Epidermal growth factor receptor tyrosine kinase

Wakeling, A. 2002. Epidermal growth factor receptor tyrosine kinase inhibitors. Current Opinion in Pharmacology 2(4), 382-387. 

The unbound fraction of the epidermal growth factor receptor tyrosine kinase inhibitor gefitinib has been extensively studied in cancer patients [39]. The drug was found to bind to serum albumin, oq-acid glycoprotein, and red blood cells with a mean unbound fraction of 3.4% which was constant over 28 days of dosing. Unbound fraction ranged from 2.2% to 5.4% and was inversely correlated with pre-treatment levels of oq-acid glycoprotein. 

Kris, M.G. et al.. Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer a randomized trial, JAMA, 290, 2149-2158, 2003. 

Nakamura, Y., Oka, M., Soda, H., et al. (2005) Gefitinib ( Iressa, ZD1839), an epidermal growth factor receptor tyrosine kinase inhibitor, reverses breast cancer resistance protein/ ABCG2-mediated drug resistance. Cancer Res. 65, 1541-1546. 

Raymond E, Faivre S, Armand JP. Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs 2000 60 Suppl 1 15-23. 

Woodburn JR, Kendrew J, Fennell M, et al. ZD1839 ( Iressa ), a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) inhibition of c-fos mRNA, an intermediate marker of... 

Carey KD, Garton AJ, Romero MS et al. Kinetic analysis of epidermal growth factor receptor somatic mutant proteins shows increased sensitivity to the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib. Cancer Res 2006 66 8163-8171. 

Burris HA, 3rd, Hurwitz HI, Dees EC et al. Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW5720I6), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. JCfiri Oncol2005 23 5305-5313. Zaks T, Akkari A, Briley L et al. Role of pharmacogenetic studies in early clinical development Phase I studies with lapatinib. JCfiW Oncol 2006 24 3029. 

S. K. Kelley, and A. Sandler. 2005. Phase I/II trial evaluating the anti-vascular endothelial growth factor monoclonal antibody bevacizumab in combination with the HER-l/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib for patients with recurrent non-small-cell lung cancer./. Clin. Oncol. 23 2544-2555. 

Tan AR et al (2004) Evaluation of biologic end points and pharmacokinetics in patients with metastatic breast cancer after treatment with erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor. J Clin Oncol 22 3080-3090... 

Cyanidin inhibits epidermal growth factor receptor tyrosine kinase (EGF-RTK), a-glycosidase and COX-1 and COX-2. Delphinidin (3,5,7,3, 4, 5 -hexahydroxyflavylium) also inhibits EGF-RTK. Anthocyanidins and anthocyanins can be anti-inflammatory antioxidants by acting as free radical scavengers. Thus, nasunin (delphinidin-3-(j6-coumaroylrutinoside)-5-glucoside) scavenges OH (hydroxyl), 02 (superoxide) and lipid peroxyl radicals and inhibits lipid peroxidation. 

Inhibition of the epidermal growth factor receptor tyrosine kinase activity by Leflunomide. FEBS Lett. 334,161-164. 

PHOSPHORYLA TWN chronic myelongenous leukemia-associated KIO BCR-ABL Drosophila Kr protein hepatitis B virus core and precore antigens human c-fos protein human c-myc protein human EGF receptor human epidermal growth factor receptor (tyrosine kinase domain) human immunodeficiency virus p24 human immunodeficiency virus tat protein human insulin receptor 6-subunit human insulin receptor - tyrosine kinase domain... 

Yoon SJ, Nakayama K, Hikita T, Handa K, Hakomori SI. Epidermal growth factor receptor tyrosine kinase is modulated by... 

Miller VA, Johnson D, Heelan RT, Pizzo BA, Perez WJ, et al. 2001. A pilot trial demonstrates the safety ofZD1839 ( Iressa ), an oral epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), in combination with car-boplatin (C) and paclitaxel (P) in previously untreated advanced non-small cell lung cancer (NSCLC). Proc. Am. Soc. Clin. Oncol. 20 1301 (Abstr.)... 

Moyer JD, Barbacci EG, Iwata KK, Arnold L, Boman B, et al. 1997. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 57 4838 18... 

Hidalgo M, Siu LL, Nemunaitis J, Rizzo J, Hammond LA, et al. 2001. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J. Clin. Oncol. 19 3267-79... 

Li J, Cusatis G, Brahmer J, Sparreboom A, Robey RW, Bates SE, Hidalgo M, Baker SD (2007) Association of variant ABCG2 and the pharmacokinetics of epidermal growth factor receptor tyrosine kinase inhibitors in cancer patients. Cancer Biol Ther 6 432 438... 

Ward, W. H. J., Cook, P. N., Slater, A. M., Davies, D. H., Holdgate, G. A., Green, L. R. Epidermal growth factor receptor tyrosine kinase investigation of catalytic mechatusm, structure-based... 

Taguchi, F. et al., Mass spectrometry to classify non-small-cell lung cancer patients for clinical outcome after treatment with epidermal growth factor receptor tyrosine kinase inhibitors A multicohort cross-institutional study, J. Natl. Cancer Inst., 99(11), 838, 2007. 

Hirata, A., S. Ogawa, T. Kometani, T. Kuwano, S. Naito, M. Kuwano, and M. Ono. ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase. Cancer Res 62 2554-60, 2002. 

Lee, L.T. et al.. Blockade of the epidermal growth factor receptor tyrosine kinase activity by quercetin and luteolin leads to growth inhibition and apoptosis of pancreatic tumor cells. Anticancer Res., 22, 1615,2002. 

Wacker B et al. Correlation between development of rash and efficacy in patients treated with the epidermal growth factor receptor tyrosine kinase inhibitor erlotinib in two large phase III studies. Clinical Cancer Research 2007 13 3913-3921. 

Massarelli E et al. KRAS mutation is an important predictor of resistance to therapy with epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancer. Clinical Cancer Research 2007 13 2890-2896. 

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