug Resistance, Neoplasm; Female; Fluorescent Antibody Technique; Humans; Indazoles; Mice; Mice, Nude; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Pyridines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sulfonamides; TOR Serine-Threonine Kinases; Triple Negative Breast Neoplasms; Tumor Cells, Cultured; Wnt Proteins; Xenograft Model Antitumor Assays | 2015 |
FcγRIIB-Independent Mechanisms Controlling Membrane Localization of the Inhibitory Phosphatase SHIP in Human B Cells.
Topics: B-Lymphocytes; Bridged Bicyclo Compounds, Heterocyclic; Cell Line; Cell Membrane; Cells, Cultured; Green Fluorescent Proteins; Humans; Indazoles; Lymphocyte Activation; Oxazines; Phosphatidylinositol Phosphates; Phosphatidylinositol-3,4,5-Trisphosphate 5-Phosphatases; Photobleaching; Pyrazines; Pyridines; Pyrimidines; Receptors, Antigen, B-Cell; Receptors, IgG; Signal Transduction; Syk Kinase | 2016 |
Crystal structures of spleen tyrosine kinase in complex with novel inhibitors: structural insights for design of anticancer drugs.
Topics: Antineoplastic Agents; Crystallography, X-Ray; Drug Design; Indazoles; Models, Molecular; Oxazines; Protein Kinase Inhibitors; Pyrazines; Pyridines; Syk Kinase | 2016 |
The kinase inhibitors R406 and GS-9973 impair T cell functions and macrophage-mediated anti-tumor activity of rituximab in chronic lymphocytic leukemia patients.
Topics: Aged; Aged, 80 and over; Cell Proliferation; Cells, Cultured; Female; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Lymphocyte Activation; Macrophages; Male; Middle Aged; Oxazines; Phagocytosis; Phosphorylation; Pyrazines; Pyridines; Receptors, Antigen, T-Cell; Rituximab; Syk Kinase; T-Lymphocytes; ZAP-70 Protein-Tyrosine Kinase | 2017 |
Insulin-like growth factor-1 signaling is responsible for cathepsin G-induced aggregation of breast cancer MCF-7 cells.
Topics: Autocrine Communication; Axitinib; Breast Neoplasms; Cathepsin G; Cell Aggregation; Female; Humans; Imidazoles; Indazoles; Indoles; Insulin-Like Growth Factor I; MCF-7 Cells; Phosphorylation; Pyrazines; Pyrroles; Receptor, IGF Type 1; Receptors, Somatomedin; Signal Transduction; Small Molecule Libraries; Sunitinib | 2017 |
Tyrosine kinase SYK is a potential therapeutic target for liver fibrosis.
Topics: Animals; Drug Evaluation, Preclinical; Hep G2 Cells; Hepatic Stellate Cells; Hepatocytes; Humans; Indazoles; Liver Cirrhosis, Experimental; Male; Mice, Inbred C57BL; Pyrazines; Rats; Syk Kinase | 2018 |
Second-Generation SYK Inhibitor Entospletinib Ameliorates Fully Established Inflammation and Bone Destruction in the Cherubism Mouse Model.
Topics: Adaptor Proteins, Signal Transducing; Animals; Bone and Bones; Cherubism; Disease Models, Animal; Indazoles; Inflammation; Mice; Protein Kinase Inhibitors; Pyrazines; Syk Kinase | 2018 |
Targeting Serotonin 2A and Adrenergic α
Topics: Animals; Drug Discovery; Indazoles; Intraocular Pressure; Ocular Hypertension; Pyrazines; Rats; Receptor, Serotonin, 5-HT2A; Receptors, Adrenergic, alpha-1; Structure-Activity Relationship | 2018 |
SYK inhibitor entospletinib prevents ocular and skin GVHD in mice.
