Page last updated: 2024-09-05

lapatinib and su 11248

lapatinib has been researched along with su 11248 in 47 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(su 11248)
Trials
(su 11248)
Recent Studies (post-2010) (su 11248)
1,9193051,4424,3385603,200

Protein Interaction Comparison

ProteinTaxonomylapatinib (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 (47)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's11 (23.40)29.6817
2010's34 (72.34)24.3611
2020's2 (4.26)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
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
Morphy, R1
Russu, WA; Shallal, HM1
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Chen, G; Chen, S; Chen, Y; Ding, J; Meng, L; Tong, L; Wang, J; Wang, X; Xie, Y; Yang, C1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Cantin, LD; Chen, H; Kenna, JG; Noeske, T; Stahl, S; Walker, CL; Warner, DJ1
Debnath, B; Ding, J; Kazemi, R; Long, YQ; Neamati, N; Odde, S; Sanchez, TW; Wang, Y; Xie, H; Xu, S; Xu, ZL; Yang, LM; Zeng, LF; Zheng, YT1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Bailey-Downs, LC; Bastian, A; Disch, BC; Dybdal-Hargreaves, NF; Gangjee, A; Hamel, E; Ihnat, M; Mooberry, SL; Raghavan, S; Rohena, CC; Thorpe, JE; Zhang, X1
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
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR1
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
Itkin, M; Kabir, M; Mathé, EA; Nguyễn, ÐT; Padilha, EC; Shah, P; Shinn, P; Siramshetty, V; Wang, AQ; Williams, J; Xu, X; Yu, KR; Zhao, T1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Saito, Y; Suzuki, Y; Tokuda, Y1
Hampton, T1
Bankhead, C1
Force, T; Krause, DS; Van Etten, RA1
Giordano, S; Petrelli, A1
Nahleh, ZA1
Decosterd, LA; Duchosal, MA; Haouala, A; Leyvraz, S; Montemurro, M; Ris, HB; Rochat, B; Widmer, N; Zaman, K; Zanolari, B1
Argyriou, AA; Dimitrakopoulos, F; Dimitropoulos, K; Giannopoulou, E; Kalofonos, HP; Koutras, AK1
Gelderblom, H; Guchelaar, HJ; van Erp, NP1
Berros, JP; Blay, P; Corral, N; Esteban, E; Estrada, E; Fernández, Y; Fonseca, PJ; Fra, J; Izquierdo, M; Lacave, ÁJ; Luque, M; Muriel, C; Pardo, P; Sanmamed, M; Vieitez, JM; Villanueva, N1
Catalano, O; De Giuli, L; Della Porta, MG; Eleuteri, E; Riccardi, A; Tondini, C; Zambelli, A1
Argyriou, AA; Dimitropoulos, K; Giannopoulou, E; Kalofonos, HP; Petsas, T; Tsiata, E; Zolota, V1
Addeo, R; Caraglia, M1
Cortes, J; Roché, H1
Barrière, J; Janus, N; Launay-Vacher, V; Thariat, J1
Andriamanana, I; Duretz, B; Gana, I; Hulin, A1
Behera, R; Mensa-Wilmot, K; Thomas, SM1
Basaran, G; Cabuk, D; Dane, F; Korkmaz, T; Seber, S; Telli, F; Teomete, M; Turhal, S; Yumuk, PF1
Croft, SL; Sanderson, L; Yardley, V1
Crews, LA; Gonzales, T; Kouznetsova, VL; Masliah, E; Overk, CR; Patrick, C; Paulino, A; Price, D; Rockenstein, E; Stocking, E; Tsigelny, IF; Wrasidlo, W1
Abdullaev, Z; Beadling, C; Berman, A; Carter, CA; Corless, CL; Doyle, A; Giaccone, G; Guha, U; Kelly, R; Killian, K; Lau, CC; Liewehr, DJ; Lopez-Chavez, A; Meltzer, PS; Morrow, B; Pack, S; Raffeld, M; Rajan, A; Sandler, A; Steinberg, SM; Szabo, E; Thomas, A; Wang, Y; Warrick, A; Xi, L1
Briley, LP; du Bois, A; Johnson, T; Parham, LR; Russo, M; Song, K; Spraggs, CF; Tada, H; Xu, CF1
Chen, YC; Chin, SY; Chou, CL; Jiang, MC; Lee, WR; Liu, KH; Shen, SC; Shih, YH; Tseng, JT1
Jiang, M; Liu, TT; Shen, GF; Shi, JH; Wang, Q1
Brunelli, C; Carbone, F; Di Iorio, C; Gigli, L; Montecucco, F; Nencioni, A; Rosa, GM; Tagliasacchi, MI1
Diao, Y; Gao, N; Jiang, W; Jin, G; Jin, Z; Li, W; Liu, Y; Wang, X; Wang, Z; Zhong, J1
Dekker, H; Labots, M; Meijer, GA; Pham, TV; Ruijter, R; Van der Hoeven, JJM; Van der Mijn, JC; Van der Vliet, HJ; Verheul, HMW1
Boswell, SA; Erickson, AR; Everley, RA; Haigis, MC; Holton, KM; Jacobson, CA; Maliszewski, L; Palmer, AC; Ringel, AE; Ron-Harel, N; Sheehan, RP; Sorger, PK; Wang, H1

