Page last updated: 2024-09-03

gefitinib and su 11248

gefitinib has been researched along with su 11248 in 44 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(su 11248)
Trials
(su 11248)
Recent Studies (post-2010) (su 11248)
5,2315662,9194,3385603,200

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)su 11248 (IC50)
Serine/threonine-protein kinase Chk1Homo sapiens (human)0.0773
Aurora kinase AHomo sapiens (human)1.837
Solute carrier family 22 member 1 Homo sapiens (human)6.1
NUAK family SNF1-like kinase 1Homo sapiens (human)0.048
Serine/threonine-protein kinase PAK 4Homo sapiens (human)0.5692
Serine/threonine-protein kinase Chk2Homo sapiens (human)0.0168
Tyrosine-protein kinase ABL1Homo sapiens (human)0.8423
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)0.555
Epidermal growth factor receptorHomo sapiens (human)0.48
Platelet-derived growth factor receptor betaMus musculus (house mouse)0.0186
Insulin receptorHomo sapiens (human)3.2
Tyrosine-protein kinase LckHomo sapiens (human)0.0089
Macrophage colony-stimulating factor 1 receptorHomo sapiens (human)0.0888
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)0.35
Hepatocyte growth factor receptorHomo sapiens (human)4.0002
Tyrosine-protein kinase HCKHomo sapiens (human)0.19
Platelet-derived growth factor receptor betaHomo sapiens (human)0.211
Mast/stem cell growth factor receptor KitHomo sapiens (human)0.2639
Fibroblast growth factor receptor 1Homo sapiens (human)1.4228
AromataseHomo sapiens (human)0.018
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)0.2764
Platelet-derived growth factor receptor alphaHomo sapiens (human)0.061
Translocator proteinRattus norvegicus (Norway rat)0.039
Vascular endothelial growth factor receptor 1 Homo sapiens (human)0.0457
AcetylcholinesteraseHomo sapiens (human)5.87
Platelet-derived growth factor receptor alpha Mus musculus (house mouse)0.0186
Tyrosine-protein kinase receptor UFOHomo sapiens (human)0.009
G protein-coupled receptor kinase 5Homo sapiens (human)0.83
Vascular endothelial growth factor receptor 3Homo sapiens (human)0.0089
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.1116
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)0.0581
Casein kinase I isoform alphaHomo sapiens (human)0.001
Ribosomal protein S6 kinase alpha-3Homo sapiens (human)0.1839
5'-AMP-activated protein kinase catalytic subunit alpha-2Homo sapiens (human)0.0617
Mu-type opioid receptorCavia porcellus (domestic guinea pig)0.018
Angiopoietin-1 receptorHomo sapiens (human)0.018
Focal adhesion kinase 1Homo sapiens (human)1.6
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)3.8389
5'-AMP-activated protein kinase catalytic subunit alpha-1Homo sapiens (human)0.158
Ribosomal protein S6 kinase alpha-1Homo sapiens (human)0.1313
AP2-associated protein kinase 1Homo sapiens (human)0.0462
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)0.0215
Aurora kinase BHomo sapiens (human)1.5
Serine/threonine-protein kinase TBK1Homo sapiens (human)0.22
ALK tyrosine kinase receptorHomo sapiens (human)1.1773
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)3

Research

Studies (44)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's16 (36.36)29.6817
2010's22 (50.00)24.3611
2020's6 (13.64)2.80

