Journal ArticleDOI
ERBB receptors and cancer: the complexity of targeted inhibitors.
Nancy E. Hynes,Heidi Lane +1 more
TLDR
This work discusses the significance of these receptors as clinical targets, in particular the molecular mechanisms underlying response, and many ERBB inhibitors used in the clinic.Abstract:
ERBB receptor tyrosine kinases have important roles in human cancer. In particular, the expression or activation of epidermal growth factor receptor and ERBB2 are altered in many epithelial tumours, and clinical studies indicate that they have important roles in tumour aetiology and progression. Accordingly, these receptors have been intensely studied to understand their importance in cancer biology and as therapeutic targets, and many ERBB inhibitors are now used in the clinic. We will discuss the significance of these receptors as clinical targets, in particular the molecular mechanisms underlying response.read more
Citations
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Journal ArticleDOI
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Peter Ballard,Robert Hugh Bradbury,Craig S. Harris,Laurent Francois Andre Hennequin,Mark Hickinson,Jason Grant Kettle,Jane Kendrew,Teresa Klinowska,Donald J. Ogilvie,Stuart E. Pearson,Emma J. Williams,Ingrid Wilson +11 more
TL;DR: The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated and strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed.
Book ChapterDOI
Activated Epidermal Growth Factor Receptor in Ovarian Cancer
TL;DR: Ligand binding promotes EGF receptor homoand heterodimerization with ErbB family members, activation of the intracellular tyrosine kinase domain, and phosphorylation of specific tyrosines of the receptor cytoplasmic domain, which leads to assembly of signaling complexes and stimulation of numerous downstream signaling cascades associated with cell growth and survival, increased angiogenesis, and metastasis in tumors.
Journal ArticleDOI
Expert Consensus on the Management of Erlotinib-Associated Cutaneous Toxicity in the u.k
Nick Thatcher,Marianne Nicolson,Richard Groves,Jeremy P.C. Steele,Beth Eaby,Joyce Dunlop,J. McPhelim,Rajinder Nijjar,Ijeoma Ukachukwu +8 more
TL;DR: The resulting expert opinion is a practical and workable version of the international proposal that considers all applicable national issues regarding the management of erlotinib-associated skin toxicity.
Journal ArticleDOI
Improving the preclinical models for the study of chemotherapy-induced cardiotoxicity: a Position Paper of the Italian Working Group on Drug Cardiotoxicity and Cardioprotection
Rosalinda Madonna,Christian Cadeddu,Martino Deidda,Donato Mele,Ines Monte,Giuseppina Novo,Pasquale Pagliaro,Alessia Pepe,Paolo Spallarossa,Carlo G. Tocchetti,Concetta Zito,Giuseppe Mercuro +11 more
TL;DR: The distinctive etiopatogenetic features of cardiac toxicity induced by cancer therapy in humans, which include new aspects of mitochondrial function and oxidative stress, neuregulin-1 modulation through the ErbB receptor family, angiogenesis inhibition, and cardiac stem cell depletion and/or dysfunction are defined.
Journal ArticleDOI
EGFR Downregulation after Anti-EGFR Therapy Predicts the Antitumor Effect in Colorectal Cancer
Yasuyuki Okada,Tetsuo Kimura,Tadahiko Nakagawa,Koichi Okamoto,Akira Fukuya,Takahiro Goji,Shota Fujimoto,Masahiro Sogabe,Hiroshi Miyamoto,Naoki Muguruma,Yasushi Tsuji,Toshiya Okahisa,Tetsuji Takayama +12 more
TL;DR: It is clearly demonstrated that anti-EGFR mAb facilitates internalization and subsequent degradation of EGFRs in lysosomes, which is an important determinant of the efficacy of anti- EGFR m Ab treatment for colorectal cancer.
References
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Journal ArticleDOI
The hallmarks of cancer.
TL;DR: This work has been supported by the Department of the Army and the National Institutes of Health, and the author acknowledges the support and encouragement of the National Cancer Institute.
Journal ArticleDOI
Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene
Dennis J. Slamon,Gary M. Clark,Steven G. Wong,Wendy J. Levin,Axel Ullrich,William L. McGuire +5 more
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Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
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TL;DR: A subgroup of patients with non-small-cell lung cancer have specific mutations in the EGFR gene which correlate with clinical responsiveness to the tyrosine kinase inhibitor gefitinib, and these mutations lead to increased growth factor signaling and confer susceptibility to the inhibitor.
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Use of Chemotherapy plus a Monoclonal Antibody against HER2 for Metastatic Breast Cancer That Overexpresses HER2
Dennis J. Slamon,Brian Leyland-Jones,Steven Shak,Hank Fuchs,Virginia E. Paton,Alex Bajamonde,Thomas Fleming,Wolfgang Eiermann,Janet M. Wolter,Mark D. Pegram,José Baselga,Larry Norton +11 more
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EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy.
J. Guillermo Paez,Pasi A. Jänne,Pasi A. Jänne,Jeffrey C. Lee,Sean Tracy,Heidi Greulich,Heidi Greulich,Stacey Gabriel,Paula Herman,Frederic J. Kaye,Neal I. Lindeman,Titus J. Boggon,Katsuhiko Naoki,Hidefumini Sasaki,Yoshitaka Fujii,Michael J. Eck,William R. Sellers,William R. Sellers,William R. Sellers,Bruce E. Johnson,Bruce E. Johnson,Matthew Meyerson,Matthew Meyerson +22 more
TL;DR: Results suggest that EGFR mutations may predict sensitivity to gefitinib, and treatment with the EGFR kinase inhibitor gefitsinib causes tumor regression in some patients with NSCLC, more frequently in Japan.
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