A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase

Oncogenes and signal transduction

Cantley, L. C., Auger, K. R., Carpenter, C. F., Duckworth, B. C., Graziani, A., Kapeller, R., & Soltoff, S. P. (1991) · Cell · doi:10.1016/0092-8674(91)90639-g · Cited by 2,697 · see citing works

Growth Factors and Cancer

Aaronson, S. A. (1991) · Science · doi:10.1126/science.1659742 · Cited by 2,017 · see citing works

Growth factor signaling by receptor tyrosine kinases

Schlessinger, J., & Ullrich, A. (1992) · Neuron · doi:10.1016/0896-6273(92)90177-f · Cited by 1,430 · see citing works

RECEPTORS FOR EPIDERMAL GROWTH FACTOR AND OTHER POLYPEPTIDE MITOGENS

Carpenter, G. F. (1987) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.56.070187.004313 · Cited by 1,282 · see citing works

Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors

Morrison, J. F. (1969) · Biochimica et Biophysica Acta (BBA) - Enzymology · doi:10.1016/0005-2744(69)90420-3 · Cited by 815 · see citing works

Overexpression of TGFα in transgenic mice: Induction of epithelial hyperplasia, pancreatic metaplasia, and carcinoma of the breast

Sandgren, E. P., Luetteke, N., Palmiter, R. D., Brinster, R. L., & Lee, D. C. (1990) · Cell · doi:10.1016/0092-8674(90)90075-p · Cited by 752 · see citing works

TGFα overexpression in transgenic mice induces liver neoplasia and abnormal development of the mammary gland and pancreas

Jhappan, C., Stahle, C., Harkins, R. N., Fausto, N., Smith, G. H., & Merlino, G. T. (1990) · Cell · doi:10.1016/0092-8674(90)90076-q · Cited by 709 · see citing works

DIOGENES SYNDROME

Clark, A. N. G., Mankikar, G. D., & Gray, I. (1975) · The Lancet · doi:10.1016/s0140-6736(75)91280-5 · Cited by 697 · see citing works

EPIDERMAL-GROWTH-FACTOR RECEPTORS IN HUMAN BLADDER CANCER: COMPARISON OF INVASIVE AND SUPERFICIAL TUMOURS

Neal, D. E., Bennett, M., Hall, R. R., Marsh, C., Abel, P., Sainsbury, J. R. C., & Harris, A. L. (1985) · The Lancet · doi:10.1016/s0140-6736(85)91386-8 · Cited by 604 · see citing works

Growth Inhibition of Human Tumor Cells in Athymic Mice by Anti-Epidermal Growth Factor Receptor Monoclonal Antibodies

Masui, H., Kawamoto, T., Sato, J., Wolf, B., SATO, G. H., & Mendelsohn, J. M. (1984) · The Journal of Urology · doi:10.1016/s0022-5347(17)50005-1 · Cited by 446 · see citing works

Epidermal-Growth-Factor-Dependent Transformation by a Human EGF Receptor Proto-Oncogene

Velu, T. J., Beguinot, L., Vass, W. C., Willingham, M. C., Merlino, G. T., Pastan, I. H., & Lowy, D. R. (1987) · Science · doi:10.1126/science.3500513 · Cited by 433 · see citing works

How receptor tyrosine kinases activate ras

Schlessinger, J. (1993) · Trends in Biochemical Sciences · doi:10.1016/0968-0004(93)90031-h · Cited by 374 · see citing works

Epidermal growth factor and its receptor

Gill, G. N., Bertics, P. J., & Santon, J. B. (1987) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(87)90027-x · Cited by 195 · see citing works

Epidermal growth factor receptor (EGFr); results of a 6 year follow-up study in operable breast cancer with emphasis on the node negative subgroup

Nicholson, S., Richard, J., Sainsbury, C. A. R., Halcrow, P., Kelly, P., Angus, B., Wright, C., Henry, J., Farndon, J. R., & Harris, A. L. (1991) · British Journal of Cancer · doi:10.1038/bjc.1991.30 · Cited by 165 · see citing works

Construction of a Novel Oncogene Based on Synthetic Sequences Encoding Epidermal Growth Factor

Stern, D. F., Hare, D. L., Cecchini, M. A., & Weinberg, R. A. (1987) · Science · doi:10.1126/science.3492043 · Cited by 156 · see citing works

Tumor growth modulation by a monoclonal antibody to the epidermal growth factor receptor: immunologically mediated and effector cell-independent effects.

Rodeck, U., Herlyn, M., Herlyn, D., Molthoff, C. F. M., Atkinson, B., Varello, M. A., Steplewski, Z., & Koprowski, H. (1987) · PubMed · Cited by 150 · see citing works

The assembly of signalling complexes by receptor tyrosine kinases

Panayotou, G., & Waterfield, M. D. (1993) · BioEssays · doi:10.1002/bies.950150305 · Cited by 130 · see citing works

Ligand activation of overexpressed epidermal growth factor receptors transforms NIH 3T3 mouse fibroblasts.