Authors

AuthorsStudies
Atteridge, CE; Azimioara, MD; Benedetti, MG; Biggs, WH; Carter, TA; Ciceri, P; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Galvin, M; Gerlach, JL; Grotzfeld, RM; Herrgard, S; Insko, DE; Insko, MA; Lai, AG; Lélias, JM; Lockhart, DJ; Mehta, SA; Milanov, ZV; Patel, HK; Treiber, DK; Velasco, AM; Wodicka, LM; Zarrinkar, PP1
Bullock, AN; Fedorov, O; Knapp, S; Marsden, B; Müller, S; Pogacic, V; Rellos, P; Schwaller, J; Sundström, M1
Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Aizenstein, B; Apsel, B; Blair, JA; Feldman, ME; Gonzalez, B; Hoffman, R; Knight, ZA; Nazif, TM; Shokat, KM; Williams, RL1
Morphy, R1
Russu, WA; Shallal, HM1
Dubey, PK; Pal, M; Piedrafita, FJ; Rajitha, C; Sunku, V; Veeramaneni, VR1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Brinkjost, T; Ehrt, C; Koch, O1
Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP1
Bharate, SB; Raghuvanshi, R1
Caballero, E; García-Cárceles, J; Gil, C; Martínez, A1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Shiotsu, Y1
Broxterman, HJ; Georgopapadakou, NH1
Cooney, MM; Remick, SC; Vogelzang, NJ1
Borner, MM1
Curtiss, FR1
Giordano, S; Petrelli, A1
Burgin, S; Heidary, N; Naik, H1
Dreyer, C; Faivre, S; Raymond, E1
Dziadziusko, R; Fennell, D; Gridelli, C; Lacombe, D; Pallis, AG; Serfass, L; van Meerbeeck, JP; Welch, J1
Gelderblom, H; Guchelaar, HJ; van Erp, NP1
Stang, JL; Tran, LM; Zhong, H1
Sherman, SI1
Baum, MS; Chen, I; Ginsberg, MS; Harmon, CS; Hudes, GR; Kim, ST; Motzer, RJ; Redman, BG1
Arango, BA; Cohen, EE; Perez, CA; Raez, LE; Santos, ES1
Cunningham, D; Yim, KL1
Cheng, H; Dicker, AP; Force, T; Kari, G; Koch, WJ; Rodeck, U1
Knecht, R; Kurzweg, T; Laban, S; Möckelmann, N1
Erdem, L; Giovannetti, E; Honeywell, R; Leon, LG; Peters, GJ1
Gallia, GL; Joshi, AD; Loilome, W; Riggins, GJ; Siu, IM; Tyler, B1
Chang, AY; Wang, M1
Ding, JF; Zhong, DF1
Jiang, M; Liu, TT; Shen, GF; Shi, JH; Wang, Q1
Chang, H; Kim, HS; Kim, JW; Lee, JS; Moon, SU; Sung, JH1
Chew, LJ; Edwards, J; Gallo, V; Ritter, J; Scafidi, J; Talbot, BM1
Bria, E; Cintoni, M; Gasbarrini, A; Mele, MC; Pompili, M; Ponziani, FR; Pozzo, C; Raoul, P; Rinninella, E; Strippoli, A; Tortora, G1
Hsia, S; Wang, H; Wu, CJ; Wu, TH1
Chen, Y; Ge, G; Hu, B; Ke, J; Liu, Q; Meng, Q; Sun, H; Tao, J; Wang, C; Wang, L; Wang, Y; Wei, T; Wu, J; Zhao, T1

Reviews

19 review(s) available for gefitinib and su 11248

ArticleYear
Selectively nonselective kinase inhibition: striking the right balance.
    Journal of medicinal chemistry, 2010, Feb-25, Volume: 53, Issue:4

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Discovery; Humans; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship

2010
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
    Drug discovery today, 2016, Volume: 21, Issue:4

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk

2016
Kinase Inhibitors as Underexplored Antiviral Agents.
    Journal of medicinal chemistry, 2022, 01-27, Volume: 65, Issue:2

    Topics: Animals; Antiviral Agents; Drug Repositioning; Humans; Protein Kinase Inhibitors; Virus Diseases; Viruses

2022
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells

2022
[Current screening for molecular target therapy of cancer].
    Gan to kagaku ryoho. Cancer & chemotherapy, 2003, Volume: 30, Issue:12

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Benzamides; Boronic Acids; Bortezomib; Drug Delivery Systems; Drug Screening Assays, Antitumor; Gefitinib; Heat-Shock Proteins; Humans; Imatinib Mesylate; Indoles; Lactones; Mice; Neoplasms; Phthalazines; Piperazines; Piperidines; Pyrazines; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sunitinib

2003
Novel agents for the treatment of advanced kidney cancer.
    Clinical advances in hematology & oncology : H&O, 2004, Volume: 2, Issue:10

    Topics: Angiogenesis Inhibitors; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Clinical Trials as Topic; Epothilones; Gefitinib; Humans; Indoles; Kidney Neoplasms; Lenalidomide; Neoplasm Staging; Niacinamide; Phenylurea Compounds; Pyridines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Thalidomide

2004
[Molecular targets in colon cancer].
    Therapeutische Umschau. Revue therapeutique, 2006, Volume: 63, Issue:4