Reviews

12 review(s) available for lapatinib 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
Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability.
    Bioorganic & medicinal chemistry, 2022, 02-15, Volume: 56

    Topics: Administration, Oral; Animals; Betamethasone; Biological Availability; Caco-2 Cells; Cell Membrane Permeability; Cells, Cultured; Dexamethasone; Dogs; Dose-Response Relationship, Drug; Humans; Hydrogen-Ion Concentration; Madin Darby Canine Kidney Cells; Mice; Molecular Structure; Neural Networks, Computer; Ranitidine; Rats; Structure-Activity Relationship; Verapamil

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
[Molecular-targeted agents in breast cancer].
    Gan to kagaku ryoho. Cancer & chemotherapy, 2006, Volume: 33, Issue:6

    Topics: Adult; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Bevacizumab; Breast Neoplasms; Chemotherapy, Adjuvant; Clinical Trials as Topic; Docetaxel; Drug Administration Schedule; Drug Delivery Systems; Female; Humans; Indoles; Lapatinib; Middle Aged; Paclitaxel; Pyrroles; Quinazolines; Randomized Controlled Trials as Topic; Receptor, ErbB-2; Sunitinib; Taxoids; Trastuzumab

2006
Molecular mechanisms of cardiotoxicity of tyrosine kinase inhibition.
    Nature reviews. Cancer, 2007, Volume: 7, Issue:5

    Topics: Adaptor Proteins, Signal Transducing; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Benzenesulfonates; Drug Delivery Systems; Enzyme Inhibitors; Heart; Heart Diseases; Humans; Indoles; Lapatinib; Models, Biological; Neoplasms; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-abl; Pyridines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Trastuzumab

2007
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
Molecularly targeted therapy in breast cancer: the new generation.
    Recent patents on anti-cancer drug discovery, 2008, Volume: 3, Issue:2

    Topics: Antineoplastic Agents; Breast Neoplasms; Drug Design; Female; Humans; Indoles; Lapatinib; Protein Kinase Inhibitors; Pyrroles; Quinazolines; Receptors, Estrogen; Sunitinib

2008
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
Predicting and preventing cardiotoxicity in the era of breast cancer targeted therapies. Novel molecular tools for clinical issues.
    Breast (Edinburgh, Scotland), 2011, Volume: 20, Issue:2