Riedel, H., Massoglia, S. L., Schlessinger, J., & Ullrich, A. (1988) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.85.5.1477 · Cited by 130 · see citing works

Mechanism of antitumor activity in mice for anti-epidermal growth factor receptor monoclonal antibodies with different isotypes.

Masui, H., Moroyama, T., & Mendelsohn, J. M. (1986) · PubMed · Cited by 103 · see citing works

The risk of subsequent primary malignant diseases after cancers of the colon and rectum a nationwide cohort study

Enblad, P., Adami, H., Glimelius, B., Krusemo, U. B., & Påhlman, L. (1990) · Cancer · doi:10.1002/1097-0142(19900501)65:9 · Cited by 100 · see citing works

Neurotoxicity of intraventricularly administered alpha-interferon for leptomeningeal disease

Meyers, C. A., Obbens, E. A. M. T., Scheibel, R. S., & Moser, R. P. (1991) · Cancer · doi:10.1002/1097-0142(19910701)68:1 · Cited by 76 · see citing works

Prognostic value of epidermal growth factor receptor in node-positive breast cancer

Grimaux, M., Romain, S., Remvikos, Y., Martin, P., & Magdelénat, H. (1989) · Breast Cancer Research and Treatment · doi:10.1007/bf01805978 · Cited by 69 · see citing works

Effects of substitution of threonine 654 of the epidermal growth factor receptor on epidermal growth factor-mediated activation of phospholipase C.

Decker, S. J., Ellis, C. A., Pawson, T. J., & Velu, T. J. (1990) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)39251-8 · Cited by 68 · see citing works

Prognostic significance of the receptor for epidermal growth factor in human mammary carcinomas.

Macias, A., Azavedo, E., Hägerström, T., Klintenberg, C., Pérez, R., & Skoog, L. K. (1987) · PubMed · Cited by 62 · see citing works

Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase

Traxler, P. M., Wacker, O., Bach, H., Geissler, J. F., Kump, W. G., Meyer, T., Regenass, U., Roesel, J. L., & Lydon, N. (1991) · Journal of Medicinal Chemistry · doi:10.1021/jm00112a003 · Cited by 57 · see citing works

Cell-signaling targets for antitumour drug development

Brunton, V. G., & Workman, P. (1993) · Cancer Chemotherapy and Pharmacology · doi:10.1007/bf00685870 · Cited by 45 · see citing works

[7] Purification of functionally active epidermal growth factor receptor protein using a competitive antagonist monoclonal antibody and competitive elution with epidermal growth factor

Gill, G. N., & Weber, W. (1987) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(87)46010-2 · Cited by 22 · see citing works

Growth inhibition of human nasopharyngeal carcinoma in athymic mice by anti‐epidermal growth factor receptor monoclonal antibodies

Guan, E., Tingchong, Z., Wang, J., Chen, Y., Sun, Y., Huang, P., Tang, W., & Zhao, M. (1989) · The International Journal Of Cell Cloning · doi:10.1002/stem.5530070406 · Cited by 6 · see citing works

PD 098059 Is a Specific Inhibitor of the Activation of Mitogen-activated Protein Kinase Kinase in Vitro and in Vivo

Alessi, D. R., Cuenda, A., Cohen, P., Dudley, D. T., & Saltiel, A. R. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.46.27489 · Cited by 3,396 · see citing works

Targeting cancer with small molecule kinase inhibitors

Zhang, J., Yang, P. L., & Gray, N. S. (2008) · Nature reviews. Cancer · doi:10.1038/nrc2559 · Cited by 2,585 · see citing works

A postmodern moral tale: the ethics of research relationships

Somerville, M. (2002) · Nature reviews. Drug discovery · doi:10.1038/nrd773 · Cited by 2,175 · see citing works

SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin‐1

Cuenda, A., Rouse, J., Doza, Y. N., Meier, R., Cohen, P., Gallagher, T. F., Young, P. R., & Lee, J. C. (1995) · FEBS Letters · doi:10.1016/0014-5793(95)00357-f · Cited by 2,086 · see citing works

STATs in oncogenesis

Bowman, T., Garcia, R., Turkson, J., & Jove, R. (2000) · Oncogene · doi:10.1038/sj.onc.1203527 · Cited by 1,743 · see citing works

Tyrosine Kinase Inhibition: An Approach to Drug Development

Levitzki, A., & Gazit, A. (1995) · Science · doi:10.1126/science.7892601 · Cited by 1,635 · see citing works

