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Review

Recent advances in the design and discovery of small-molecule therapeutics targeting HER2/neu

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Pages 83-102 | Published online: 03 Jan 2007

Bibliography

  • SCHLESSINGER J: Cell signaling by receptor tyrosine kinases. Cell (2000) 103(2):211-225.
  • WELLS A: EGF receptor. Int. J. Biochem. Cell Biol. (1999) 31(6):637-643.
  • GUY PM, PLATKO JV, CANTLEY LC, CERIONE RA, CARRAWAY KL III: Insect cell-expressed p180erbB3 possesses an impaired tyrosine kinase activity. Proc. Natl. Acad. Sci. USA (1994) 91(17):8132-8136.
  • JONES JT, AKITA RW, SLIWKOWSKI MX: Binding specificities and affinities of egf domains for ErbB receptors. FEBS Lett. (1999) 447(2-3):227-231.
  • GULLICK WJ: The type 1 growth factor receptors and their ligands considered as a complex system. Endocr. Relat. Cancer (2001) 8(2):75-82.
  • CHO HS, MASON K, RAMYAR KX et al.: Structure of the extracellular region of HER2 alone and in complex with the herceptin Fab. Nature (2003) 421(6924):756-760.
  • GARRETT TP, MCKERN NM, LOU M et al.: The crystal structure of a truncated ErbB2 ectodomain reveals an active conformation, poised to interact with other ErbB receptors. Mol. Cell (2003) 11(2):495-505.
  • ALIMANDI M, ROMANO A, CURIA MC et al.: Cooperative signaling of ErbB3 and ErbB2 in neoplastic transformation and human mammary carcinomas. Oncogene (1995) 10(9):1813-1821.
  • BLENIS J: Signal transduction via the MAP kinases: proceed at your own RSK. Proc. Natl. Acad. Sci. USA (1993) 90(13):5889-5892.
  • BURGERING BM, COFFER PJ: Protein kinase B (c-Akt) in phosphatidylinositol-3-OH kinase signal transduction. Nature (1995) 376(6541):599-602.
  • OLAYIOYE MA, NEVE RM, LANE HA, HYNES NE: The ErbB signaling network: receptor heterodimerization in development and cancer. Embo. J. (2000) 19(13):3159-3167.
  • ZHANG W, LIU HT: MAPK signal pathways in the regulation of cell proliferation in mammalian cells. Cell Res. (2002) 12(1):9-18.
  • CANTLEY LC: The phosphoinositide 3-kinase pathway. Science (2002) 296(5573):1655-1657.
  • MOSCATELLO DK, HOLGADO-MADRUGA M, EMLET DR, MONTGOMERY RB, WONG AJ: Constitutive activation of phosphatidylinositol 3-kinase by a naturally occurring mutant epidermal growth factor receptor. J. Biol. Chem. (1998) 273(1):200-206.
  • HYNES NE, LANE HA: ERBB receptors and cancer: the complexity of targeted inhibitors. Nat. Rev. Cancer (2005) 5(5):341-354.
  • SLAMON DJ, CLARK GM, WONG SG et al.: Human breast cancer: correlation of relapse and survival with amplification of the HER-2/neu oncogene. Science (1987) 235(4785):177-182.
  • SLAMON DJ, GODOLPHIN W, JONES LA et al.: Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. Science (1989) 244(4905):707-712.
  • KAPITANOVIC S, RADOSEVIC S, KAPITANOVIC M et al.: The expression of p185(HER-2/neu) correlates with the stage of disease and survival in colorectal cancer. Gastroenterology (1997) 112(4):1103-1113.
  • NAHTA R, ESTEVA FJ: HER-2-targeted therapy: lessons learned and future directions. Clin. Cancer Res. (2003) 9(14):5078-5084.
  • SLIWKOWSKI MX, LOFGREN JA, LEWIS GD et al.: Nonclinical studies addressing the mechanism of action of trastuzumab (Herceptin). Semin. Oncol. (1999) 26(4 Suppl. 12):60-70.
  • DREBIN JA, LINK VC, STERN DF, WEINBERG RA, GREENE MI: Down-modulation of an oncogene protein product and reversion of the transformed phenotype by mAbs. Cell (1985) 41(3):697-706.
