Biochemical Assay-Based Selectivity Profiling of Clinically Relevant Kinase Inhibitors on Mutant Forms of EGF Receptor

REFERENCES

• Gridelli C, Bareschino M A, Schettino C, Rossi A, Maione P, Ciardiello F. Erlotinib in non-small cell lung cancer treatment: Current status and future development. Oncologist 2007; 12: 840–849
   PubMed Web of Science ®Google Scholar
• Scagliotti G V, Selvaggi G. The place of targeted therapies in the management of non-small cell bronchial carcinoma. Target therapies in lung cancer management. Rev Mal Respir 2006; 23: 16S137–16S147
   Google Scholar
• Fukuoka M, Yano S, Giaccone G, Tamura T, Nakagawa K, Douillard J Y, Nishiwaki Y, Vansteenkiste J, Kudoh S, Rischin D, Eek R, Horai T, Noda K, Takata I, Smit E, Averbuch S, Macleod A, Feyereislova A, Dong R P, Baselga J. Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial). J Clin Oncol 2003; 21: 2237–2246
   PubMed Web of Science ®Google Scholar
• Pérez-Soler R, Chachoua A, Hammond L A, Rowinsky E K, Huberman M, Karp D, Rigas J, Clark G M, Santabárbara P, Bonomi P. Determinants of tumor response and survival with erlotinib in patients with non–small-cell lung cancer. J Clin Oncol 2004; 22: 3238–3247
   PubMed Web of Science ®Google Scholar
• Lynch T J, Bell D W, Sordella R, Gurubhagavatula S, Okimoto R A, Brannigan B W, Harris P L, Haserlat S M, Supko J G, Haluska F G, Louis D N, Christiani D C, Settleman J, Haber D A. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med 2004; 20: 2129–2139
   Google Scholar
• Sordella R, Bell D W, Haber D A, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004; 305: 1163–1167
   PubMed Web of Science ®Google Scholar
• Kosaka T, Yatabe Y, Endoh H, Kuwano H, Takahashi T, Mitsudomi T. Mutations of the epidermal growth factor receptor gene in lung cancer: biological and clinical implications. Cancer Res 2004; 64: 8919–8923
   PubMed Web of Science ®Google Scholar
• Pao W, Miller V A, Politi K A, Riely G J, Somwar R, Zakowski M F, Kris M G, Varmus H. Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med 2005; 2: e73
   PubMed Web of Science ®Google Scholar
• Carter T A, Wodicka L M, Shah N P, Velasco A M, Fabian M A, Treiber D K, Milanov Z V, Atteridge C E, Biggs W H, III, Edeen P T, Floyd M, Ford J M, Grotzfeld R M, Herrgard S, Insko D E, Mehta S A, Patel H K, Pao W, Sawyers C L, Varmus H, Zarrinkar P P, Lockhart D J. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci USA 2005; 102: 11011–11016
   PubMed Web of Science ®Google Scholar
• Bridges A J, Zhou H, Cody D R, Rewcastle G W, Mc Michael A, Showalter H D, Fry D W, Kraker A J, Denny W A. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem 1996; 39: 267–276
   PubMed Web of Science ®Google Scholar
• Partik G, Hochegger K, Schorkhuber M, Marian B. Inhibition of epidermal-growth-factor-receptor-dependent signalling by tyrphostins A25 and AG1478 blocks growth and induces apoptosis in colorectal tumor cells in vitro. J Cancer Res Clin Oncol 1999; 125: 379–388
   PubMedGoogle Scholar
• Copeland R A. Evaluation of Enzyme Inhibitors in Drug Discovery. Effect of Tight Binding Inhibition Concentration-Response Data. John Wiley & Sons, Inc., Hoboken, NJ 2005; 179–180
   Google Scholar
• Zhang X, Gureasko J, Shen K, Cole P A, Kuriyan J. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006; 125: 1137–1149
   PubMed Web of Science ®Google Scholar
• Rarey M, Kramer B, Lengauer T, Klebe G. A fast flexible docking method using an incremental construction algorithm. J. Mol. Biol 1996; 261: 470–489
   Google Scholar
• Riely G J, Pao W, Pham D, Li A R, Rizvi N, Venkatraman E S, Zakowski M F, Kris M G, Ladanyi M, Miller V A. Clinical course of patients with non-small cell lung cancer and epidermal growth factor receptor exon 19 and exon 21 mutations treated with gefitinib or erlotinib. Clin Cancer Res 2006; 12: 839–844
   PubMed Web of Science ®Google Scholar
• Fry D W, Bridges A J, Denny W A, Doherty A, Greis K D, Hicks J L, Hook K E, Keller P R, Leopold W R, Loo J A, Mc Namara D J, Nelson J M, Sherwood V, Smaill J B, Trumpp-Kallmeyer S, Dobrusin E M. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci USA 1998; 95: 12022–12027
   PubMed Web of Science ®Google Scholar
• Mukohara T, Engelman J A, Hanna N H, Yeap B Y, Kobayashi S, Lindeman N, Halmos B, Pearlberg J, Tsuchihashi Z, Cantley L C, Tenen D G, Johnson B E, Jänne P A. Differential effects of gefitinib and cetuximab on non-small-cell lung cancers bearing epidermal growth factor receptor mutations. J Natl Cancer Inst 2005; 97: 1185–1194
   PubMed Web of Science ®Google Scholar
• Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, Singh B, Heelan R, Rusch V, Fulton L, Mardis E, Kupfer D, Wilson R, Kris M, Varmus H. EGF receptor gene mutations are common in lung cancers from “ever smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci USA 2004; 101: 13306–13311
   PubMed Web of Science ®Google Scholar
• Mitsudomi T, Kosaka T, Endoh H, Horio Y, Hida T, Mori S, Hatooka S, Shinoda M, Takahashi T, Yatabe Y. Mutations of the epidermal growth factor receptor gene predict prolonged survival after gefitinib treatment in patients with non-small-cell lung cancer with postoperative recurrence. J Clin Oncol 2005; 23: 2513–2520
   PubMed Web of Science ®Google Scholar
• Kwak E L, Sordella R, Bell D W, Godin-Heymann N, Okimoto R A, Brannigan B W, Harris P L, Driscoll D R, Fidias P, Lynch T J, Rabindran S K, Mc Ginnis J P, Wissner A, Sharma S V, Isselbacher K J, Settleman J, Haber D A. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci USA 2005; 102: 7665–7670
   PubMed Web of Science ®Google Scholar
• Wang S E, Narasanna A, Perez-Torres M, Xiang B, Wu F Y, Yang S, Carpenter G, Gazdar A F, Muthuswamy S K, Arteaga C L. HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors. Cancer Cel 2006; 10: 25–38
   PubMed Web of Science ®Google Scholar