Impact of high-throughput screening in biomedical research

Macarron, R., Banks, M. N., Bojanic, D., Burns, D. J., Cirovic, D. A., Garyantes, T., Green, D. V. S., Hertzberg, R. P., Janzen, W. P., Paslay, J. W., et al. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3368 · Cited by 1,364 · see citing works

The EGF receptor family as targets for cancer therapy

Mendelsohn, J. M., & Baselga, J. M. (2000) · Oncogene · doi:10.1038/sj.onc.1204082 · Cited by 1,341 · see citing works

The discovery of receptor tyrosine kinases: targets for cancer therapy

Gschwind, A., Fischer, O. M., & Ullrich, A. (2004) · Nature Reviews Cancer · doi:10.1038/nrc1360 · Cited by 1,227 · see citing works

The quest to overcome resistance to EGFR-targeted therapies in cancer

Chong, C. R., & Janne, P. A. (2013) · Nature Medicine · doi:10.1038/nm.3388 · Cited by 1,055 · see citing works

SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types.

Fong, T. A. T., Shawver, L. K., Sun, L., Tang, C., App, H., Powell, T., Kim, Y. H., Schreck, R., Wang, X., Risau, W., et al. (1999) · PubMed · Cited by 1,032 · see citing works

Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor.

Ciardiello, F., Caputo, R., Bianco, R., Damiano, Pomatico, G., De Placido, S., Bianco, A. R., & Tortora, G. (2000) · PubMed · Cited by 937 · see citing works

Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker

Solca, F., Dahl, G., Zoephel, A., Bader, G., Sanderson, M., Klein, C., Kraemer, O., Himmelsbach, F., Haaksma, E., & Adolf, G. R. (2012) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.112.197756 · Cited by 865 · see citing works

Distinct Neural Stem Cells Proliferate in Response to EGF and FGF in the Developing Mouse Telencephalon

Tropepe, V., Sibilia, M. C., Ciruna, B. G., Rossant, J., Wagner, E. F., & van der Kooy, D. (1999) · Developmental Biology · doi:10.1006/dbio.1998.9192 · Cited by 815 · see citing works

Understanding resistance to EGFR inhibitors—impact on future treatment strategies

Wheeler, D. L., Dunn, E. F., & Harari, P. M. (2010) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2010.97 · Cited by 683 · see citing works

Review on Epidermal Growth Factor Receptor (EGFR) Structure, Signaling Pathways, Interactions, and Recent Updates of EGFR Inhibitors

Sabbah, D. A., Hajjo, R., & Sweidan, K. (2020) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026620666200303123102 · Cited by 606 · see citing works

ErbB receptors: from oncogenes to targeted cancer therapies

Zhang, H., Berezov, A., Wang, Q., Zhang, G., Drebin, J. A., Murali, R., & Greene, M. I. (2007) · Journal of Clinical Investigation · doi:10.1172/jci32278 · Cited by 573 · see citing works

Nuclear interaction of EGFR and STAT3 in the activation of the iNOS/NO pathway

Lo, H., Hsu, S.-C., Ali‐Seyed, M., Gündüz, M., Xia, W., Wei, Y., Bartholomeusz, G. A., Shih, J. Y., & Hung, M. (2005) · Cancer Cell · doi:10.1016/j.ccr.2005.05.007 · Cited by 539 · see citing works

Requirement of Stat3 but not Stat1 activation for epidermal growth factor receptor- mediated cell growth In vitro.

Grandis, J. R., Drenning, S. D., Chakraborty, A., Zhou, M. Y., Zeng, Q., Pitt, A. S., & Tweardy, D. J. (1998) · Journal of Clinical Investigation · doi:10.1172/jci3785 · Cited by 507 · see citing works

Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain

Mohammadi, M., Froum, S., Hamby, J. M., Schroeder, M. C., Panek, R. L., Lu, G. H., Eliseenkova, A. V., Green, D., Schlessinger, J., & Hubbard, S. R. (1998) · The EMBO Journal · doi:10.1093/emboj/17.20.5896 · Cited by 484 · see citing works

Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: Synthetic approaches and multifarious applications

Khan, I. A., Ibrar, A., Abbas, N., & Saeed, A. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.02.005 · Cited by 472 · see citing works

Fabrication of gold nanoparticles for targeted therapy in pancreatic cancer

Patra, C. R., Bhattacharya, R., Mukhopadhyay, D., & Mukherjee, P. (2009) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2009.11.007 · Cited by 464 · see citing works

Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: The advances continue

Khan, I. A., Ibrar, A., Ahmed, W., & Saeed, A. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.10.084 · Cited by 431 · see citing works

Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor

Fry, D. W., Bridges, A. J., Denny, W. A., Doherty, A. M., Greis, K. D., Hicks, J. L., Hook, K. E., Keller, P. R., Leopold, W. R., Loo, J. A., et al. (1998) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.95.20.12022 · Cited by 424 · see citing works