    Topics: Angiogenesis Inhibitors; Antibiotics, Antineoplastic; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Benzamides; Camptothecin; Cetuximab; Clinical Trials as Topic; Clinical Trials, Phase II as Topic; Colonic Neoplasms; Drug Delivery Systems; ErbB Receptors; Gefitinib; Humans; Imatinib Mesylate; Indoles; Irinotecan; Organoplatinum Compounds; Oxaliplatin; Phthalazines; Piperazines; Platelet-Derived Growth Factor; Protein Kinase Inhibitors; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Quinolones; Receptors, Platelet-Derived Growth Factor; Receptors, Somatomedin; Signal Transduction; Sirolimus; Sunitinib

2006
From single- to multi-target drugs in cancer therapy: when aspecificity becomes an advantage.
    Current medicinal chemistry, 2008, Volume: 15, Issue:5

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Benzenesulfonates; Bevacizumab; Cetuximab; Clinical Trials as Topic; Enzyme Inhibitors; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Indoles; Lapatinib; Neoplasms; Neovascularization, Pathologic; Niacinamide; Phenylurea Compounds; Piperazines; Piperidines; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptor Protein-Tyrosine Kinases; Sorafenib; Sunitinib; Trastuzumab

2008
Chemotherapeutic agents and the skin: An update.
    Journal of the American Academy of Dermatology, 2008, Volume: 58, Issue:4

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antimetabolites; Antineoplastic Agents; Benzamides; Benzenesulfonates; Cetuximab; Drug Eruptions; Drug-Related Side Effects and Adverse Reactions; ErbB Receptors; Erlotinib Hydrochloride; Fusion Proteins, bcr-abl; Gefitinib; Hair Diseases; Humans; Imatinib Mesylate; Indoles; Mucous Membrane; Nail Diseases; Niacinamide; Phenylurea Compounds; Piperazines; Platinum Compounds; Proteasome Inhibitors; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Signal Transduction; Skin; Skin Diseases; Sorafenib; Sunitinib; Taxoids

2008
[Targeted therapies and their indications in solid neoplasias].
    La Revue de medecine interne, 2009, Volume: 30, Issue:5

    Topics: Angiogenesis Inhibitors; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Benzenesulfonates; Bevacizumab; ErbB Receptors; Erlotinib Hydrochloride; Everolimus; Gefitinib; Humans; Indoles; Kidney Neoplasms; Liver Neoplasms; Neoplasms; Niacinamide; Phenylurea Compounds; Pyridines; Pyrroles; Quinazolines; Receptor, ErbB-2; Receptors, Vascular Endothelial Growth Factor; Sirolimus; Sorafenib; Sunitinib; Vascular Endothelial Growth Factor A

2009
Targeted therapies in the treatment of advanced/metastatic NSCLC.
    European journal of cancer (Oxford, England : 1990), 2009, Volume: 45, Issue:14

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Carcinoma, Non-Small-Cell Lung; Cetuximab; Erlotinib Hydrochloride; Gefitinib; Humans; Indoles; Lung Neoplasms; Niacinamide; Phenylurea Compounds; Piperidines; Pyridines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Treatment Outcome

2009
Clinical pharmacokinetics of tyrosine kinase inhibitors.
    Cancer treatment reviews, 2009, Volume: 35, Issue:8

    Topics: Administration, Oral; Antineoplastic Agents; Benzamides; Benzenesulfonates; Biological Availability; Cytochrome P-450 Enzyme System; Dasatinib; Drug Interactions; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Indoles; Intestinal Absorption; Lapatinib; Niacinamide; Phenylurea Compounds; Piperazines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Thiazoles; Tissue Distribution

2009
Tyrosine kinase inhibitors and the thyroid.
    Best practice & research. Clinical endocrinology & metabolism, 2009, Volume: 23, Issue:6

    Topics: Axitinib; Benzenesulfonates; Clinical Trials as Topic; Gefitinib; Humans; Imidazoles; Indazoles; Indoles; Niacinamide; Oligonucleotides; Pharmaceutical Preparations; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins B-raf; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Sorafenib; Sulfonamides; Sunitinib; Thyroid Gland; Thyroid Neoplasms

2009
Novel molecular targeted therapies for refractory thyroid cancer.
    Head & neck, 2012, Volume: 34, Issue:5

    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
Targeted drug therapies and cancer.
    Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer, 2011, Volume: 185

