Ligand-based receptor tyrosine kinase partial agonists: New paradigm for cancer drug discovery?

Expert Opinion on Drug Discovery

Volumn 6, Issue 2, 2011, Pages 185-193

  Riese II, David J ^a  

^a AUBURN UNIVERSITY   (United States)

Author keywords

ErbB EGF receptors; ligand based antagonists; receptor partial agonists and antagonists; receptor tyrosine kinases; targeted cancer chemotherapeutics

Indexed keywords

BEVACIZUMAB; CETUXIMAB; EPIDERMAL GROWTH FACTOR RECEPTOR; ERLOTINIB; GEFITINIB; IMATINIB; LIGAND; NEU DIFFERENTIATION FACTOR; PERTUZUMAB; PROTEIN TYROSINE KINASE; RECOMBINANT PROTEIN; RITUXIMAB; TRASTUZUMAB;

B CELL LYMPHOMA; BREAST CANCER; BREAST TUMOR; CANCER CHEMOTHERAPY; CHRONIC MYELOID LEUKEMIA; COLORECTAL CANCER; DRUG MECHANISM; GASTROINTESTINAL STROMAL TUMOR; HUMAN; KIDNEY CANCER; LIGAND BINDING; LUNG NON SMALL CELL CANCER; PRIORITY JOURNAL; REVIEW; SIGNAL TRANSDUCTION;

EID: 79251502034     PISSN: 17460441     EISSN: None     Source Type: Journal    
DOI: 10.1517/17460441.2011.547468     Document Type: Review

References (54)