THE CROONIAN LECTURE 1997. The phosphorylation of proteins on tyrosine: its role in cell growth and disease

Hunter, T. R. (1998) · Philosophical Transactions of the Royal Society B Biological Sciences · doi:10.1098/rstb.1998.0228 · Cited by 409 · see citing works

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

Dar, A. C., & Shokat, K. M. (2011) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-090308-173656 · Cited by 388 · see citing works

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

Xie, X., Yu, T., Li, X., Zhang, N., Foster, L. J., Peng, C., Huang, W., & He, G. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01589-z · Cited by 396 · see citing works

Strategies toward the Design of Novel and Selective Protein Tyrosine Kinase Inhibitors

Traxler, P. M., & Furet, P. (1999) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(98)00044-8 · Cited by 390 · see citing works

STAT signaling in head and neck cancer

Song, J. I., & Grandis, J. R. (2000) · Oncogene · doi:10.1038/sj.onc.1203483 · Cited by 374 · see citing works

Homogeneous and heterogeneous catalysts for multicomponent reactions

Climent, M. J., Corma, A., & Iborra, S. (2011) · RSC Advances · doi:10.1039/c1ra00807b · Cited by 374 · see citing works

HER2/neu kinase-dependent modulation of androgen receptor function through effects on DNA binding and stability.

Mellinghoff, I. K., Vivanco, I., Kwon, A., Tran, C., Wongvipat, J., & Sawyers, C. L. (2004) · Cancer Cell · doi:10.1016/j.ccr.2004.09.031 · Cited by 344 · see citing works

Targeted inhibition of Stat3 with a decoy oligonucleotide abrogates head and neck cancer cell growth

Leong, P. L., Andrews, G. A., Johnson, D. E., Dyer, K. F., Xi, S., Mai, J. C., Robbins, P. D., Gadiparthi, S., Burke, N. A., Watkins, S. F., et al. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0534764100 · Cited by 340 · see citing works

Activation of preformed EGF receptor dimers by ligand-induced rotation of the transmembrane domain11Edited by B. Holland

Moriki, T., Maruyama, H., & MARUYAMA, I. N. (2001) · Journal of Molecular Biology · doi:10.1006/jmbi.2001.4923 · Cited by 337 · see citing works

The epidermal growth factor receptor as a target for cancer therapy.

Mendelsohn, J. M. (2001) · Endocrine Related Cancer · doi:10.1677/erc.0.0080003 · Cited by 330 · see citing works

Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids

Auti, P. S., George, G., & Paul, A. T. (2020) · RSC Advances · doi:10.1039/d0ra06642g · Cited by 328 · see citing works

Probing the Probes: Fitness Factors For Small Molecule Tools

Workman, P., & Collins, I. (2010) · Chemistry & Biology · doi:10.1016/j.chembiol.2010.05.013 · Cited by 300 · see citing works

Protein tyrosine kinases and cancer

Kolibaba, K. S., & Druker, B. J. (1997) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/s0304-419x(97)00022-x · Cited by 295 · see citing works

Quinazolines and quinazolinones as ubiquitous structural fragments in medicinal chemistry: An update on the development of synthetic methods and pharmacological diversification

Khan, I. A., Zaib, S., Batool, S., Abbas, N., Ashraf, Z., Iqbal, J., & Saeed, A. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.03.031 · Cited by 281 · see citing works

ErbB1 dimerization is promoted by domain co-confinement and stabilized by ligand binding

Low-Nam, S. T., Lidke, K. A., Cutler, P. J., Roovers, R. C., Henegouwen, P. M. P. V. B. E., Wilson, B. S., & Lidke, D. S. (2011) · Nature Structural & Molecular Biology · doi:10.1038/nsmb.2135 · Cited by 273 · see citing works

Tethered Epidermal Growth Factor Provides a Survival Advantage to Mesenchymal Stem Cells

Fan, V. H., Au, A., Tamama, K., Littrell, R., Richardson, L. B., Wright, J. W., Wells, A. H., & Griffith, L. G. (2007) · Stem Cells · doi:10.1634/stemcells.2006-0320 · Cited by 268 · see citing works

Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras?

Cox, A. D., & Der, C. J. (1997) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/s0304-419x(97)00011-5 · Cited by 266 · see citing works

The selective tyrosine kinase inhibitor STI571 inhibits small cell lung cancer growth.

