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Items: 22


Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.

Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1332-6. doi: 10.1016/j.bmcl.2009.01.080. Epub 2009 Feb 7.


Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.

Rheault TR, Caferro TR, Dickerson SH, Donaldson KH, Gaul MD, Goetz AS, Mullin RJ, McDonald OB, Petrov KG, Rusnak DW, Shewchuk LM, Spehar GM, Truesdale AT, Vanderwall DE, Wood ER, Uehling DE.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011. Epub 2008 Dec 7.


Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.

Stevens KL, Alligood KJ, Alberti JG, Caferro TR, Chamberlain SD, Dickerson SH, Dickson HD, Emerson HK, Griffin RJ, Hubbard RD, Keith BR, Mullin RJ, Petrov KG, Gerding RM, Reno MJ, Rheault TR, Rusnak DW, Sammond DM, Smith SC, Uehling DE, Waterson AG, Wood ER.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):21-6. doi: 10.1016/j.bmcl.2008.11.023. Epub 2008 Nov 13.


Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.

Hubbard RD, Dickerson SH, Emerson HK, Griffin RJ, Reno MJ, Hornberger KR, Rusnak DW, Wood ER, Uehling DE, Waterson AG.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5738-40. doi: 10.1016/j.bmcl.2008.09.090. Epub 2008 Sep 27.


6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.

Wood ER, Shewchuk LM, Ellis B, Brignola P, Brashear RL, Caferro TR, Dickerson SH, Dickson HD, Donaldson KH, Gaul M, Griffin RJ, Hassell AM, Keith B, Mullin R, Petrov KG, Reno MJ, Rusnak DW, Tadepalli SM, Ulrich JC, Wagner CD, Vanderwall DE, Waterson AG, Williams JD, White WL, Uehling DE.

Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):2773-8. doi: 10.1073/pnas.0708281105. Epub 2008 Feb 19. Erratum in: Proc Natl Acad Sci U S A. 2008 Apr 22;105(16):6208.


Assessment of epidermal growth factor receptor (EGFR, ErbB1) and HER2 (ErbB2) protein expression levels and response to lapatinib (Tykerb, GW572016) in an expanded panel of human normal and tumour cell lines.

Rusnak DW, Alligood KJ, Mullin RJ, Spehar GM, Arenas-Elliott C, Martin AM, Degenhardt Y, Rudolph SK, Haws TF Jr, Hudson-Curtis BL, Gilmer TM.

Cell Prolif. 2007 Aug;40(4):580-94.


Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.

King AJ, Patrick DR, Batorsky RS, Ho ML, Do HT, Zhang SY, Kumar R, Rusnak DW, Takle AK, Wilson DM, Hugger E, Wang L, Karreth F, Lougheed JC, Lee J, Chau D, Stout TJ, May EW, Rominger CM, Schaber MD, Luo L, Lakdawala AS, Adams JL, Contractor RG, Smalley KS, Herlyn M, Morrissey MM, Tuveson DA, Huang PS.

Cancer Res. 2006 Dec 1;66(23):11100-5.


Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.

Petrov KG, Zhang YM, Carter M, Cockerill GS, Dickerson S, Gauthier CA, Guo Y, Mook RA Jr, Rusnak DW, Walker AL, Wood ER, Lackey KE.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4686-91. Epub 2006 Jun 13.


Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.

Waterson AG, Stevens KL, Reno MJ, Zhang YM, Boros EE, Bouvier F, Rastagar A, Uehling DE, Dickerson SH, Reep B, McDonald OB, Wood ER, Rusnak DW, Alligood KJ, Rudolph SK.

Bioorg Med Chem Lett. 2006 May 1;16(9):2419-22. Epub 2006 Feb 17.


Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells.

Konecny GE, Pegram MD, Venkatesan N, Finn R, Yang G, Rahmeh M, Untch M, Rusnak DW, Spehar G, Mullin RJ, Keith BR, Gilmer TM, Berger M, Podratz KC, Slamon DJ.