1. Lemmon MA, Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell 2010;141(7):1117-34
2. Lemmon MA. Ligand-induced ErbB receptor dimerization. Exp Cell Res 2009;315(4):638-48
3. Jura N, Endres NF, Engel K, et al. Mechanism for activation of the EGF receptor catalytic domain by the juxtamembrane segment. Cell 2009;137(7):1293-307
4. Zhang X, Gureasko J, Shen K, et al. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell 2006;125(6):1137-49
5. Hubbard SR EGF receptor activation: push comes to shove. Cell 2006;125(6):1029-31
6. Landau M, Fleishman SJ, Ben-Tal N. A putative mechanism for downregulation of the catalytic activity of the EGF receptor via direct contact between its kinase and C-terminal domains. Structure 2004;12(12):2265-75
7. Aifa S, Miled N, Frikha F, et al. Electrostatic interactions of peptides flanking the tyrosine kinase domain in the epidermal growth factor receptor provides a model for intracellular dimerization and autophosphorylation. Proteins 2006;62(4):1036-43
8. Waller CF. Imatinib mesylate. Recent Results Cancer Res 2010;184:3-20
9. Stegmeier F, Warmuth M, Sellers WR, Dorsch M. Targeted cancer therapies in the twenty-first century: lessons from imatinib. Clin Pharmacol Ther 2010;87(5):543-52
10. Shi F, Telesco SE, Liu Y, et al. ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation. Proc Natl Acad Sci USA 2010;107(17):7692-7
11. Pierotti MA, Negri T, Tamborini E, et al. Targeted therapies: the rare cancer paradigm. Mol Oncol 2010;4(1):19-37
12. Mena AC, Pulido EG, Guillen-Ponce C. Understanding the molecular-based mechanism of action of the tyrosine kinase inhibitor: sunitinib. Anticancer Drugs 2010;21(Suppl 1):S3-11
13. Bayraktar UD, Bayraktar S, Rocha-Lima CM. Molecular basis and management of gastrointestinal stromal tumors. World J Gastroenterol 2010;16(22):2726-34
14. An X, Tiwari AK, Sun Y, et al. BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review. Leuk Res 2010;34(10):1255-68
15. Agrawal M, Garg RJ, Cortes J, Quintas-Cardama A. Tyrosine kinase inhibitors: the first 5 decade. Curr Hematol Malig Rep 2010;5(2):70-80
16. De Luca A, Normanno N. Predictive biomarkers to tyrosine kinase inhibitors for the epidermal growth factor receptor in non-small-cell lung cancer. Curr Drug Targets 2010;11(7):851-64
17. Gazdar AF. Epidermal growth factor receptor inhibition in lung cancer: the evolving role of individualized therapy. Cancer Metastasis Rev 2010;29(1):37-48
18. Beers SA, Chan CH, French RR, et al. CD20 as a target for therapeutic type I and II monoclonal antibodies. Semin Hematol 2010;47(2):107-14
19. Capietto AH, Keirallah S, Gross E, et al. Emerging concepts for the treatment of hematological malignancies with therapeutic monoclonal antibodies. Curr Drug Targets 2010;11(7):790-800
20. Cillessen SA, Meijer CJ, Notoya M, et al. Molecular targeted therapies for diffuse large B-cell lymphoma based on apoptosis profiles. J Pathol 2010;220(5):509-20
21. Czuczman MS, Gregory SA. The future of CD20 monoclonal antibody therapy in B-cell malignancies. Leuk Lymphoma 2010;51(6):983-94
22. Hagemeister F. Rituximab for the treatment of non-Hodgkin's lymphoma and chronic lymphocytic leukaemia. Drugs 2010;70(3):261-72
23. Weiner GJ. Rituximab: mechanism of action. Semin Hematol 2010;47(2):115-23
24. Bossung V, Harbeck N. Angiogenesis inhibitors in the management of breast cancer. Curr Opin Obstet Gynecol 2010;22(1):79-86
25. Greenberg S, Rugo HS. Triple-negative breast cancer: role of antiangiogenic agents. Cancer J 2010;16(1):33-8
26. Korpanty G, Smyth E, Sullivan LA, et al. Antiangiogenic therapy in lung cancer: focus on vascular endothelial growth factor pathway. Exp Biol Med (Maywood) 2010;235(1):3-9
27. Koutras AK, Fountzilas G, Makatsoris T, et al. Bevacizumab in the treatment of breast cancer. Cancer Treat Rev 2010;36(1):75-82
28. Loupakis F, Bocci G, Pasqualetti G, et al. Targeting vascular endothelial growth factor pathway in first-line treatment of metastatic colorectal cancer: state-of-the-art and future perspectives in clinical and molecular selection of patients. Curr Cancer Drug Targets 2010;10(1):37-45
29. McDermott DF, George DJ. Bevacizumab as a treatment option in advanced renal cell carcinoma: an analysis and interpretation of clinical trial data. Cancer Treat Rev 2010;36(3):216-23
30. Ramalingam SS, Belani CP. Antiangiogenic agents in the treatment of nonsmall cell lung cancer: reality and hope. Curr Opin Oncol 2010;22(2):79-85
31. Welch S, Spithoff K, Rumble RB, Maroun J. Bevacizumab combined with chemotherapy for patients with advanced colorectal cancer: a systematic review. Ann Oncol 2010;21(6):1152-62
32. Ruzzo A, Graziano F, Canestrari E, Magnani M. Molecular predictors of efficacy to anti-EGFR agents in colorectal cancer patients. Curr Cancer Drug Targets 2010;10(1):68-79
33. Vincenzi B, Zoccoli A, Pantano F, et al. Cetuximab: from bench to bedside. Curr Cancer Drug Targets 2010;10(1):80-95
34. Kristjansdottir K, Dizon D. HER-dimerization inhibitors: evaluating pertuzumab in women's cancers. Expert Opin Biol Ther 2010;10(2):243-50
35. Langdon SP, Faratian D, Nagumo Y, et al. Pertuzumab for the treatment of ovarian cancer. Expert Opin Biol Ther 2010;10(7):1113-20
36. Barros FF, Powe DG, Ellis IO, Green AR Understanding the HER family in breast cancer: interaction with ligands, dimerization and treatments. Histopathology 2010;56(5):560-72
37. Brufsky A. Trastuzumab-based therapy for patients with HER2-positive breast cancer: from early scientific development to foundation of care. Am J Clin Oncol 2010;33(2):186-95
38. Esteva FJ, Yu D, Hung MC, Hortobagyi GN. Molecular predictors of response to trastuzumab and lapatinib in breast cancer. Nat Rev Clin Oncol 2010;7(2):98-107
39. Tagliabue E, Balsari A, Campiglio M, Pupa SM. HER2 as a target for breast cancer therapy. Expert Opin Biol Ther 2010;10(5):711-24
40. Hudziak RM, Lewis GD, Winget M, et al. p185HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor. Mol Cell Biol 1989;9(3):1165-72
41. Gilmore JL, Riese DJ III. secErbB4-26/549 antagonizes ligand-induced ErbB4 tyrosine phosphorylation. Oncol Res 2004;14(11-12):589-602
42. Klein DE, Nappi VM, Reeves GT, et al. Argos inhibits epidermal growth factor receptor signalling by ligand sequestration. Nature 2004;430(7003):1040-4
43. Klein DE, Stayrook SE, Shi F, et al. Structural basis for EGFR ligand sequestration by Argos. Nature 2008;453(7199):1271-5
44. Nelson J, Allen WE, Scott WN, et al. Murine epidermal growth factor (EGF) fragment (33-42) inhibits both EGF-and laminin-dependent endothelial cell motility and angiogenesis. Cancer Res 1995;55(17):3772-6
45. Wilson KJ, Gilmore JL, Foley J, et al. Functional selectivity of EGF family peptide growth factors: implications for cancer. Pharmacol Ther 2009;122(1):1-8
46. Gilmore JL, Scott JA, Bouizar Z, et al. Amphiregulin-EGFR signaling regulates PTHrP gene expression in breast cancer cells. Breast Cancer Res Treat 2008;110(3):493-505
47. Willmarth NE, Baillo A, Dziubinski ML, et al. Altered EGFR localization and degradation in human breast cancer cells with an amphiregulin/EGFR autocrine loop. Cell Signal 2009;21(2):212-19
48. Alvarado D, Klein DE, Lemmon MA. Structural basis for negative cooperativity in growth factor binding to an EGF receptor. Cell 2010;142(4):568-79
49. Hobbs SS, Cameron EM, Hammer RP, et al. Five carboxyl-terminal residues of neuregulin2 are critical for stimulation of signaling by the ErbB4 receptor tyrosine kinase. Oncogene 2004;23(4):883-93
50. Hobbs SS, Coffing SL, Le AT, et al. Neuregulin isoforms exhibit distinct patterns of ErbB family receptor activation. Oncogene 2002;21(55):8442-52
51. Hobbs SS, Gallo RM, Riese DJ Jr. Phe45 of NRG2beta is critical for the affinity of NRG2beta for ErbB4 and for potent stimulation of ErbB4 signaling by NRG2beta*. Growth Factors 2005;23(4):273-83
52. Wilson KJ, Mill CP, Cameron EM, et al. Inter-conversion of neuregulin2 full and partial agonists for ErbB4. Biochem Biophys Res Commun 2007;364(2):351-7
53. Gilmore JL, Gallo RM, Riese DJ II. The epidermal growth factor receptor (EGFR)-S442F mutant displays increased affinity for neuregulin-2beta and agonist-independent coupling with downstream signalling events. Biochem J 2006;396(1):79-88
54. Riese DJ II, Gallo RM, Settleman J. Mutational activation of ErbB family receptor tyrosine kinases: insights into mechanisms of signal transduction and tumorigenesis. Bioessays 2007;29(6):558-65