Topics: Administration, Oral; Animals; B-Lymphocytes; Disease Models, Animal; Drug Evaluation, Preclinical; Eye; Female; Graft vs Host Disease; Hematopoietic Stem Cell Transplantation; Humans; Indazoles; Mice; Protein Kinase Inhibitors; Pyrazines; Skin; Survival Analysis; Syk Kinase; T-Lymphocytes; Treatment Outcome | 2018 |
Resistance Mechanisms to SYK Inhibition in Acute Myeloid Leukemia.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Cell Line, Tumor; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Diphenylamine; Drug Resistance, Neoplasm; Drug Synergism; Female; Gene Expression Regulation, Leukemic; Humans; Indazoles; Leukemia, Myeloid, Acute; MAP Kinase Signaling System; Mice; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase Kinases; Mutagenesis, Site-Directed; Mutation; Open Reading Frames; Primary Cell Culture; Protein Kinase Inhibitors; Protein Tyrosine Phosphatase, Non-Receptor Type 11; Pyrazines; Syk Kinase; Xenograft Model Antitumor Assays | 2020 |
SYK Targeting Represents a Potential Therapeutic Option for Relapsed Resistant Pediatric
Topics: Aminopyridines; Cell Proliferation; Child; Core Binding Factor Alpha 2 Subunit; Cyclohexylamines; Drug Resistance, Neoplasm; Humans; Indazoles; Morpholines; Neoplasm Recurrence, Local; Oncogene Proteins, Fusion; Oxazines; Precursor B-Cell Lymphoblastic Leukemia-Lymphoma; Protein Kinase Inhibitors; Pyrazines; Pyridines; Pyrimidines; Syk Kinase; Tumor Cells, Cultured | 2019 |
Combinatorial efficacy of entospletinib and chemotherapy in patient-derived xenograft models of infant acute lymphoblastic leukemia.
Topics: Animals; Heterografts; Humans; Indazoles; Infant; Myeloid-Lymphoid Leukemia Protein; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Pyrazines | 2021 |
Pan- and Isoform-specific Inhibition of the Bromodomain and Extra-terminal Proteins and Evaluation of Synergistic Potential With Entospletinib in Canine Lymphoma.
Topics: Animals; Cell Line, Tumor; Dogs; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, 4 or More Rings; Indazoles; Lymphoma, Large B-Cell, Diffuse; Nuclear Proteins; Piperazines; Protein Isoforms; Protein Serine-Threonine Kinases; Pyrazines; Pyrazoles; Pyridazines; Syk Kinase | 2020 |
Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome.
Topics: Agammaglobulinaemia Tyrosine Kinase; Dose-Response Relationship, Drug; Humans; Indazoles; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-bcr; Pyrazines; Signal Transduction; Syk Kinase | 2020 |
Precursor B-ALL Cell Lines Differentially Respond to SYK Inhibition by Entospletinib.
Topics: Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Flow Cytometry; Gene Expression Regulation, Leukemic; Humans; Indazoles; Precursor B-Cell Lymphoblastic Leukemia-Lymphoma; Precursor Cells, B-Lymphoid; Pyrazines; Sequence Analysis, RNA; Syk Kinase | 2021 |
Entospletinib and obinutuzumab in patients with relapsed/refractory chronic lymphocytic leukemia and B-cell malignancies.
Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; B-Lymphocytes; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Pyrazines | 2021 |
Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer.
Topics: Aminopyridines; Aniline Compounds; Animals; Apoptosis; Benzamides; Carbazoles; Cell Line; Cell Survival; Crizotinib; Drug Resistance, Neoplasm; Enzyme Inhibitors; Humans; Immunoblotting; Indazoles; Lactams; Lactams, Macrocyclic; Lung Neoplasms; Mice; Mice, Inbred BALB C; Molecular Dynamics Simulation; Neoplasm Recurrence, Local; Piperidines; Proto-Oncogene Proteins; Pyrazines; Pyrazoles; Receptor Protein-Tyrosine Kinases | 2021 |