Page last updated: 2024-09-05

lapatinib and hki 272

lapatinib has been researched along with hki 272 in 49 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(hki 272)
Trials
(hki 272)
Recent Studies (post-2010) (hki 272)
1,9193051,44228342248

Protein Interaction Comparison

ProteinTaxonomylapatinib (IC50)hki 272 (IC50)
Epidermal growth factor receptorHomo sapiens (human)0.0416
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.0298
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.8582
Serine/threonine-protein kinase Nek2Homo sapiens (human)0.274

Research

Studies (49)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (4.08)29.6817
2010's36 (73.47)24.3611
2020's11 (22.45)2.80

Authors

AuthorsStudies
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Bai, F; Jiang, H; Li, H; Liu, H; Liu, L; Liu, X; Tong, L; Wang, X; Xie, H; Zhao, Z; Zhou, W1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Abou El Ella, DA; Aly, RM; El-Motwally, AM; Ibrahim, DA1
Bedair, TM; Elkamhawy, A; Farag, AK; Lee, KT; Leem, DG; Pae, AN; Roh, EJ; Viswanath, AN1
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
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Basetti, V; Keesara, M; Maiti, P; Mansour, TS; Moghudula, AG; Pallepati, RR; Potluri, V1
Kabir, M; Kerns, E; Nguyen, K; Shah, P; Sun, H; Wang, Y; Xu, X; Yu, KR1
Bauer, S; Baumann, M; Becker, C; Grabe, T; Hardick, J; Hodson, L; Jeyakumar, K; Ketzer, J; Keul, M; Kirschner, T; Klövekorn, P; Lategahn, J; Müller, MP; Niggenaber, J; Rauh, D; Terheyden, S; Tumbrink, HL; Unger, A; van Otterlo, WAL; Weisner, J1
Amir, E; Ocaña, A1
Iwata, K; Yamashita, T1
Arnould, L; Coudert, B; Favier, L; Fumoleau, P; Guiu, S1
Pandiella, A; Sánchez-Martín, M1
Azim, HA; de Azambuja, E; Loi, S; Metzger-Filho, O; Piccart, M; Saini, KS; Sotiriou, C1
Chudenko, VA; Dashian, GA; Filatova, LV; Gershanovich, ML; Latipova, DKh; Luk'ianchikova, VS; Paltuev, RM; Semiglazov, VV; Semiglazova, TIu1
Awada, A; Bozovic-Spasojevic, I; Chow, L1
Amir, E; Bouganim, N; Clemons, M; Fralick, M; Hilton, JF1
Bozovic-Spasojevic, I; de Azambuja, E; Zardavas, D1
Aronson, AB; Bose, R; Ding, L; Ellis, MJ; Goel, N; Kavuri, SM; Koboldt, DC; Li, S; Ma, CX; Mardis, ER; Monsey, J; Searleman, AC; Shen, D; Shen, W1
Majem, M; Pallarès, C1
Aherne, ST; Clynes, M; Crown, J; Doolan, P; Madden, SF; O'Connor, R; O'Neill, F1
Awada, A; Bonneterre, J; Germa, C; Geyer, CE; Ito, Y; Kim, SB; Lang, I; Martin, M; Ro, J; Vermette, J; Wang, K1
Kümler, I; Nielsen, DL; Tuxen, MK1
Gyõrffy, B; Mihály, Z1
Beyer, WF; Gooden, D; Liu, L; Soderblom, EJ; Spector, NL; Toone, EJ; Walder, H; Xia, W; Zhao, S1