    Topics: Antineoplastic Agents; Benzamides; Benzenesulfonates; Drug Delivery Systems; Erlotinib Hydrochloride; Gastrointestinal Neoplasms; Gefitinib; Humans; Imatinib Mesylate; Indoles; Niacinamide; Phenylurea Compounds; Piperazines; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptor Protein-Tyrosine Kinases; Signal Transduction; Sorafenib; Sunitinib; Vascular Endothelial Growth Factor A

2011
Current treatment options for recurrent/metastatic head and neck cancer: a post-ASCO 2011 update and review of last year's literature.
    European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery, 2012, Volume: 269, Issue:10

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzodioxoles; Carcinoma, Squamous Cell; Cetuximab; Combined Modality Therapy; Dasatinib; ErbB Receptors; Fluorouracil; Gefitinib; Head and Neck Neoplasms; Humans; Indoles; Neoplasm Recurrence, Local; Palliative Care; Pyrimidines; Pyrroles; Quinazolines; Quinazolinones; Salvage Therapy; Squamous Cell Carcinoma of Head and Neck; Sunitinib; Thiazoles

2012
Polymorphisms to predict outcome to the tyrosine kinase inhibitors gefitinib, erlotinib, sorafenib and sunitinib.
    Current topics in medicinal chemistry, 2012, Volume: 12, Issue:15

    Topics: Animals; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Clinical Trials as Topic; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Germ-Line Mutation; Humans; Indoles; Molecular Targeted Therapy; Neoplasm Proteins; Neoplasms; Niacinamide; Phenylurea Compounds; Polymorphism, Genetic; Predictive Value of Tests; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-akt; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Treatment Outcome

2012
[Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors].
    Yao xue xue bao = Acta pharmaceutica Sinica, 2013, Volume: 48, Issue:7

    Topics: Antineoplastic Agents; Crown Ethers; Cytochrome P-450 Enzyme System; Dasatinib; Drug Interactions; Erlotinib Hydrochloride; Gefitinib; Glucuronosyltransferase; Humans; Imatinib Mesylate; Indoles; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib

2013
Prognostic value of skeletal muscle mass during tyrosine kinase inhibitor (TKI) therapy in cancer patients: a systematic review and meta-analysis.
    Internal and emergency medicine, 2021, Volume: 16, Issue:5

    Topics: Gefitinib; Humans; Imatinib Mesylate; Indazoles; Muscle, Skeletal; Neoplasms; Phenylurea Compounds; Prognosis; Pyrazoles; Pyridines; Pyrimidines; Quinolines; Sorafenib; Sulfonamides; Sunitinib; Survival Analysis

2021

Trials

1 trial(s) available for gefitinib and su 11248

ArticleYear
Phase I/II trial of sunitinib plus gefitinib in patients with metastatic renal cell carcinoma.
    American journal of clinical oncology, 2010, Volume: 33, Issue:6

    Topics: Administration, Oral; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Renal Cell; Disease-Free Survival; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Follow-Up Studies; Gefitinib; Humans; Indoles; Kidney Neoplasms; Male; Maximum Tolerated Dose; Middle Aged; Neoplasm Staging; Pyrroles; Quinazolines; Sunitinib; Survival Analysis; Treatment Outcome

2010

Other Studies

24 other study(ies) available for gefitinib and su 11248

ArticleYear
A small molecule-kinase interaction map for clinical kinase inhibitors.
    Nature biotechnology, 2005, Volume: 23, Issue:3

    Topics: Benzamides; Drug Design; Escherichia coli; Escherichia coli Proteins; Imatinib Mesylate; Microchemistry; Pharmaceutical Preparations; Piperazines; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Pyrimidines

2005
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
    Proceedings of the National Academy of Sciences of the United States of America, 2007, Dec-18, Volume: 104, Issue:51

    Topics: Amino Acid Sequence; Binding Sites; Clinical Trials as Topic; Drug Evaluation, Preclinical; Enzyme Stability; Humans; Molecular Sequence Data; Phylogeny; Protein Array Analysis; Protein Conformation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases

2007
A quantitative analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2008, Volume: 26, Issue:1

    Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship

2008
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
    Nature chemical biology, 2008, Volume: 4, Issue:11