    Topics: Angiogenesis Inhibitors; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Biomarkers; Breast Neoplasms; Cardiotoxins; Cardiovascular Diseases; Female; Heart Failure; Humans; Indoles; Lapatinib; Molecular Targeted Therapy; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyridines; Pyrroles; Quinazolines; Risk Assessment; Sorafenib; Sunitinib; Trastuzumab

2011
Docetaxel combined with targeted therapies in metastatic breast cancer.
    Cancer treatment reviews, 2012, Volume: 38, Issue:5

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Bevacizumab; Breast Neoplasms; Disease-Free Survival; Docetaxel; Erlotinib Hydrochloride; Female; Humans; Indoles; Lapatinib; Pyrroles; Quinazolines; Sunitinib; Taxoids; Trastuzumab

2012
Update on cardiotoxicity of anti-cancer treatments.
    European journal of clinical investigation, 2016, Volume: 46, Issue:3

    Topics: Anthracyclines; Antineoplastic Agents; Antineoplastic Agents, Alkylating; Bevacizumab; Cardiotoxicity; Echocardiography; Humans; Indoles; Lapatinib; Magnetic Resonance Imaging; Neoplasms; Positron-Emission Tomography; Pyrroles; Quinazolines; Radiation Injuries; Radiotherapy; Sunitinib; Taxoids; Trastuzumab; Troponin; Vinca Alkaloids

2016

Trials

1 trial(s) available for lapatinib and su 11248

ArticleYear
Molecular profiling and targeted therapy for advanced thoracic malignancies: a biomarker-derived, multiarm, multihistology phase II basket trial.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2015, Mar-20, Volume: 33, Issue:9

    Topics: Adolescent; Adult; Aged; Benzimidazoles; Biomarkers, Tumor; Carcinoma, Non-Small-Cell Lung; Class I Phosphatidylinositol 3-Kinases; ErbB Receptors; Erlotinib Hydrochloride; Female; Genes, ras; Humans; Indoles; Lapatinib; Lung Neoplasms; Male; Middle Aged; Molecular Targeted Therapy; Mutation; Phosphatidylinositol 3-Kinases; Protein Kinase Inhibitors; Proto-Oncogene Proteins B-raf; PTEN Phosphohydrolase; Pyrroles; Quinazolines; ras Proteins; Reproducibility of Results; Small Cell Lung Carcinoma; Sunitinib; Thymus Neoplasms; Treatment Outcome; Young Adult

2015

Other Studies

34 other study(ies) available for lapatinib 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 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
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
FDA-approved drug labeling for the study of drug-induced liver injury.
    Drug discovery today, 2011, Volume: 16, Issue:15-16

    Topics: Animals; Benchmarking; Biomarkers, Pharmacological; Chemical and Drug Induced Liver Injury; Drug Design; Drug Labeling; Drug-Related Side Effects and Adverse Reactions; Humans; Pharmaceutical Preparations; Reproducibility of Results; United States; United States Food and Drug Administration

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
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
    Bioorganic & medicinal chemistry letters, 2012, Jan-01, Volume: 22, Issue:1

    Topics: Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Furans; Humans; Inhibitory Concentration 50; Morpholines; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Pyridines; Pyrimidines

2012
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
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:12

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Bile Acids and Salts; Cell Line; Chemical and Drug Induced Liver Injury; Humans; Quantitative Structure-Activity Relationship

2012
Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
    Journal of medicinal chemistry, 2012, Nov-26, Volume: 55, Issue:22

    Topics: Antineoplastic Agents; Drug Design; HIV Infections; HIV Integrase; HIV Integrase Inhibitors; HIV-1; Humans; Models, Molecular; Molecular Structure; Naphthyridines; Neoplasms; Structure-Activity Relationship; Tumor Cells, Cultured; Virus Integration

2012
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
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
    Bioorganic & medicinal chemistry, 2014, Jul-15, Volume: 22, Issue:14

    Topics: Aniline Compounds; Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Female; HeLa Cells; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Microtubules; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Receptor Protein-Tyrosine Kinases; Solubility; Structure-Activity Relationship; Water

