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147 results

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Page 1
Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity.
Wilson WH, O'Connor OA, Czuczman MS, LaCasce AS, Gerecitano JF, Leonard JP, Tulpule A, Dunleavy K, Xiong H, Chiu YL, Cui Y, Busman T, Elmore SW, Rosenberg SH, Krivoshik AP, Enschede SH, Humerickhouse RA. Wilson WH, et al. Among authors: rosenberg sh. Lancet Oncol. 2010 Dec;11(12):1149-59. doi: 10.1016/S1470-2045(10)70261-8. Epub 2010 Nov 18. Lancet Oncol. 2010. PMID: 21094089 Free PMC article. Clinical Trial.
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW. Souers AJ, et al. Among authors: rosenberg sh. Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6. Nat Med. 2013. PMID: 23291630
The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo.
Chen J, Jin S, Abraham V, Huang X, Liu B, Mitten MJ, Nimmer P, Lin X, Smith M, Shen Y, Shoemaker AR, Tahir SK, Zhang H, Ackler SL, Rosenberg SH, Maecker H, Sampath D, Leverson JD, Tse C, Elmore SW. Chen J, et al. Among authors: rosenberg sh. Mol Cancer Ther. 2011 Dec;10(12):2340-9. doi: 10.1158/1535-7163.MCT-11-0415. Epub 2011 Sep 13. Mol Cancer Ther. 2011. PMID: 21914853
Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models.
Shoemaker AR, Mitten MJ, Adickes J, Ackler S, Refici M, Ferguson D, Oleksijew A, O'Connor JM, Wang B, Frost DJ, Bauch J, Marsh K, Tahir SK, Yang X, Tse C, Fesik SW, Rosenberg SH, Elmore SW. Shoemaker AR, et al. Among authors: rosenberg sh. Clin Cancer Res. 2008 Jun 1;14(11):3268-77. doi: 10.1158/1078-0432.CCR-07-4622. Clin Cancer Res. 2008. PMID: 18519752
ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.
Tse C, Shoemaker AR, Adickes J, Anderson MG, Chen J, Jin S, Johnson EF, Marsh KC, Mitten MJ, Nimmer P, Roberts L, Tahir SK, Xiao Y, Yang X, Zhang H, Fesik S, Rosenberg SH, Elmore SW. Tse C, et al. Among authors: rosenberg sh. Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836. Cancer Res. 2008. PMID: 18451170
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW. Bruncko M, et al. Among authors: rosenberg sh. J Med Chem. 2007 Feb 22;50(4):641-62. doi: 10.1021/jm061152t. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256834
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Petros AM, Huth JR, Oost T, Park CM, Ding H, Wang X, Zhang H, Nimmer P, Mendoza R, Sun C, Mack J, Walter K, Dorwin S, Gramling E, Ladror U, Rosenberg SH, Elmore SW, Fesik SW, Hajduk PJ. Petros AM, et al. Among authors: rosenberg sh. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6587-91. doi: 10.1016/j.bmcl.2010.09.033. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20870405
Bcl-2 family proteins are essential for platelet survival.
Zhang H, Nimmer PM, Tahir SK, Chen J, Fryer RM, Hahn KR, Iciek LA, Morgan SJ, Nasarre MC, Nelson R, Preusser LC, Reinhart GA, Smith ML, Rosenberg SH, Elmore SW, Tse C. Zhang H, et al. Among authors: rosenberg sh. Cell Death Differ. 2007 May;14(5):943-51. doi: 10.1038/sj.cdd.4402081. Epub 2007 Jan 5. Cell Death Differ. 2007. PMID: 17205078
A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo.
Shoemaker AR, Oleksijew A, Bauch J, Belli BA, Borre T, Bruncko M, Deckwirth T, Frost DJ, Jarvis K, Joseph MK, Marsh K, McClellan W, Nellans H, Ng S, Nimmer P, O'Connor JM, Oltersdorf T, Qing W, Shen W, Stavropoulos J, Tahir SK, Wang B, Warner R, Zhang H, Fesik SW, Rosenberg SH, Elmore SW. Shoemaker AR, et al. Among authors: rosenberg sh. Cancer Res. 2006 Sep 1;66(17):8731-9. doi: 10.1158/0008-5472.CAN-06-0367. Cancer Res. 2006. PMID: 16951189
147 results