Krystal, G. W., Honsawek, S., Litz, J., & Buchdunger, E. (2000) · PubMed · Cited by 265 · see citing works

Inhibitors of protein kinases and phosphatases

MacKintosh, C., & MacKintosh, R. W. (1994) · Trends in Biochemical Sciences · doi:10.1016/0968-0004(94)90127-9 · Cited by 264 · see citing works

Metalloprotease-mediated ligand release regulates autocrine signaling through the epidermal growth factor receptor

Dong, J., Opresko, L. K., Dempsey, P. J., Lauffenburger, D. A., Coffey, R. J., & Wiley, H. S. (1999) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.96.11.6235 · Cited by 263 · see citing works

HB-EGF is Necessary and Sufficient for Müller Glia Dedifferentiation and Retina Regeneration

Wan, J., Ramachandran, R., & Goldman, D. (2012) · Developmental Cell · doi:10.1016/j.devcel.2011.11.020 · Cited by 262 · see citing works

Activated signal transducer and activator of transcription 3 (STAT3) supports the malignant phenotype of human pancreatic cancer

Scholz, A., Heinze, S., Detjen, K. M., Peters, M., Welzel, M., Hauff, P., Schirner, M., Wiedenmann, B. J., & Rosewicz, S. (2003) · Gastroenterology · doi:10.1016/s0016-5085(03)01064-3 · Cited by 256 · see citing works

Prognostic significance of epidermal growth factor receptor in laryngeal squamous cell carcinoma

Maurizi, M., Almadori, G., Ferrandina, G., Distefano, M., Romanini, M., Cadoni, G., Benedetti-Panici, P., Paludetti, G., Scambia, G., & Mancuso, S. (1996) · British Journal of Cancer · doi:10.1038/bjc.1996.525 · Cited by 249 · see citing works

Reaching out for signals

Lidke, D. S., Lidke, K. A., Rieger, B., Jovin, T. M., & Arndt‐Jovin, D. J. (2005) · The Journal of Cell Biology · doi:10.1083/jcb.200503140 · Cited by 229 · see citing works

Profiling receptor tyrosine kinase activation by using Ab microarrays

Nielsen, U. B., Cardone, M. H., Sinskey, A. J., MacBeath, G., & Sorger, P. K. (2003) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1633513100 · Cited by 226 · see citing works

Design of allele-specific inhibitors to probe protein kinase signaling

Bishop, A. C., Shah, K., Liu, Y., Witucki, L. A., Kung, C.-Y., & Shokat, K. M. (1998) · Current Biology · doi:10.1016/s0960-9822(98)70198-8 · Cited by 226 · see citing works

Transcriptome analysis of HER2 reveals a molecular connection to fatty acid synthesis.

Kumar‐Sinha, C., Ignatoski, K. W., Lippman, M. E., Ethier, S. P., & Chinnaiyan, A. M. (2003) · PubMed · Cited by 222 · see citing works

Thrombin (PAR-1)-induced proliferation in astrocytes via MAPK involves multiple signaling pathways

Wang, H., Ubl, J. J., Stricker, R., & Reiser, G. (2002) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00001.2002 · Cited by 217 · see citing works

Hypermethylation of the APC (adenomatous Polyposis Coli) gene promoter region in human colorectal carcinoma

Hiltunen, M., Alhonen, L. I., Koıstınaho, J., Myöhänen, S., Pääkkönen, M. E., Marin, S., Kosma, V.-M., & Jänne, J. (1997) · International Journal of Cancer · doi:10.1002/(sici)1097-0215(19970317)70:6 · Cited by 192 · see citing works

ErbB-targeted therapeutic approaches in human cancer

Arteaga, C. L. (2003) · Experimental Cell Research · doi:10.1016/s0014-4827(02)00104-0 · Cited by 215 · see citing works

Protein Tyrosine Kinase Inhibitors as Novel Therapeutic Agents

Levitzki, A. (1999) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(98)00066-7 · Cited by 214 · see citing works

The Ascension of Targeted Covalent Inhibitors

Singh, J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02134 · Cited by 210 · see citing works

Flavonoids as Protein Kinase Inhibitors for Cancer Chemoprevention: Direct Binding and Molecular Modeling

Hou, D., & Kumamoto, T. (2010) · Antioxidants and Redox Signaling · doi:10.1089/ars.2009.2816 · Cited by 212 · see citing works

Ezrin oligomers are major cytoskeletal components of placental microvilli: a proposal for their involvement in cortical morphogenesis.