2014
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
Highly predictive and interpretable models for PAMPA permeability.
    Bioorganic & medicinal chemistry, 2017, 02-01, Volume: 25, Issue:3

    Topics: Artificial Intelligence; Caco-2 Cells; Cell Membrane Permeability; Humans; Models, Biological; Organic Chemicals; Regression Analysis; Support Vector Machine

2017
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
Trials probe new agents for kidney cancer.
    JAMA, 2006, Jul-12, Volume: 296, Issue:2

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Carcinoma, Renal Cell; Clinical Trials as Topic; Humans; Indoles; Kidney Neoplasms; Lapatinib; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyridines; Pyrroles; Quinazolines; Sirolimus; Sorafenib; Sunitinib

2006
Three new drugs available to fight kidney cancer.
    Journal of the National Cancer Institute, 2006, Sep-06, Volume: 98, Issue:17

    Topics: Animals; Antineoplastic Agents; Carcinoma, Renal Cell; Disease-Free Survival; Humans; Indoles; Interferon-alpha; Kidney Neoplasms; Lapatinib; Multicenter Studies as Topic; Platelet-Derived Growth Factor; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrroles; Quinazolines; Randomized Controlled Trials as Topic; Sirolimus; Sunitinib; Treatment Outcome; Vascular Endothelial Growth Factor A

2006
New hope for RCC patients.
    European journal of cancer (Oxford, England : 1990), 2006, Volume: 42, Issue:12

    Topics: Antineoplastic Agents; Carcinoma, Renal Cell; Humans; Indoles; Kidney Neoplasms; Lapatinib; Pyrroles; Quinazolines; Sirolimus; Sunitinib

2006
Therapeutic Drug Monitoring of the new targeted anticancer agents imatinib, nilotinib, dasatinib, sunitinib, sorafenib and lapatinib by LC tandem mass spectrometry.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2009, Jul-15, Volume: 877, Issue:22

    Topics: Antineoplastic Agents; Benzamides; Benzenesulfonates; Chromatography, Liquid; Dasatinib; Drug Monitoring; Humans; Imatinib Mesylate; Indoles; Lapatinib; Neoplasms; Niacinamide; Phenylurea Compounds; Piperazines; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Tandem Mass Spectrometry; Thiazoles

2009
An in vitro study, evaluating the effect of sunitinib and/or lapatinib on two glioma cell lines.
    Investigational new drugs, 2010, Volume: 28, Issue:5

    Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Movement; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Glioma; Humans; Indoles; Lapatinib; Matrix Metalloproteinase 2; Matrix Metalloproteinase 9; Pyrroles; Quinazolines; Sunitinib

2010
Impact of the incorporation of tyrosine kinase inhibitor agents on the treatment of patients with a diagnosis of advanced renal cell carcinoma: study based on experience at the Hospital Universitario Central de Asturias.
    Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, 2010, Volume: 12, Issue:8

    Topics: Adult; Aged; Angiogenesis Inhibitors; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Carcinoma, Renal Cell; Disease-Free Survival; Drug Therapy, Combination; Female; Humans; Immunologic Factors; Indoles; Interferon-alpha; Interleukin-2; Kaplan-Meier Estimate; Kidney Neoplasms; Lapatinib; Male; Middle Aged; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyridines; Pyrroles; Quinazolines; Retrospective Studies; Sorafenib; Sunitinib; Treatment Outcome

2010
The effects of anti-VEGFR and anti-EGFR agents on glioma cell migration through implication of growth factors with integrins.
    Anticancer research, 2010, Volume: 30, Issue:12

    Topics: Cell Line, Tumor; Cell Movement; ErbB Receptors; Focal Adhesion Kinase 1; Glioblastoma; Humans; Indoles; Integrin beta1; Integrin beta3; Integrins; Lapatinib; Protein Kinase Inhibitors; Pyrroles; Quinazolines; Sunitinib; Vascular Endothelial Growth Factor Receptor-1