    Topics: Amino Acid Sequence; Antineoplastic Agents; Apoptosis; Blotting, Western; Catalytic Domain; Cell Proliferation; Cells, Cultured; Crystallography, X-Ray; Drug Delivery Systems; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Fusion Proteins, bcr-abl; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Molecular Structure; Phosphoinositide-3 Kinase Inhibitors; Protein Kinases; Protein Subunits; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Sequence Alignment; Signal Transduction; TOR Serine-Threonine Kinases

2008
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2011
Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:10

    Topics: Antineoplastic Agents; Benzene Derivatives; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Neoplasms; Oxazines; Structure-Activity Relationship

2011
Comprehensive analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2011, Oct-30, Volume: 29, Issue:11

    Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity

2011
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
    European journal of medicinal chemistry, 2013, Volume: 61

    Topics: Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Glycolipids; Humans; Membrane Proteins; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship

2013
Identification of potent Yes1 kinase inhibitors using a library screening approach.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship

2013
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
    Journal of medicinal chemistry, 2014, Oct-09, Volume: 57, Issue:19

    Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship

2014
Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.
    Journal of medicinal chemistry, 2016, 05-12, Volume: 59, Issue:9

    Topics: Binding Sites; Chemistry, Pharmaceutical; Drug Design; Models, Chemical; Proteins

2016
The target landscape of clinical kinase drugs.
    Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
    Journal of medicinal chemistry, 2022, 01-27, Volume: 65, Issue:2

    Topics: Antiviral Agents; COVID-19; COVID-19 Drug Treatment; Drug Approval; Drug Repositioning; High-Throughput Screening Assays; Humans; Protein Kinase Inhibitors; SARS-CoV-2; United States; United States Food and Drug Administration; Virus Diseases

2022
New cancer therapeutics: target-specific in, cytotoxics out?
    Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy, 2004, Volume: 7, Issue:2

    Topics: Antineoplastic Agents; Biomarkers, Tumor; Drug Delivery Systems; Enzyme Inhibitors; Gefitinib; Humans; Indoles; Intracellular Signaling Peptides and Proteins; Neoplasms; Proteomics; Pyrroles; Quinazolines; Sunitinib

2004
Pharmacy benefit spending on oral chemotherapy drugs.
    Journal of managed care pharmacy : JMCP, 2006, Volume: 12, Issue:7

    Topics: Administration, Oral; Ambulatory Care; Antineoplastic Agents; Benzamides; Benzenesulfonates; Capecitabine; Dasatinib; Deoxycytidine; Drug Costs; Employer Health Costs; Erlotinib Hydrochloride; Fluorouracil; Gefitinib; Health Benefit Plans, Employee; Humans; Imatinib Mesylate; Indoles; Insurance, Pharmaceutical Services; Lenalidomide; Neoplasms; Niacinamide; Phenylurea Compounds; Piperazines; Prescription Fees; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Thalidomide; Thiazoles; United States

2006
Induced-fit docking studies of the active and inactive states of protein tyrosine kinases.
    Journal of molecular graphics & modelling, 2009, Volume: 28, Issue:4

    Topics: Binding Sites; Crystallography, X-Ray; Enzyme Activation; ErbB Receptors; Gefitinib; Hydrogen Bonding; Indoles; Ligands; Models, Molecular; Oxindoles; Propionates; Protein Structure, Secondary; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-abl; Pyrroles; Quinazolines; Reproducibility of Results; Sunitinib

2009
A novel preclinical strategy for identifying cardiotoxic kinase inhibitors and mechanisms of cardiotoxicity.
    Circulation research, 2011, Dec-09, Volume: 109, Issue:12

    Topics: Animals; Animals, Genetically Modified; Apoptosis; Benzenesulfonates; Cardiotoxins; Cell Survival; Cells, Cultured; Extracellular Signal-Regulated MAP Kinases; Female; Gefitinib; Indoles; Male; Models, Animal; Myocytes, Cardiac; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; Proto-Oncogene Proteins c-raf; Pyridines; Pyrroles; Quinazolines; Rats; Rats, Sprague-Dawley; Signal Transduction; Sorafenib; Sunitinib; Zebrafish

2011
Evaluation of tyrosine kinase inhibitor combinations for glioblastoma therapy.
    PloS one, 2012, Volume: 7, Issue:10