Breslin, S; Corcoran, C; Crown, J; Ghobrial, IM; Gogarty, M; O'Driscoll, L; Rani, S1
Baselga, J; Cortés, J; Garcia-Saenz, JA; Germa, C; Harb, W; Kiger, C; Kim, SB; Martin, M; Moroose, R; Pluard, T; Saura, C; Wang, K; Xu, B1
Di Luca, A; Henry, M; Meleady, P; O'Connor, R1
Arteaga, CL; Bose, R; Button, B; Chu, D; Cidado, J; Cimino-Mathews, A; Cochran, RL; Cravero, K; Croessmann, S; Dalton, WB; Erlanger, B; Kavuri, SM; Konstantopoulos, K; Kyker-Snowman, K; Lauring, J; Manto, KM; Park, BH; Parsons, HA; Red Brewer, M; Rosen, DM; Wong, HY; Yankaskas, CL; Zabransky, DJ1
Barlesi, F; Beau-Faller, M; Besse, B; Cappuzzo, F; Cortot, A; Dansin, E; Filleron, T; Fournel, P; Früh, M; Gautschi, O; Mazières, J; Milia, J; Monnet, I; Moro-Sibilot, D; Peters, S; Pless, M; Rosell, R; Westeel, V; Wislez, M1
Breslin, S; Lowry, MC; O'Driscoll, L1
Collins, DM; Crown, J; Davies, A; Edwards, C; Gately, K; Hughes, C; Madden, SF; O'Byrne, KJ; O'Donovan, N1
Bucher, E; Chin, K; Dane, M; Gray, JW; Heiser, LM; Jonas, O; Kilburn, D; Korkola, JE; Liby, T; Liu, M; Mills, GB; Nederlof, M; Smith, R; Sudar, D; Tatarova, Z; Thompson, W; Watson, SS; Whitman, M1
Duchnowska, R; Jassem, J; Loibl, S1
Browne, BC; Canonici, A; Collins, DM; Conlon, NT; Crown, J; Gaynor, N; Gullo, G; Ivers, L; O'Brien, NA; O'Donovan, N; Pedersen, K1
Barroso-Sousa, R; Pernas, S; Tolaney, SM1
Avogadri-Connors, F; Baselga, J; Berger, MF; Boni, V; Bryce, RP; Cai, Y; Chan, C; Chandarlapaty, S; Cocco, E; Cownie, J; Cutler, RE; Hyman, DM; Javier Carmona, F; Lalani, AS; Loi, S; Montemurro, F; Moriarty, A; Papadopoulos, KP; Razavi, P; Rossi, V; Sarotto, I; Savas, P; Scaltriti, M; Shifman, SG; Solit, DB; Soong, J; Toska, E; Wick, MJ; Won, HH1
Exman, P; Pernas, S; Tolaney, SM1
Díaz-Gil, L; Díaz-Rodríguez, E; Gandullo-Sánchez, L; Ocaña, A; Pandiella, A; Ríos-Luci, C1
Benonisson, H; Breukel, C; Brouwers, C; Camps, M; Claassens, J; Fransen, MF; Linssen, MM; Ossendorp, F; Sow, HS; van Hall, T; Verbeek, JS1
Gelmon, KA; Tesch, ME1
Bera, T; Das, A; Shetty, SR; Yeeravalli, R1
Cai, N; Cheng, K; Liang, H; Wen, J; Xiong, Y; Zhang, W; Zhang, Y; Zhu, J1
Collins, DM; Conlon, NT; Crown, J; Diala, I; Eli, LD; Kooijman, JJ; Lalani, AS; Mulder, WR; van Gerwen, SJC; Zaman, GJR1
Arribas, J; Chandarlapaty, S; de Stanchina, E; Ferraro, E; Kulick, A; Lahuerta, EJA; Li, Q; Morales, CB; Razavi, P; Reis-Filho, J; Rosen, N; Ross, D; Safonov, A; Smith, AE; Solit, DB1
Bachelot, T; Bailleux, C; Darlix, A; Jacot, W1
Bachelot, T; Carbonnaux, M; Dufresne, A; Heudel, PE; Mery, B; Toussaint, P; Trédan, O; Vanacker, H1
Dong, Z; Fang, Q; Wang, J; Wu, Y1