2010
The oral tyrosine kinase inhibitors lapatinib and sunitinib: new opportunities for the treatment of brain metastases from breast cancer?
    Expert review of anticancer therapy, 2011, Volume: 11, Issue:2

    Topics: Antineoplastic Agents; Brain Neoplasms; Breast Neoplasms; Female; Humans; Indoles; Lapatinib; Protein Kinase Inhibitors; Pyrroles; Quinazolines; Sunitinib

2011
[Renal tolerance of targeted therapies].
    Bulletin du cancer, 2012, Mar-01, Volume: 99, Issue:3

    Topics: Antibodies, Monoclonal; Benzenesulfonates; Boronic Acids; Bortezomib; Erlotinib Hydrochloride; Glomerulonephritis; Humans; Indoles; Kidney; Kidney Tubules; Lapatinib; Molecular Targeted Therapy; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyrazines; Pyridines; Pyrroles; Quinazolines; Sirolimus; Sorafenib; Sunitinib

2012
Simultaneous analysis of anticancer agents bortezomib, imatinib, nilotinib, dasatinib, erlotinib, lapatinib, sorafenib, sunitinib and vandetanib in human plasma using LC/MS/MS.
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2013, May-01, Volume: 926

    Topics: Antineoplastic Agents; Benzamides; Boronic Acids; Bortezomib; Chromatography, Liquid; Dasatinib; Erlotinib Hydrochloride; Humans; Imatinib Mesylate; Indoles; Lapatinib; Niacinamide; Phenylurea Compounds; Piperazines; Piperidines; Pyrazines; Pyrimidines; Pyrroles; Quinazolines; Reproducibility of Results; Sorafenib; Sunitinib; Tandem Mass Spectrometry; Thiazoles

2013
New chemical scaffolds for human african trypanosomiasis lead discovery from a screen of tyrosine kinase inhibitor drugs.
    Antimicrobial agents and chemotherapy, 2014, Volume: 58, Issue:4

    Topics: Animals; Axitinib; Benzamides; Erlotinib Hydrochloride; Female; HeLa Cells; Humans; Imatinib Mesylate; Imidazoles; Indazoles; Indoles; Lapatinib; Mice; Morpholines; Piperazines; Protein Kinase Inhibitors; Purines; Pyrimidines; Pyrroles; Quinazolines; Sunitinib; Trypanosomiasis, African

2014
Clinical outcome of Turkish metastatic breast cancer patients with currently available treatment modalities--single center experience.
    Asian Pacific journal of cancer prevention : APJCP, 2014, Volume: 15, Issue:1

    Topics: Adult; Aged; Aged, 80 and over; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Aromatase Inhibitors; Breast Neoplasms; Carcinoma, Ductal, Breast; Disease-Free Survival; Female; Follow-Up Studies; Humans; Indoles; Kaplan-Meier Estimate; Lapatinib; Middle Aged; Neoplasm Metastasis; Postmenopause; Premenopause; Pyrroles; Quinazolines; Receptor, ErbB-2; Receptors, Estrogen; Receptors, Progesterone; Retrospective Studies; Sunitinib; Survival Rate; Trastuzumab; Turkey; Young Adult

2014
Activity of anti-cancer protein kinase inhibitors against Leishmania spp.
    The Journal of antimicrobial chemotherapy, 2014, Volume: 69, Issue:7

    Topics: Animals; Antineoplastic Agents; Antiprotozoal Agents; Disease Models, Animal; Drug Repositioning; Indoles; Inhibitory Concentration 50; Lapatinib; Leishmania; Leishmaniasis; Mice, Inbred BALB C; Niacinamide; Phenylurea Compounds; Protein Kinase Inhibitors; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Treatment Outcome

2014
Neuroprotective effects of the anti-cancer drug sunitinib in models of HIV neurotoxicity suggests potential for the treatment of neurodegenerative disorders.
    British journal of pharmacology, 2014, Volume: 171, Issue:24

