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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Randomized Phase II Study of Dacomitinib (PF-00299804), an Irreversible Pan-Human Epidermal Growth Factor Receptor Inhibitor, Versus Erlotinib in Patients With Advanced Non-Small-Cell Lung Cancer
Suresh S. Ramalingam,Fiona H Blackhall,Maciej Krzakowski,Carlos H. Barrios,Keunchil Park,Isabel Bover,Dae Seog Heo,Rafael Rosell,Denis C. Talbot,Richard G. Frank,Stephen P. Letrent,Ana Ruiz-Garcia,Ian Taylor,Jane Q. Liang,A. Campbell,Joe O'Connell,Michael Boyer +16 more
TL;DR: Dacomitinib demonstrated significantly improved PFS versus erlotinib, with acceptable toxicity, in patients with advanced non-small-cell lung cancer (NSCLC), and PFS benefit was observed in most clinical and molecular subsets, notably KRAS wild-type/EGFR any status, EGFR wild- type, and EGFR mutants.
Journal ArticleDOI
Direct activation of TACE-mediated ectodomain shedding by p38 MAP kinase regulates EGF receptor-dependent cell proliferation.
Pinglong Xu,Rik Derynck +1 more
TL;DR: Autocrine EGF receptor activation through TACE-mediated ectodomain shedding intimately links inflammation and cancer progression and may play a role in stress and conditions that relate to p38 MAP kinase activation.
Journal ArticleDOI
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
Xiong Cai,Haixiao Zhai,Jing Wang,Jeffrey Forrester,Hui Qu,Ling Yin,Cheng-Jung Lai,Rudi Bao,Changgeng Qian +8 more
TL;DR: The results suggest that a single compound that simultaneously inhibits HDAC, EGFR, and HER2 may offer greater therapeutic benefits in cancer over single-acting agents through the interference with multiple pathways and potential synergy among HDAC and EGFR/HER2 inhibitors.
Journal ArticleDOI
Targeting the tumor microenvironment with interferon-β bridges innate and adaptive immune responses
Xuanming Yang,Xunmin Zhang,May Lynne Fu,Ralph Ralph R Weichselbaum,Thomas F. Gajewski,Yajun Guo,Yang Xin Fu,Yang Xin Fu +7 more
TL;DR: A next-generation Ab-based immunotherapy that targets and eradicates established Ab-resistant tumors and blocking PD-L1 overcomes treatment-acquired resistance and completely eradicatesestablished tumors is established.
Journal ArticleDOI
EGFR amplification and lack of activating mutations in metaplastic breast carcinomas
Jorge S. Reis-Filho,Céline Pinheiro,M B K Lambros,Fernanda Milanezi,Fernanda Milanezi,Silvia Carvalho,Kay Savage,Peter T. Simpson,Chris Jones,Sally Swift,Alan Mackay,Rui Manuel Reis,Jason L. Hornick,Emílio M. Pereira,Fátima Baltazar,Christopher D.M. Fletcher,Alan Ashworth,Sunil R. Lakhani,Fernando Schmitt +18 more
TL;DR: It is indicated that further studies are warranted to explore EGFR tyrosine kinase inhibitors as potential therapeutic agents for metaplastic breast carcinomas harbouring amplification of 7p11.2.
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
TL;DR: Amplification of the HER-2/neu gene was a significant predictor of both overall survival and time to relapse in patients with breast cancer, and had greater prognostic value than most currently used prognostic factors in lymph node-positive disease.
Journal ArticleDOI
Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib
Thomas J. Lynch,Daphne W. Bell,Raffaella Sordella,Sarada Gurubhagavatula,Ross A. Okimoto,Brian W. Brannigan,Patricia L. Harris,Sara M. Haserlat,Jeffrey G. Supko,Frank G. Haluska,David N. Louis,David C. Christiani,Jeff Settleman,Daniel A. Haber +13 more
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.
Journal ArticleDOI
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
TL;DR: The addition of trastuzumab to chemotherapy was associated with a longer time to disease progression, a higher rate of objective response, a longer duration of response, and a lower rate of death at 1 year.
Journal ArticleDOI
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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