Reviews

17 review(s) available for lapatinib and hki 272

ArticleYear
Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.
    Cancer treatment reviews, 2009, Volume: 35, Issue:8

    Topics: Afatinib; Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Biomarkers, Tumor; Breast Neoplasms; Drug Resistance, Neoplasm; ErbB Receptors; Female; Forecasting; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Morpholines; Prognosis; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Quinolines; Trastuzumab; Up-Regulation

2009
[Management of metastatic HER2-positive breast cancer: present and future].
    Bulletin du cancer, 2010, Volume: 97, Issue:3

    Topics: Anastrozole; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Hormonal; Antineoplastic Combined Chemotherapy Protocols; Benzoquinones; Bevacizumab; Brain Neoplasms; Breast Neoplasms; Disease Progression; Female; Heart; Humans; Lactams, Macrocyclic; Lapatinib; Letrozole; Neoplasm Proteins; Nitriles; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab; Triazoles

2010
Beyond trastuzumab: new treatment options for HER2-positive breast cancer.
    Breast (Edinburgh, Scotland), 2011, Volume: 20 Suppl 3

    Topics: Adult; Antibodies, Monoclonal, Humanized; Belgium; Breast Neoplasms; Chemotherapy, Adjuvant; Clinical Trials, Phase II as Topic; Disease-Free Survival; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Resistance, Neoplasm; Female; Humans; Lapatinib; Middle Aged; Molecular Targeted Therapy; Neoadjuvant Therapy; Prognosis; Protein Kinase Inhibitors; Quinazolines; Quinolines; Randomized Controlled Trials as Topic; Receptor, ErbB-2; Risk Assessment; Survival Analysis; Trastuzumab

2011
[Novel target therapies used in breast cancer management].
    Voprosy onkologii, 2011, Volume: 57, Issue:5

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Biomarkers, Tumor; Breast Neoplasms; Female; Genes, BRCA1; Genes, BRCA2; Humans; Lapatinib; Molecular Targeted Therapy; Mutation; Poly(ADP-ribose) Polymerase Inhibitors; Protein Kinase Inhibitors; Quinazolines; Quinolines; RANK Ligand; Receptor, ErbB-2; Receptors, Estrogen; Trastuzumab

2011
New therapies in HER2-positive breast cancer: a major step towards a cure of the disease?
    Cancer treatment reviews, 2012, Volume: 38, Issue:5

    Topics: Afatinib; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Breast Neoplasms; Female; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2012
Dual blockade of HER2 - twice as good or twice as toxic?
    Clinical oncology (Royal College of Radiologists (Great Britain)), 2012, Volume: 24, Issue:9

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Breast Neoplasms; Drug Resistance, Neoplasm; Female; Humans; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2012
Dual human epidermal growth factor receptor 2 blockade: another step forward in treating patients with human epidermal growth factor receptor 2-positive breast cancer.
    Current opinion in oncology, 2012, Volume: 24, Issue:6

    Topics: Afatinib; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Clinical Trials as Topic; Female; Humans; Lapatinib; Molecular Targeted Therapy; Neoplasms, Hormone-Dependent; Quinazolines; Quinolines; Receptor, ErbB-2; Signal Transduction; Trastuzumab

2012
An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.
    Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, 2013, Volume: 15, Issue:5

    Topics: Afatinib; Aminoquinolines; Angiogenesis Inhibitors; Aniline Compounds; Carcinoma, Non-Small-Cell Lung; ErbB Receptors; Humans; Lapatinib; Lung Neoplasms; Molecular Targeted Therapy; Protein Kinase Inhibitors; Quinazolines; Quinolines

2013
A systematic review of dual targeting in HER2-positive breast cancer.
    Cancer treatment reviews, 2014, Volume: 40, Issue:2

    Topics: Ado-Trastuzumab Emtansine; Afatinib; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Biomarkers, Tumor; Breast Neoplasms; Clinical Trials as Topic; Disease-Free Survival; Everolimus; Female; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Maytansine; Molecular Targeted Therapy; Neoadjuvant Therapy; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Quinolines; Receptor, ErbB-2; Sirolimus; TOR Serine-Threonine Kinases; Trastuzumab; Treatment Outcome; Up-Regulation

2014
[HER2-positive breast cancer: available targeted agents and biomarkers for therapy response].
    Magyar onkologia, 2013, Volume: 57, Issue:3

    Topics: Ado-Trastuzumab Emtansine; Afatinib; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Bevacizumab; Biomarkers, Tumor; Breast Neoplasms; Clinical Trials as Topic; Everolimus; Female; Gene Amplification; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Maytansine; Molecular Targeted Therapy; Phosphoinositide-3 Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Quinazolines; Quinolines; Receptor, ErbB-2; Sirolimus; TOR Serine-Threonine Kinases; Trastuzumab

2013
Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer.
    Cancer treatment reviews, 2018, Volume: 67