    Topics: AIDS Dementia Complex; Animals; Antineoplastic Agents; Cyclin-Dependent Kinase 5; Dasatinib; Erlotinib Hydrochloride; Flavonoids; HIV Envelope Protein gp120; In Vitro Techniques; Indoles; Lapatinib; Mice; Mice, Transgenic; Neurodegenerative Diseases; Neurons; Neuroprotective Agents; Protein Kinase Inhibitors; Purines; Pyrimidines; Pyrroles; Quinazolines; Rats; Roscovitine; Sunitinib; Thiazoles

2014
Different effects of the BIM deletion polymorphism on treatment of solid tumors by the tyrosine kinase inhibitors (TKI) pazopanib, sunitinib, and lapatinib.
    Annals of oncology : official journal of the European Society for Medical Oncology, 2015, Volume: 26, Issue:7

    Topics: Angiogenesis Inhibitors; Apoptosis Regulatory Proteins; Bcl-2-Like Protein 11; Gene Deletion; Humans; Indazoles; Indoles; Lapatinib; Membrane Proteins; Neoplasms; Polymorphism, Genetic; Prognosis; Prospective Studies; Protein Kinase Inhibitors; Proto-Oncogene Proteins; Pyrimidines; Pyrroles; Quinazolines; Signal Transduction; Sulfonamides; Sunitinib

2015
Early decline in serum phospho-CSE1L levels in vemurafenib/sunitinib-treated melanoma and sorafenib/lapatinib-treated colorectal tumor xenografts.
    Journal of translational medicine, 2015, Jun-13, Volume: 13

    Topics: Animals; Antibodies, Neoplasm; Cell Line, Tumor; Cell Proliferation; Cellular Apoptosis Susceptibility Protein; Colorectal Neoplasms; Extracellular Signal-Regulated MAP Kinases; Humans; Indoles; Lapatinib; Male; Melanoma; Mice, Inbred NOD; Mice, SCID; Niacinamide; Phenylurea Compounds; Phosphorylation; Pyrroles; Quinazolines; Sorafenib; Sulfonamides; Sunitinib; Vemurafenib; Xenograft Model Antitumor Assays

2015
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
Immunomodulatory and Antitumor Effects of a Novel TLR7 Agonist Combined with Lapatinib.
    Scientific reports, 2016, 12-21, Volume: 6

    Topics: Adenine; Animals; Antineoplastic Agents; Bone Marrow Cells; Cell Line; Dendritic Cells; Female; Immunotherapy; Indoles; Lapatinib; Lymphocytes; Membrane Glycoproteins; Mice; Mice, Inbred BALB C; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrroles; Quinazolines; Spleen; Succinates; Sunitinib; Toll-Like Receptor 7

2016
Selection of Protein Kinase Inhibitors Based on Tumor Tissue Kinase Activity Profiles in Patients with Refractory Solid Malignancies: An Interventional Molecular Profiling Study.
    The oncologist, 2018, Volume: 23, Issue:10

    Topics: Adult; Aged; Antineoplastic Agents; Dasatinib; Erlotinib Hydrochloride; Everolimus; Female; Humans; Lapatinib; Male; Middle Aged; Neoplasms; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Sorafenib; Sunitinib

2018
Adaptation of Human iPSC-Derived Cardiomyocytes to Tyrosine Kinase Inhibitors Reduces Acute Cardiotoxicity via Metabolic Reprogramming.
    Cell systems, 2019, 05-22, Volume: 8, Issue:5

    Topics: Acclimatization; Antineoplastic Agents; Cardiotoxicity; Cell Differentiation; Cells, Cultured; Erlotinib Hydrochloride; Gene Expression Profiling; Humans; Induced Pluripotent Stem Cells; Lapatinib; Myocytes, Cardiac; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Signal Transduction; Sorafenib; Sunitinib

2019