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Brain Neoplasms; Cell Line, Tumor; Cell Proliferation; Drug Evaluation, Preclinical; Drug Synergism; Female; Gefitinib; Glioblastoma; Humans; Immunoblotting; Indoles; Inhibitory Concentration 50; Mice; Mice, Nude; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrroles; Quinazolines; Rats, Inbred F344; Spheroids, Cellular; Sunitinib; Treatment Outcome; Xenograft Model Antitumor Assays

2012
In-vitro growth inhibition of chemotherapy and molecular targeted agents in hepatocellular carcinoma.
    Anti-cancer drugs, 2013, Volume: 24, Issue:3

    Topics: Alanine; alpha-Fetoproteins; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzimidazoles; Carcinoma, Hepatocellular; Cetuximab; Dasatinib; Doxorubicin; Drug Screening Assays, Antitumor; Epothilones; Gefitinib; Humans; Indoles; Inhibitory Concentration 50; Liver Neoplasms; Niacinamide; Phenylurea Compounds; Piperidines; Pyridones; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Thiazoles; Triazines

2013
Spectroscopic and molecular docking studies of binding interaction of gefitinib, lapatinib and sunitinib with bovine serum albumin (BSA).
    Journal of photochemistry and photobiology. B, Biology, 2015, Volume: 153

    Topics: Animals; Binding Sites; Cattle; Circular Dichroism; Fluorescence Resonance Energy Transfer; Gefitinib; Indoles; Lapatinib; Molecular Docking Simulation; Protein Binding; Protein Structure, Tertiary; Pyrroles; Quinazolines; Serum Albumin, Bovine; Spectrophotometry, Ultraviolet; Spectroscopy, Fourier Transform Infrared; Sunitinib; Thermodynamics

2015
EGF Induced RET Inhibitor Resistance in CCDC6-RET Lung Cancer Cells.
    Yonsei medical journal, 2017, Volume: 58, Issue:1

    Topics: Adenocarcinoma; Cell Line, Tumor; Cetuximab; Drug Resistance, Neoplasm; Epidermal Growth Factor; ErbB Receptors; fms-Like Tyrosine Kinase 3; Gefitinib; Gene Rearrangement; Hepatocyte Growth Factor; Humans; Indoles; Lung Neoplasms; MAP Kinase Signaling System; Mutation; Niacinamide; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Proto-Oncogene Mas; Proto-Oncogene Proteins c-ret; Pyrroles; Quinazolines; RNA, Small Interfering; Signal Transduction; Sorafenib; Sunitinib

2017
Age-Dependent Cellular and Behavioral Deficits Induced by Molecularly Targeted Drugs Are Reversible.
    Cancer research, 2018, 04-15, Volume: 78, Issue:8

    Topics: Age Factors; Animals; Antineoplastic Agents; Behavior, Animal; Female; Gefitinib; Hippocampus; Male; Memory; Mice; Mice, Inbred C57BL; Molecular Targeted Therapy; Neurons; Oligodendroglia; Sirolimus; Sunitinib

2018
Fish Oil, Se Yeast, and Micronutrient-Enriched Nutrition as Adjuvant Treatment during Target Therapy in a Murine Model of Lung Cancer.
    Marine drugs, 2021, May-04, Volume: 19, Issue:5

    Topics: Administration, Oral; Animals; Apoptosis; Cachexia; Carcinoma, Lewis Lung; Cell Line, Tumor; Chemotherapy, Adjuvant; Disease Models, Animal; Epithelial-Mesenchymal Transition; Fish Oils; Gefitinib; Inflammation; Male; Mice, Inbred C57BL; Micronutrients; Neoplasm Metastasis; Oxidation-Reduction; Protein Kinase Inhibitors; Selenium; Sunitinib; Tumor Burden; Yeast, Dried

2021
In vitro Measurement and In vivo Prediction of Time-Dependent Inhibitory Effects of Three Tyrosine Kinase Inhibitors on CYP3A Activity.
    Current drug metabolism, 2021, Volume: 22, Issue:10

    Topics: Cytochrome P-450 CYP3A; Drug Interactions; Gefitinib; Humans; Hydroxytestosterones; Imatinib Mesylate; Inhibitory Concentration 50; Microsomes, Liver; Molecular Docking Simulation; Protein Kinase Inhibitors; Structure-Activity Relationship; Sunitinib

2021