    Topics: Afatinib; Brain Neoplasms; Breast Neoplasms; Female; Humans; Lapatinib; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Quinolines; Receptor, ErbB-2

2018
Optimal treatment of early stage HER2-positive breast cancer.
    Cancer, 2018, 12-01, Volume: 124, Issue:23

    Topics: Ado-Trastuzumab Emtansine; Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Immunological; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Chemotherapy, Adjuvant; Clinical Trials as Topic; Female; Humans; Lapatinib; Maytansine; Progression-Free Survival; Quinolines; Receptor, ErbB-2; Trastuzumab; Treatment Outcome

2018
Targeting HER2 in Breast Cancer: Latest Developments on Treatment Sequencing and the Introduction of Biosimilars.
    Drugs, 2020, Volume: 80, Issue:17

    Topics: Ado-Trastuzumab Emtansine; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Biosimilar Pharmaceuticals; Breast; Breast Neoplasms; Camptothecin; Chemotherapy, Adjuvant; Clinical Trials, Phase III as Topic; Disease-Free Survival; Female; Humans; Immunoconjugates; Lapatinib; Mastectomy; Maytansine; Medical Oncology; Molecular Targeted Therapy; Neoadjuvant Therapy; Neoplasm Recurrence, Local; Oxazoles; Practice Guidelines as Topic; Pyridines; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2020
Recent Advances on Epidermal Growth Factor Receptor as a Molecular Target for Breast Cancer Therapeutics.
    Anti-cancer agents in medicinal chemistry, 2021, Volume: 21, Issue:14

    Topics: Antineoplastic Agents; Breast Neoplasms; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Female; Humans; Lapatinib; Protein Kinase Inhibitors; Quinolines; Trastuzumab

2021
The Molecular Mechanisms of Regulating Oxidative Stress-Induced Ferroptosis and Therapeutic Strategy in Tumors.
    Oxidative medicine and cellular longevity, 2020, Volume: 2020

    Topics: Acetaminophen; Antineoplastic Agents; Antioxidants; Apoptosis; Artemisinins; Auranofin; Cell Death; Cisplatin; Epigenesis, Genetic; Fatty Acids; Ferroptosis; Haloperidol; Humans; Indoles; Iron; Lapatinib; Mevalonic Acid; NADP; Neoplasms; Oxidation-Reduction; Oxidative Stress; Oxygen; Quinolines; Reactive Oxygen Species; Sorafenib; Spiro Compounds; Sulfasalazine; Trigonella

2020
    Bulletin du cancer, 2021, Volume: 108, Issue:11S

    Topics: Aged; Antineoplastic Combined Chemotherapy Protocols; Blood-Brain Barrier; Brain Neoplasms; Breast Neoplasms; Capecitabine; Cranial Irradiation; Disease Progression; Female; Humans; Lapatinib; Life Expectancy; Magnetic Resonance Imaging; Metastasectomy; Middle Aged; Oxazoles; Pyridines; Quinazolines; Quinolines; Radiosurgery; Receptor, ErbB-2; Receptors, Estrogen; Trastuzumab

2021
    Bulletin du cancer, 2021, Volume: 108, Issue:11S

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Immunological; Breast Neoplasms; Clinical Trials as Topic; Female; Genes, erbB-2; Humans; Lapatinib; Neoadjuvant Therapy; Quinolines; Receptor, ErbB-2; Trastuzumab

2021

Trials

2 trial(s) available for lapatinib and hki 272

ArticleYear
A phase two randomised trial of neratinib monotherapy versus lapatinib plus capecitabine combination therapy in patients with HER2+ advanced breast cancer.
    European journal of cancer (Oxford, England : 1990), 2013, Volume: 49, Issue:18

    Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Capecitabine; Deoxycytidine; Diarrhea; Disease-Free Survival; Drug Administration Schedule; Female; Fluorouracil; Humans; Kaplan-Meier Estimate; Lapatinib; Middle Aged; Nausea; Quinazolines; Quinolines; Receptor, ErbB-2; Treatment Outcome; Vomiting

2013
Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2014, Nov-10, Volume: 32, Issue:32

