Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library

Biochemical and Biophysical Research Communications

Volumn 389, Issue 3, 2009, Pages 415-419

  Kim, Eung Yoon ^a,b   Choi, Young Jin ^a,b   Park, Chan Won ^a   Kang, In Cheol ^a,b  

^a Hoseo University   (South Korea)

^b Innopharmascreen Inc   (South Korea)

Author keywords

Anti tumor agent; EGFR kinase; EGFR kinase inhibitor; In silico virtual screening; Protein chip

Indexed keywords

EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; ERKITINIB; ERLOTINIB; IPS 01001; IPS 01002; LAPATINIB; MONOCLONAL ANTIBODY; PHOSPHOLIPASE C GAMMA1; PROTEIN TYROSINE KINASE INHIBITOR; QUINAZOLINE; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; EGFR PROTEIN, HUMAN; EPIDERMAL GROWTH FACTOR RECEPTOR; PROTEIN KINASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL PROLIFERATION; COMPUTER MODEL; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG SCREENING; DRUG STRUCTURE; ENZYME PHOSPHORYLATION; HELA CELL; HUMAN; HUMAN CELL; IC 50; PHYTOCHEMISTRY; PRIORITY JOURNAL; PROTEIN MICROARRAY; PROTEIN PHOSPHORYLATION; CHEMISTRY; DRUG ANTAGONISM; ISOLATION AND PURIFICATION; METHODOLOGY;

ANTINEOPLASTIC AGENTS, PHYTOGENIC; DRUG SCREENING ASSAYS, ANTITUMOR; HELA CELLS; HUMANS; PROTEIN ARRAY ANALYSIS; PROTEIN KINASE INHIBITORS; RECEPTOR, EPIDERMAL GROWTH FACTOR;

EID: 70449709100     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2009.08.141     Document Type: Article

References (19)

1. M.F. Templin, D. Stroll, M. Schrenk, et al., Protein microarray technology, Trends Biotechnol. 20 (4) (2002) 160-166.
2. H. Zhu, J.F. Klemic, S. Chang, et al., Analysis of yeast protein kinases using protein chips, Nat. Genet. 26 (3) (2000) 283-289.
3. X. Han, G. Yamanouchi, T. Mori, et al., Monitoring protein kinase activity in cell lysates using a high-density peptide microarray, J. Biomol. Screen. 14 (3) (2009) 256-262.
4. A.A. San Juan, Towards predictive inhibitor design for the EGFR autophosphorylation activity, Eur. J. Med. Chem. 43 (4) (2008) 781-791.
5. J. Stamos, M.X. Sliwkowski, C. Eigenbrot, Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor, J. Biol. Chem. 277 (48) (2002) 46265-46272.
6. T. Shien, H. Doihara, H. Hara, et al., PLC and PI3K pathways are important in the inhibition of EGF-induced cell migration by gefitinib ('Iressa', ZD1839), Breast Cancer 11 (4) (2004) 367-373.
7. R.E. Gates, L.E. King Jr., Different forms of the epidermal growth factor receptor kinase have different autophosphorylation sites, Biochemistry 24 (19) (1985) 5209-5215.
8. W.J. Gullick, J. Downward, M.D. Waterfield, Antibodies to the autophosphorylation sites of the epidermal growth factor receptor proteintyrosine kinase as probes of structure and function, EMBO J. 4 (11) (1985) 2869-2877.
9. J. Downward, M.D. Waterfield, P.J. Parker, Autophosphorylation and protein kinase C phosphorylation of the epidermal growth factor receptor. Effect on tyrosine kinase activity and ligand binding affinity, J. Biol. Chem. 260 (27) (1985) 14538-14546.
10. E. Zwick et al., The EGF receptor as central transducer of heterologous signalling systems, Trends Pharmacol. Sci. 20 (10) (1999) 408-412.
11. D.R. Emlet, D.K. Moscatello, L.B. Ludlow, A.J. Wong, Subsets of epidermal growth factor receptors during activation and endocytosis, J. Biol. Chem. 272 (7) (1997) 4079-4086.
12. P. Mertins, H.C. Eberl, J. Renkawitz, et al., Investigation of protein-tyrosine phosphatase 1B function by quantitative proteomics, Mol. Cell Proteomics 7 (9) (2008) 1763-1777.
13. P. Chen, H. Xie, M.C. Sekar, K. Gupta, A. Wells, Epidermal growth factor receptor-mediated cell motility: phospholipase C activity is required, but mitogen-activated protein kinase activity is not sufficient for induced cell movement, J. Cell Biol. 127 (3) (1994) 847-857.
14. Y. Lee, E.K. Lee, Y.W. Cho, et al., ProteoChip: a highly sensitive protein microarray prepared by a novel method of protein immobilization for application of protein-protein interaction studies, Proteomics 3 (12) (2003) 2289-2304.
15. S.M. Khan, R.H. Oliver, J. Yeh, Epidermal growth factor receptor inhibition by tyrphostin 51 induces apoptosis in luteinized granulosa cells, J. Clin. Endocrinol. Metab. 90 (1) (2005) 469-473.
16. S. Skvortsov, B. Sarg, J. Loeffler-Ragg, et al., Different proteome pattern of epidermal growth factor receptor-positive colorectal cancer cell lines that are responsive and nonresponsive to C225 antibody treatment, Mol. Cancer Ther. 3 (12) (2004) 1551-1558.
17. Y.X. Fan, L. Wong, T.B. Deb, G.R. Johnson, Ligand regulates epidermal growth factor receptor kinase specificity: activation increases preference for GAB1 and SHC versus autophosphorylation sites, J. Biol. Chem. 279 (37) (2004) 38143-38150.
18. J. Gandhi, J. Zhang, Y. Xie, et al., Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines, PLoS One 4 (2) (2009) e4576.
19. U. McDermott, S.V. Sharma, J. Settleman, High-throughput lung cancer cell line screening for genotype-correlated sensitivity to an EGFR kinase inhibitor, Methods Enzymol. 438 (2008) 331-341.