Berryman, M. A., Gary, R. K., & Bretscher, A. P. (1995) · The Journal of Cell Biology · doi:10.1083/jcb.131.5.1231 · Cited by 207 · see citing works

Reversible G1 Arrest Induced by Inhibition of the Epidermal Growth Factor Receptor Tyrosine Kinase Requires Up-regulation of p27KIP1 Independent of MAPK Activity

Busse, D., Doughty, R. S., Ramsey, T. T., Russell, W. E., Price, J. O., Flanagan, W. M., Shawver, L. K., & Arteaga, C. L. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.275.10.6987 · Cited by 205 · see citing works

Structure-guided development of affinity probes for tyrosine kinases using chemical genetics

Blair, J. A., Rauh, D., Kung, C. K.-H., Yun, C., Fan, Q.-W., Rode, H. B., Zhang, C., Eck, M. J., Weiss, W. A., & Shokat, K. M. (2007) · Nature Chemical Biology · doi:10.1038/nchembio866 · Cited by 204 · see citing works

Quinazoline derivatives: synthesis and bioactivities

Wang, D., & Gao, F. (2013) · Chemistry Central Journal · doi:10.1186/1752-153x-7-95 · Cited by 199 · see citing works

PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner.

Bos, M., Mendelsohn, J. M., Kim, Y. M., Albanell, J., Fry, D. W., & Baselga, J. M. (1997) · PubMed · Cited by 199 · see citing works

Protein Kinase InhibitorsThe Tyrosine-Specific Protein Kinases

Lawrence, D. S., & Niu, J. (1998) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(97)00052-1 · Cited by 198 · see citing works

Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors as Anticancer Agents

Ciardiello, F. (2000) · Drugs · doi:10.2165/00003495-200060001-00003 · Cited by 194 · see citing works

Hypoxia Inducible Factor Activates the Transforming Growth Factor-α/Epidermal Growth Factor Receptor Growth Stimulatory Pathway in VHL-/- Renal Cell Carcinoma Cells

Gunaratnam, L., Morley, M., Franovic, A., de Paulsen, N., Mekhail, K., Parolin, D. A. E., Nakamura, E., Lorimer, I. A. J., & Lee, S. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m305502200 · Cited by 188 · see citing works

Role of transforming growth factor-alpha in von Hippel- Lindau (VHL)-/- clear cell renal carcinoma cell proliferation: A possible mechanism coupling VHL tumor suppressor inactivation and tumorigenesis

de Paulsen, N., Brychzy, A., Fournier, M.-C., Klausner, R. D., Gnarra, J. R., Pause, A., & Lee, S. B. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.98.4.1387 · Cited by 193 · see citing works

Characterization of Chemical Libraries for Luciferase Inhibitory Activity

Auld, D. S., Southall, N. T., Jadhav, A., Johnson, R. L., Diller, D., Simeonov, A. M., Austin, C. P., & Inglese, J. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm701302v · Cited by 183 · see citing works

Small Molecules as Inhibitors of Cyclin‐Dependent Kinases

Huwe, A., Mazitschek, R., & Giannis, A. (2003) · Angewandte Chemie International Edition · doi:10.1002/anie.200200540 · Cited by 181 · see citing works

Src Kinases Mediate STAT Growth Pathways in Squamous Cell Carcinoma of the Head and Neck

Xi, S., Zhang, Q. H., Dyer, K. F., Lerner, E. C., Smithgall, T. E., Gooding, W. E., Kamens, J., & Grandis, J. R. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m303499200 · Cited by 180 · see citing works

Copper-catalyzed annulation of amidines for quinazoline synthesis

Lv, Y., Li, Y., Xiong, T., Pu, W., Zhang, H., Sun, K., Liu, Q., & Zhang, Q. (2013) · Chemical Communications · doi:10.1039/c3cc43129k · Cited by 178 · see citing works

The Development of HKI‐272 and Related Compounds for the Treatment of Cancer

Wissner, A., & Mansour, T. S. (2008) · Archiv der Pharmazie · doi:10.1002/ardp.200800009 · Cited by 179 · see citing works

Tyrosine Kinase Inhibitors Targeted to the Epidermal Growth Factor Receptor Subfamily

Noonberg, S. B., & Benz, C. C. (2000) · Drugs · doi:10.2165/00003495-200059040-00003 · Cited by 173 · see citing works

Testosterone Activates Mitogen-Activated Protein Kinase via Src Kinase and the Epidermal Growth Factor Receptor in Sertoli Cells

Cheng, J., Watkins, S. C., & Walker, W. H. (2007) · Endocrinology · doi:10.1210/en.2006-1465 · Cited by 172 · see citing works

In vivo antitumor efficacy of STAT3 blockade using a transcription factor decoy approach: implications for cancer therapy

Xi, S., Gooding, W. E., & Grandis, J. R. (2004) · Oncogene · doi:10.1038/sj.onc.1208316 · Cited by 170 · see citing works

RTK mutations and human syndromes: when good receptors turn bad

Robertson, S. C., Tynan, J. A., & Donoghue, D. J. (2000) · Trends in Genetics · doi:10.1016/s0168-9525(00)02077-1 · Cited by 168 · see citing works

EGF-Receptor Tyrosine Kinase Inhibition Induces Keratinocyte Growth Arrest and Terminal Differentiation