    Topics: Administration, Oral; Adult; Aged; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Breast Neoplasms, Male; Capecitabine; Deoxycytidine; Diarrhea; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Fluorouracil; Humans; Kaplan-Meier Estimate; Lapatinib; Male; Middle Aged; Neoplasm Metastasis; Paresthesia; Quinazolines; Quinolines; Receptor, ErbB-2; Syndrome; Trastuzumab; Treatment Outcome

2014

Other Studies

30 other study(ies) available for lapatinib and hki 272

ArticleYear
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 of novel selective inhibitors for EGFR-T790M/L858R.
    Bioorganic & medicinal chemistry letters, 2012, Feb-01, Volume: 22, Issue:3

    Topics: Catalytic Domain; Cell Line, Tumor; Cell Proliferation; Drug Discovery; ErbB Receptors; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Structure; Mutation; Protein Kinase Inhibitors

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
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
    European journal of medicinal chemistry, 2015, Sep-18, Volume: 102

    Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; MCF-7 Cells; Molecular Structure; Protein Kinase Inhibitors; Quinolines; Structure-Activity Relationship

2015
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.
    Bioorganic & medicinal chemistry letters, 2015, Nov-15, Volume: 25, Issue:22

    Topics: Aniline Compounds; Antineoplastic Agents; Cell Line, Tumor; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Docking Simulation; Protein Kinase Inhibitors; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship

2015
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
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
    Journal of medicinal chemistry, 2019, 05-09, Volume: 62, Issue:9

    Topics: Aminoquinolines; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Chordoma; Drug Design; ErbB Receptors; HEK293 Cells; Humans; Intracellular Signaling Peptides and Proteins; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Quinazolines

2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12

    Topics: Exons; Humans; Mutation; Protein Kinase Inhibitors; Thioctic Acid

2019
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
    Bioorganic & medicinal chemistry, 2019, 07-15, Volume: 27, Issue:14

    Topics: Drug Discovery; Organic Chemicals; Pharmaceutical Preparations; Solubility

2019
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
    Journal of medicinal chemistry, 2020, 10-22, Volume: 63, Issue:20

    Topics: Dose-Response Relationship, Drug; Drug Design; Drug Evaluation, Preclinical; Humans; Kinetics; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor, ErbB-2; Structure-Activity Relationship; Tumor Cells, Cultured

2020
[New development in the treatment of breast cancer. II. Future anti-HER2 therapy].
    Gan to kagaku ryoho. Cancer & chemotherapy, 2009, Volume: 36, Issue:13

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Breast Neoplasms; Female; Humans; Lapatinib; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2009
Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.
    International journal of cancer, 2012, Jul-01, Volume: 131, Issue:1

    Topics: Aminoquinolines; Aniline Compounds; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lapatinib; Morpholines; Protein Kinase Inhibitors; Protein Multimerization; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab

2012
Activating HER2 mutations in HER2 gene amplification negative breast cancer.
    Cancer discovery, 2013, Volume: 3, Issue:2

    Topics: Amino Acid Sequence; Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line; Drug Resistance, Neoplasm; Female; Gene Amplification; Gene Expression; Humans; Lapatinib; Mammary Neoplasms, Experimental; MCF-7 Cells; Mice; Mice, Nude; Models, Molecular; Molecular Sequence Data; Mutation; NIH 3T3 Cells; Protein Structure, Tertiary; Quinazolines; Quinolines; Receptor, ErbB-2; Reverse Transcriptase Polymerase Chain Reaction; Sequence Homology, Amino Acid; Transplantation, Heterologous

2013
A gene expression profile indicative of early stage HER2 targeted therapy response.
    Molecular cancer, 2013, Jul-01, Volume: 12

    Topics: Afatinib; Breast Neoplasms; Cell Line, Tumor; Female; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Humans; Inhibitory Concentration 50; Lapatinib; Protein Kinase Inhibitors; Quinazolines; Quinolines; Receptor, ErbB-2; Time Factors

2013
Photo-activated psoralen binds the ErbB2 catalytic kinase domain, blocking ErbB2 signaling and triggering tumor cell apoptosis.
    PloS one, 2014, Volume: 9, Issue:2