  • IZUMI Y, XU L, DI TOMASO E, FUKUMURA D, JAIN RK: Tumour biology: herceptin acts as an anti-angiogenic cocktail. Nature (2002) 416(6878):279-280.
  • PICCART-GEBHART MJ, PROCTER M, LEYLAND-JONES B et al.: Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N. Engl. J. Med. (2005) 353(16):1659-1672.
  • AGUS DB, AKITA RW, FOX WD et al.: Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell (2002) 2(2):127-137.
  • FRANKLIN MC, CAREY KD, VAJDOS FF et al.: Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex. Cancer Cell (2004) 5(4):317-328.
  • RABINDRAN SK: Antitumor activity of HER-2 inhibitors. Cancer Lett. (2005) 227(1):9-23.
  • MOULDER SL, YAKES FM, MUTHUSWAMY SK et al.: Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer Res. (2001) 61(24):8887-8895.
  • MOASSER MM, BASSO A, AVERBUCH SD, ROSEN N: The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. (2001) 61(19):7184-7188.
  • ANDERSON NG, AHMAD T, CHAN K, DOBSON R, BUNDRED NJ: ZD1839 (Iressa), a novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, potently inhibits the growth of EGFR-positive cancer cell lines with or without ErbB2 overexpression. Int. J. Cancer (2001) 94(6):774-782.
  • ARORA A, SCHOLAR EM: Role of tyrosine kinase inhibitors in cancer therapy. J. Pharmacol. Exp. Ther. (2005) 315(3):971-979.
  • XIA W, MULLIN RJ, KEITH BR et al.: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/ErbB2 and downstream Erk1/2 and AKT pathways. Oncogene (2002) 21(41):6255-6263.
  • RUSNAK DW, LACKEY K, AFFLECK K et al.: The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor- derived cell lines in vitro and in vivo. Mol. Cancer Ther. (2001) 1(2):85-94.
  • BENCE AK, ANDERSON EB, HALEPOTA MA et al.: Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. Invest. New Drugs (2005) 23(1):39-49.
  • XIA W, LIU LH, HO P, SPECTOR NL: Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Oncogene (2004) 23(3):646-653.
  • KONECNY GE, PEGRAM MD, VENKATESAN N et al.: Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-over- expressing and trastuzumab-treated breast cancer cells. Cancer Res. (2006) 66(3):1630-1639.
  • XIA W, GERARD CM, LIU L et al.: Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene (2005) 24(41):6213-6221.
  • GEYER CE, CAMERON D, LINDQUIST D et al.: A Phase III randomized, open-label, international study comparing lapatinib and capecitabine vs capacitabine in women with refractory advanced or metastatic breast cancer (EGF100151). 2006 American Society of Clinical Oncology Annual Meeting. Atlanta, Georgia (2006).
  • SMAILL JB, PALMER BD, REWCASTLE GW et al.: Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor. J. Med. Chem. (1999) 42(10):1803-1815.
  • FRY DW, BRIDGES AJ, DENNY WA et al.: 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(20):12022-12027.
  • SIMON GR, GARRETT CR, OLSON SC et al.: Increased bioavailability of intravenous versus oral CI-1033, a pan erbB tyrosine kinase inhibitor: results of a Phase I pharmacokinetic study. Clin. Cancer Res. (2006) 12(15):4645-4651.
  • GARLAND LL, HIDALGO M, MENDELSON DS et al.: A Phase I clinical and pharmacokinetic study of oral CI-1033 in combination with docetaxel in patients with advanced solid tumors. Clin. Cancer Res. (2006) 12(14 Pt 1):4274-4282.
  • MOMOSE Y, MAEKAWA T, ODAKA H, IKEDA H, SOHDA T: Novel 5-substituted-1H-tetrazole derivatives as potent glucose and lipid lowering agents. Chem. Pharm. Bull. (Tokyo) (2002) 50(1):100-111.