Péus, D., Hamacher, K. L., & Pittelkow, M. R. (1997) · Journal of Investigative Dermatology · doi:10.1111/1523-1747.ep12340759 · Cited by 167 · see citing works

The Biochemistry of Cancer Dissemination

Price, J. T., Bonovich, M. T., Kohn, E. C., Welch, D. R., & Hershey, M. S. (1997) · Critical Reviews in Biochemistry and Molecular Biology · doi:10.3109/10409239709082573 · Cited by 167 · see citing works

Activation of the EGF receptor signaling pathway in human airway epithelial cells exposed to metals

Wu, W., Graves, L. M., Jaspers, I., Devlin, R. B., Reed, W., & Samet, J. M. (1999) · American Journal of Physiology-Lung Cellular and Molecular Physiology · doi:10.1152/ajplung.1999.277.5.l924 · Cited by 167 · see citing works

Specific inhibition of epidermal growth factor receptor tyrosine kinase by 4-anilinoquinazolines

Wakeling, A. E., Barker, A. J., Davies, D. H., Brown, D. S., Green, L. R., Cartlidge, S. A., & Woodburn, J. R. (1996) · Breast Cancer Research and Treatment · doi:10.1007/bf01803785 · Cited by 166 · see citing works

Epidermal growth factor receptor relocalization and kinase activity are necessary for directional migration of keratinocytes in DC electric fields

Fang, K. S., Ionides, E. L., OSTER, G. F., Nuccitelli, R., & Isseroff, R. R. (1999) · Journal of Cell Science · doi:10.1242/jcs.112.12.1967 · Cited by 164 · see citing works

Bile acids induce hepatic stellate cell proliferation via activation of the epidermal growth factor receptor

Svegliati‐Baroni, G., Ridolfi, F., Hannivoort, R. A., Saccomanno, S., Buist‐Homan, M., Minicis, S. D., Jansen, P. L. M., Candelaresi, C., Benedetti, A., & Moshage, H. J. (2005) · Gastroenterology · doi:10.1053/j.gastro.2005.01.007 · Cited by 162 · see citing works

An in vitro tubulogenesis system using cell lines derived from the embryonic kidney shows dependence on multiple soluble growth factors

Sakurai, H., Barros, E. J. G., Tsukamoto, T., Barasch, J. M., & Nigám, S. K. (1997) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.94.12.6279 · Cited by 160 · see citing works

Involvement of steroid hormone and growth factor cross-talk in endocrine response in breast cancer.

Nicholson, R. I., McClelland, R. A., Robertson, J. F. R., & Gee, J. M. W. (1999) · Endocrine Related Cancer · doi:10.1677/erc.0.0060373 · Cited by 160 · see citing works

HER2 overexpression and paclitaxel sensitivity in breast cancer: therapeutic implications.

Baselga, J. M., Seidman, A. D., Rosen, P. P., & Norton, L. (1997) · PubMed · Cited by 157 · see citing works

Evidence for a size-sensing mechanism in animal cells

Dolznig, H., Grebien, F., Sauer, T., Beug, H., & Müllner, E. W. (2004) · Nature Cell Biology · doi:10.1038/ncb1166 · Cited by 154 · see citing works

The relative role of ErbB1–4 receptor tyrosine kinases in radiation signal transduction responses of human carcinoma cells

Bowers, G. D., Reardon, D. B., Hewitt, T., Dent, P., Mikkelsen, R. B., Valerie, K. C., Lammering, G., Amir, C., & Schmidt‐Ullrich, R. (2001) · Oncogene · doi:10.1038/sj.onc.1204255 · Cited by 153 · see citing works

Angiotensin II stimulates ERK via two pathways in epithelial cells: protein kinase C suppresses a G–protein coupled receptor–EGF receptor transactivation pathway

Li, X., Lee, J. W., Graves, L. M., & Earp, H. S. (1998) · The EMBO Journal · doi:10.1093/emboj/17.9.2574 · Cited by 151 · see citing works

Podocytes are sensitive to fluid shear stress in vitro

Friedrich, C., Endlich, N., Kriz, W., & Endlich, K. (2006) · American Journal of Physiology-Renal Physiology · doi:10.1152/ajprenal.00196.2005 · Cited by 150 · see citing works

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors

Lu, X., Smaill, J. B., Patterson, A. V., & Ding, K. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01719 · Cited by 146 · see citing works

Role of Tyrosine Kinase Activity of Epidermal Growth Factor Receptor in the Lysophosphatidic Acid-stimulated Mitogen-activated Protein Kinase Pathway

Cunnick, J. M., Dorsey, J. F., Standley, T. B., Turkson, J., Kraker, A. J., Fry, D. W., Jove, R., & Wu, J. (1998) · Journal of Biological Chemistry · doi:10.1074/jbc.273.23.14468 · Cited by 148 · see citing works