    Topics: Antineoplastic Agents; Apoptosis; Breast Neoplasms; Catalytic Domain; Cell Line, Tumor; Cell Nucleus; Cross-Linking Reagents; Drug Resistance, Neoplasm; Female; Ficusin; Humans; Lapatinib; Molecular Targeted Therapy; Protein Kinase Inhibitors; PUVA Therapy; Quinazolines; Quinolines; Receptor, ErbB-2; Signal Transduction; Ultraviolet Rays

2014
miR-630 targets IGF1R to regulate response to HER-targeting drugs and overall cancer cell progression in HER2 over-expressing breast cancer.
    Molecular cancer, 2014, Mar-24, Volume: 13

    Topics: Anoikis; Breast Neoplasms; Cell Proliferation; Drug Resistance, Neoplasm; Female; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; MicroRNAs; Quinazolines; Quinolines; Receptor, ErbB-2; Receptor, IGF Type 1

2014
Label-free LC-MS analysis of HER2+ breast cancer cell line response to HER2 inhibitor treatment.
    Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 2015, Aug-04, Volume: 23

    Topics: Afatinib; Breast Neoplasms; Cell Line, Tumor; Chromatography, Liquid; Female; Humans; Lapatinib; Mass Spectrometry; Protein Kinase Inhibitors; Proteomics; Quinazolines; Quinolines; Receptor, ErbB-2

2015
HER2 missense mutations have distinct effects on oncogenic signaling and migration.
    Proceedings of the National Academy of Sciences of the United States of America, 2015, Nov-10, Volume: 112, Issue:45

    Topics: Blotting, Western; Cell Line, Tumor; Cell Movement; Cell Proliferation; Colony-Forming Units Assay; Flow Cytometry; Gene Targeting; HEK293 Cells; Humans; Immunoblotting; Lapatinib; Mutation, Missense; Neoplasms; Quinazolines; Quinolines; Receptor, ErbB-2; Signal Transduction; Thiazoles

2015
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.
    Annals of oncology : official journal of the European Society for Medical Oncology, 2016, Volume: 27, Issue:2

    Topics: Adenocarcinoma; Adenocarcinoma of Lung; Adult; Afatinib; Aged; Aged, 80 and over; Anaplastic Lymphoma Kinase; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cohort Studies; Disease-Free Survival; ErbB Receptors; Europe; Female; Humans; Lapatinib; Lung Neoplasms; Male; Middle Aged; Molecular Targeted Therapy; Quinazolines; Quinolines; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Retrospective Studies; Trastuzumab; Treatment Outcome

2016
Neratinib resistance and cross-resistance to other HER2-targeted drugs due to increased activity of metabolism enzyme cytochrome P4503A4.
    British journal of cancer, 2017, Feb-28, Volume: 116, Issue:5

    Topics: Afatinib; Breast Neoplasms; Cell Line, Tumor; Cell Movement; Cytochrome P-450 CYP3A; Drug Resistance, Neoplasm; Female; Humans; Lapatinib; Quinazolines; Quinolines; Receptor, ErbB-2; Trastuzumab; Up-Regulation

2017
Tyrosine kinase inhibitors as modulators of trastuzumab-mediated antibody-dependent cell-mediated cytotoxicity in breast cancer cell lines.
    Cellular immunology, 2017, Volume: 319

    Topics: Afatinib; Antineoplastic Agents; Cell Line, Tumor; Cytotoxicity, Immunologic; Drug Interactions; Gene Expression Regulation, Neoplastic; Humans; K562 Cells; L-Lactate Dehydrogenase; Lapatinib; MCF-7 Cells; Protein Kinase Inhibitors; Quinazolines; Quinolines; Receptor, ErbB-2; Signal Transduction; Trastuzumab

2017
Microenvironment-Mediated Mechanisms of Resistance to HER2 Inhibitors Differ between HER2+ Breast Cancer Subtypes.
    Cell systems, 2018, Mar-28, Volume: 6, Issue:3

    Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Databases, Genetic; Drug Resistance, Neoplasm; Enzyme Inhibitors; Female; Gene Expression Regulation, Neoplastic; Genes, erbB-2; High-Throughput Screening Assays; Humans; Lapatinib; MCF-7 Cells; Mice; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-met; Quinazolines; Quinolines; Receptor, ErbB-2; Receptor, ErbB-3; Signal Transduction; Tumor Microenvironment; Xenograft Model Antitumor Assays