Cancer Res. 2006 Feb 1;66(3):1630-9.


Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM, Johnson JH, Frick L, Lin MH, Depee S, Tadepalli S, Votta B, James I, Fuller K, Chambers TJ, Kull FC, Chamberlain SD, Hutchins JT.

Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83. Epub 2005 Oct 25.


A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells.

Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, Alligood KJ, Rusnak DW, Gilmer TM, Shewchuk L.

Cancer Res. 2004 Sep 15;64(18):6652-9.


A simple method for predicting serum protein binding of compounds from IC(50) shift analysis for in vitro assays.

Rusnak DW, Lai Z, Lansing TJ, Rhodes N, Gilmer TM, Copeland RA.

Bioorg Med Chem Lett. 2004 May 3;14(9):2309-12.


Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.

Gaul MD, Guo Y, Affleck K, Cockerill GS, Gilmer TM, Griffin RJ, Guntrip S, Keith BR, Knight WB, Mullin RJ, Murray DM, Rusnak DW, Smith K, Tadepalli S, Wood ER, Lackey K.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):637-40.


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.

Rusnak DW, Lackey K, Affleck K, Wood ER, Alligood KJ, Rhodes N, Keith BR, Murray DM, Knight WB, Mullin RJ, Gilmer TM.

Mol Cancer Ther. 2001 Dec;1(2):85-94.


Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways.

Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL.

Oncogene. 2002 Sep 12;21(41):6255-63.


The characterization of novel, dual ErbB-2/EGFR, tyrosine kinase inhibitors: potential therapy for cancer.

Rusnak DW, Affleck K, Cockerill SG, Stubberfield C, Harris R, Page M, Smith KJ, Guntrip SB, Carter MC, Shaw RJ, Jowett A, Stables J, Topley P, Wood ER, Brignola PS, Kadwell SH, Reep BR, Mullin RJ, Alligood KJ, Keith BR, Crosby RM, Murray DM, Knight WB, Gilmer TM, Lackey K.

Cancer Res. 2001 Oct 1;61(19):7196-203.


The formation of a covalent complex between a dipeptide ligand and the src SH2 domain.

Alligood KJ, Charifson PS, Crosby R, Consler TG, Feldman PL, Gampe RT Jr, Gilmer TM, Jordan SR, Milstead MW, Mohr C, Peel MR, Rocque W, Rodriguez M, Rusnak DW, Shewchuk LM, Sternbach DD.

Bioorg Med Chem Lett. 1998 May 19;8(10):1189-94.


The production and characterization of murine monoclonal antibodies to human Gadd45 raised against a recombinant protein.

Kilpatrick KE, Carrier F, Smith ML, Chen CY, Lee AJ, Rusnak DW, Kastan MB, Fornace AJ Jr, Champion BR, Gilmer TM, et al.

Hybridoma. 1995 Aug;14(4):355-9.


Alterations in the localization of F-actin, fibronectin, and thrombospondin occur prior to neoplastic transformation in rat tracheal epithelial cells.

Carter CA, Doherty MM, Rusnak DW, Nettesheim P, Ferriola PC.

Exp Cell Res. 1994 May;212(1):141-50. Erratum in: Exp Cell Res 1994 Sep;214(1):437-8.


Epidermal growth factor dependence and TGF alpha autocrine growth regulation in primary rat tracheal epithelial cells.

Ferriola PC, Robertson AT, Rusnak DW, Diaugustine R, Nettesheim P.

J Cell Physiol. 1992 Aug;152(2):302-9.


Altered growth factor dependence and transforming growth factor gene expression in transformed rat tracheal epithelial cells.

Ferriola PC, Walker C, Robertson AT, Earp HS, Rusnak DW, Nettesheim P.

Mol Carcinog. 1989;2(6):336-44.


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