High EGFR expression predicts poor prognosis in patients with squamous cell carcinoma of the oral cavity and oropharynx: A TMA-based immunohistochemical analysis

Laimer, K., Spizzo, G., Gastl, G. A., Obrist, P., Brunhuber, T., Fong, D., Barbieri, V., Jank, S., Doppler, W., Rasse, M., et al. (2006) · Oral Oncology · doi:10.1016/j.oraloncology.2006.02.009 · Cited by 145 · see citing works

Targeting EGFR and HER-2 receptor tyrosine kinases for cancer drug discovery and development

Kamath, S., & Buolamwini, J. K. (2006) · Medicinal Research Reviews · doi:10.1002/med.20070 · Cited by 145 · see citing works

Discovering novel chemotherapeutic drugs for the third millennium

Garrett, M. D., & Workman, P. (1999) · European Journal of Cancer · doi:10.1016/s0959-8049(99)00280-4 · Cited by 141 · see citing works

Activation-dependent clustering of the erbB2 receptor tyrosine kinase detected by scanning near-field optical microscopy

Nagy, P., Jenei, A., Kirsch, A. K., Szöllõsi, J., Damjanovich, S., & Jovin, T. M. (1999) · Journal of Cell Science · doi:10.1242/jcs.112.11.1733 · Cited by 143 · see citing works

LEUKOCYTE PROTEIN TYROSINE KINASES:Potential Targets for Drug Discovery

Bolen, J. B., & Brugge, J. S. (1997) · Annual Review of Immunology · doi:10.1146/annurev.immunol.15.1.371 · Cited by 143 · see citing works

Copper-Catalyzed Synthesis of Quinazoline Derivatives via Ullmann-Type Coupling and Aerobic Oxidation

Wang, C., Li, S., Liu, H., Jiang, Y., & Fu, H. (2010) · The Journal of Organic Chemistry · doi:10.1021/jo101685d · Cited by 142 · see citing works

RTK mutations and human syndromes

Robertson, S. C., Tynan, J. A., & Donoghue, D. J. (2000) · Trends in Genetics · doi:10.1016/s0168-9525(00)02021-7 · Cited by 141 · see citing works

Epidermal Growth Factor Receptor Signaling and the Invasive Phenotype of Ovarian Carcinoma Cells

Alper, Ö., Bergmann‐Leitner, E. S., Bennett, T. A., Hacker, N. F., Stromberg, K., & Stetler‐Stevenson, W. G. (2001) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/93.18.1375 · Cited by 141 · see citing works

Synthesis and Target Identification of Hymenialdisine Analogs

Wan, Y., Hur, W., Cho, C. Y., Liu, Y., Adrian, F. J., Lozach, O., Bach, S., Mayer, T., Fabbro, D., Meijer, L., et al. (2004) · Chemistry & Biology · doi:10.1016/j.chembiol.2004.01.015 · Cited by 140 · see citing works

EGFR Activation Results in Enhanced Cyclooxygenase-2 Expression through p38 Mitogen-Activated Protein Kinase–Dependent Activation of the Sp1/Sp3 Transcription Factors in Human Gliomas

Xu, K., & Shu, H. G. (2007) · Cancer Research · doi:10.1158/0008-5472.can-07-0141 · Cited by 140 · see citing works

PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner.

Bos, M., Mendelsohn, J. M., Kim, Y. M., Albanell, J., Fry, D. W., & Baselga, J. M. (1997) · PubMed · Cited by 199 · see citing works

Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice

Kunkel, M. W., Hook, K. E., Howard, C. T., Przybranowski, S. A., Roberts, B. J., Elliott, W. L., & Leopold, W. R. (1995) · Investigational New Drugs · doi:10.1007/bf00873135 · Cited by 59 · see citing works

Evaluation of Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors

Rae, J. M., & Lippman, M. E. (2004) · Breast Cancer Research and Treatment · doi:10.1023/b:brea.0000010702.10130.29 · Cited by 29 · see citing works

Cytoskeletal and Morphological Changes Associated with the Specific Suppression of the Epidermal Growth Factor Receptor Tyrosine Kinase Activity in A431 Human Epidermoid Carcinoma

Nelson, J. M., & Fry, D. W. (1997) · Experimental Cell Research · doi:10.1006/excr.1997.3571 · Cited by 17 · see citing works

Biochemical and antiproliferative properties of 4-[Ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor

Fry, D. W., Nelson, J. M., Slintak, V., Keller, P. R., Rewcastle, G. W., Denny, W. A., Zhou, H., & Bridges, A. J. (1997) · Biochemical Pharmacology · doi:10.1016/s0006-2952(97)00242-6 · Cited by 65 · see citing works