2018
HER-targeted tyrosine kinase inhibitors enhance response to trastuzumab and pertuzumab in HER2-positive breast cancer.
    Investigational new drugs, 2019, Volume: 37, Issue:3

    Topics: Afatinib; Antibodies, Monoclonal, Humanized; Antibody-Dependent Cell Cytotoxicity; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Cell Proliferation; Drug Synergism; Female; Humans; Lapatinib; Protein Kinase Inhibitors; Quinolines; Receptor, ErbB-2; Trastuzumab; Tumor Cells, Cultured

2019
Neratinib is effective in breast tumors bearing both amplification and mutation of ERBB2 (HER2).
    Science signaling, 2018, 10-09, Volume: 11, Issue:551

    Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cell Line, Tumor; Drug Resistance, Neoplasm; Female; Humans; Lapatinib; Lung Neoplasms; Mice; Mice, Nude; Mutation; Proportional Hazards Models; Protein Kinase Inhibitors; Quinolines; Receptor, ErbB-2; Trastuzumab; Treatment Outcome; Xenograft Model Antitumor Assays

2018
How we treat locally advanced HER2-positive breast cancer.
    Clinical advances in hematology & oncology : H&O, 2019, Volume: 17, Issue:5

    Topics: Ado-Trastuzumab Emtansine; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Carcinoma; Clinical Trials as Topic; Combined Modality Therapy; Female; Genes, erbB-2; Humans; Lapatinib; Mastectomy; Maytansine; Molecular Targeted Therapy; Neoadjuvant Therapy; Neoplasm Micrometastasis; Quinolines; Randomized Controlled Trials as Topic; Receptor, ErbB-2; Taxoids; Trastuzumab

2019
Adaptive resistance to trastuzumab impairs response to neratinib and lapatinib through deregulation of cell death mechanisms.
    Cancer letters, 2020, 02-01, Volume: 470

    Topics: Animals; Antineoplastic Agents, Immunological; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Cell Line, Tumor; DNA Damage; Drug Resistance, Neoplasm; Female; Gene Expression Profiling; Humans; Imidazoles; Lapatinib; Mice; Naphthoquinones; Protein Kinase Inhibitors; Pyridines; Quinolines; Receptor, ErbB-2; Trastuzumab; Xenograft Model Antitumor Assays

2020
Immunogenicity of rat-neu
    Scientific reports, 2020, 03-03, Volume: 10, Issue:1

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; CD4-Positive T-Lymphocytes; CD8-Positive T-Lymphocytes; Cell Line, Tumor; Female; Flow Cytometry; Lapatinib; Leukocyte Common Antigens; Male; Mammary Neoplasms, Animal; Mammary Neoplasms, Experimental; Mice; Mice, Inbred BALB C; Quinolines; Rats; Receptor, ErbB-2; Signal Transduction; T-Lymphocytes; Trastuzumab

2020
Comparative analysis of drug response and gene profiling of HER2-targeted tyrosine kinase inhibitors.
    British journal of cancer, 2021, Volume: 124, Issue:7

    Topics: Apoptosis; Biomarkers, Tumor; Cell Proliferation; Gene Expression Regulation, Neoplastic; Humans; Lapatinib; Neoplasms; Protein Kinase Inhibitors; Quinolines; Receptor, ErbB-2; Trastuzumab; Tumor Cells, Cultured

2021
HER2 + breast cancers evade anti-HER2 therapy via a switch in driver pathway.
    Nature communications, 2021, 11-18, Volume: 12, Issue:1

    Topics: Breast Neoplasms; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; Female; Humans; Lapatinib; MAP Kinase Signaling System; Mutation; Oxazoles; Protein Kinase Inhibitors; Pyridines; Quinazolines; Quinolines; Receptor, ErbB-2; Tumor Escape

2021
Neratinib plus capecitabine versus lapatinib plus capecitabine as the third-line therapy for HER2-positive metastatic breast cancer in China: a cost-effectiveness analysis.
    BMJ open, 2022, 11-15, Volume: 12, Issue:11

    Topics: Adolescent; Adult; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Capecitabine; China; Clinical Trials as Topic; Cost-Benefit Analysis; Female; Humans; Lapatinib; Quality-Adjusted Life Years; Receptor, ErbB-2

2022