  • MOMOSE Y, MAEKAWA T, YAMANO T et al.: Novel 5-substituted 2,4-thiazolidine- dione and 2,4-oxazolidinedione derivatives as insulin sensitizers with antidiabetic activities. J. Med. Chem. (2002) 45(7):1518-1534.
  • SRIDHAR SS, SEYMOUR L, SHEPHERD FA: Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol. (2003) 4(7):397-406.
  • NAGASAWA J, MIZOKAMI A, KOSHIDA K et al.: Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int. J. Urol. (2006) 13(5):587-592.
  • GUNDERSEN LL, MALTERUD KE, NEGUSSIE AH et al.: Indolizines as novel potent inhibitors of 15-lipoxygenase. Bioorg. Med. Chem. (2003) 11(24):5409-5415.
  • CHEN Z, KIM SH, BARBOSA SA et al.: Pyrrolopyridazine MEK inhibitors. Bioorg. Med. Chem. Lett (2006) 16(3):628-632.
  • HUNT JT, MITT T, BORZILLERI R et al.: Discovery of the pyrrolo[2,1-f][1,2,4] triazine nucleus as a new kinase inhibitor template. J. Med. Chem. (2004) 47(16):4054-4059.
  • FINK BE, VITE GD, MASTALERZ H et al.: New dual inhibitors of EGFR and HER2 protein tyrosine kinases. Bioorg. Med. Chem. Lett (2005) 15(21):4774-4779.
  • WONG TW, LEE FY, YU C et al.: Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin. Cancer Res. (2006) 12(20 Pt 1):6186-6193.
  • BORZILLERI RM, ZHENG X, QIAN L et al.: Design, synthesis and evaluation of orally active 4-(2,4-difluoro-5-(methoxy- carbamoyl)phenylamino)pyrrolo[2,1-f] [1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors. J. Med. Chem. (2005) 48(12):3991-4008.
  • BORZILLERI RM, CAI ZW, ELLIS C et al.: Synthesis and SAR of 4-(3-hydroxy- phenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors. Bioorg. Med. Chem. Lett. (2005) 15(5):1429-1433.
  • TRAXLER PM, FURET P, METT H et al.: 4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase. J. Med. Chem. (1996) 39(12):2285-2292.
  • TRAXLER P, BOLD G, BUCHDUNGER E et al.: Tyrosine kinase inhibitors: from rational design to clinical trials. Med. Res. Rev. (2001) 21(6):499-512.
  • HOEKSTRA R, DUMEZ H, ESKENS FA et al.: Phase I and pharmacologic study of PKI166, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. Clin. Cancer Res. (2005) 11(19 Pt 1):6908-6915.
  • MELLINGHOFF IK, TRAN C, SAWYERS CL: Growth inhibitory effects of the dual ErbB1/ErbB2 tyrosine kinase inhibitor PKI-166 on human prostate cancer xenografts. Cancer Res. (2002) 62(18):5254-5259.
  • CHANG CH, SCOTT GK, KUO WL et al.: ESX: a structurally unique Ets overexpressed early during human breast tumorigenesis. Oncogene (1997) 14(13):1617-1622.
  • LIN YZ, CLINTON GM: A soluble protein related to the HER-2 proto-oncogene product is released from human breast carcinoma cells. Oncogene (1991) 6(4):639-643.
  • PUPA SM, MENARD S, MORELLI D et al.: The extracellular domain of the c-erbB-2 oncoprotein is released from tumor cells by proteolytic cleavage. Oncogene (1993) 8(11):2917-2923.
  • KANDL H, SEYMOUR L, BEZWODAW R: Soluble c-erbB-2 fragment in serum correlates with disease stage and predicts for shortened survival in patients with early-stage and advanced breast cancer. Br. J. Cancer (1994) 70(4):739-742.
  • SAEZ R, MOLINA MA, RAMSEY EE et al.: p95HER-2 predicts worse outcome in patients with HER-2-positive breast cancer. Clin. Cancer Res. (2006) 12(2):424-431.
  • KERKELA R, GRAZETTE L, YACOBI R et al.: Cardiotoxicity of the cancer therapeutic agent imatinib mesylate. Nat. Med. (2006) 12(8):908-916.

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