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Items: 26

1.

Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach.

Higgins B, Glenn K, Walz A, Tovar C, Filipovic Z, Hussain S, Lee E, Kolinsky K, Tannu S, Adames V, Garrido R, Linn M, Meille C, Heimbrook D, Vassilev L, Packman K.

Clin Cancer Res. 2014 Jul 15;20(14):3742-52. doi: 10.1158/1078-0432.CCR-14-0460. Epub 2014 May 8.

2.

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.

Liu JJ, Higgins B, Ju G, Kolinsky K, Luk KC, Packman K, Pizzolato G, Ren Y, Thakkar K, Tovar C, Zhang Z, Wovkulich PM.

ACS Med Chem Lett. 2013 Jan 15;4(2):259-63. doi: 10.1021/ml300351e. eCollection 2013 Feb 14.

3.

MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models.

Tovar C, Graves B, Packman K, Filipovic Z, Higgins B, Xia M, Tardell C, Garrido R, Lee E, Kolinsky K, To KH, Linn M, Podlaski F, Wovkulich P, Vu B, Vassilev LT.

Cancer Res. 2013 Apr 15;73(8):2587-97. doi: 10.1158/0008-5472.CAN-12-2807. Epub 2013 Feb 11.

4.

Resistance to selective BRAF inhibition can be mediated by modest upstream pathway activation.

Su F, Bradley WD, Wang Q, Yang H, Xu L, Higgins B, Kolinsky K, Packman K, Kim MJ, Trunzer K, Lee RJ, Schostack K, Carter J, Albert T, Germer S, Rosinski J, Martin M, Simcox ME, Lestini B, Heimbrook D, Bollag G.

Cancer Res. 2012 Feb 15;72(4):969-78. doi: 10.1158/0008-5472.CAN-11-1875. Epub 2011 Dec 28.

5.

Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer.

Yang H, Higgins B, Kolinsky K, Packman K, Bradley WD, Lee RJ, Schostack K, Simcox ME, Kopetz S, Heimbrook D, Lestini B, Bollag G, Su F.

Cancer Res. 2012 Feb 1;72(3):779-89. doi: 10.1158/0008-5472.CAN-11-2941. Epub 2011 Dec 16.

6.

Preclinical evaluation of the novel multi-targeted agent R1530.

Kolinsky K, Tovar C, Zhang YE, Railkar A, Yang H, Carvajal D, Nevins T, Geng W, Linn M, Packman K, Liu JJ, Zhang Z, Wovkulich P, Ju G, Higgins B.

Cancer Chemother Pharmacol. 2011 Dec;68(6):1585-94. doi: 10.1007/s00280-011-1608-x. Epub 2011 May 8.

PMID:
21553286
7.

MDM2 antagonists boost antitumor effect of androgen withdrawal: implications for therapy of prostate cancer.

Tovar C, Higgins B, Kolinsky K, Xia M, Packman K, Heimbrook DC, Vassilev LT.

Mol Cancer. 2011 May 3;10:49. doi: 10.1186/1476-4598-10-49.

8.

High tumor levels of IL6 and IL8 abrogate preclinical efficacy of the γ-secretase inhibitor, RO4929097.

He W, Luistro L, Carvajal D, Smith M, Nevins T, Yin X, Cai J, Higgins B, Kolinsky K, Rizzo C, Packman K, Heimbrook D, Boylan JF.

Mol Oncol. 2011 Jun;5(3):292-301. doi: 10.1016/j.molonc.2011.01.001. Epub 2011 Jan 21.

9.

Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. doi: 10.1016/j.bmcl.2010.08.079. Epub 2010 Aug 21.

PMID:
20832307
10.

Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.

Tovar C, Higgins B, Deo D, Kolinsky K, Liu JJ, Heimbrook DC, Vassilev LT.

Cell Cycle. 2010 Aug 15;9(16):3364-75. doi: 10.4161/cc.9.16.12732. Epub 2010 Aug 21.

PMID:
20814247
11.

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models.

Yang H, Higgins B, Kolinsky K, Packman K, Go Z, Iyer R, Kolis S, Zhao S, Lee R, Grippo JF, Schostack K, Simcox ME, Heimbrook D, Bollag G, Su F.

Cancer Res. 2010 Jul 1;70(13):5518-27. doi: 10.1158/0008-5472.CAN-10-0646. Epub 2010 Jun 15. Erratum in: Cancer Res. 2010 Nov 15;70(22):9527.

12.

Optimizing chemotherapy dose and schedule by Norton-Simon mathematical modeling.

Traina TA, Dugan U, Higgins B, Kolinsky K, Theodoulou M, Hudis CA, Norton L.

Breast Dis. 2010;31(1):7-18. doi: 10.3233/BD-2009-0290.

13.

Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.

Daouti S, Higgins B, Kolinsky K, Packman K, Wang H, Rizzo C, Moliterni J, Huby N, Fotouhi N, Liu M, Goelzer P, Sandhu HK, Li JK, Railkar A, Heimbrook D, Niu H.

Mol Cancer Ther. 2010 Jan;9(1):134-44. doi: 10.1158/1535-7163.MCT-09-0601. Epub 2010 Jan 6.

14.

Novel regimens of capecitabine alone and combined with irinotecan and bevacizumab in colorectal cancer xenografts.

Kolinsky K, Zhang YE, Dugan U, Heimbrook D, Packman K, Higgins B.

Anticancer Res. 2009 Jan;29(1):91-8.

15.

Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy.

Daouti S, Wang H, Li WH, Higgins B, Kolinsky K, Packman K, Specian A Jr, Kong N, Huby N, Wen Y, Xiang Q, Podlaski FJ, He Y, Fotouhi N, Heimbrook D, Niu H.

Cancer Res. 2009 Mar 1;69(5):1924-32. doi: 10.1158/0008-5472.CAN-08-2627. Epub 2009 Feb 24.

16.

In vivo activity of novel capecitabine regimens alone and with bevacizumab and oxaliplatin in colorectal cancer xenograft models.

Kolinsky K, Shen BQ, Zhang YE, Kohles J, Dugan U, Zioncheck TF, Heimbrook D, Packman K, Higgins B.

Mol Cancer Ther. 2009 Jan;8(1):75-82. doi: 10.1158/1535-7163.MCT-08-0596.

17.

Antitumor activity of capecitabine and bevacizumab combination in a human estrogen receptor-negative breast adenocarcinoma xenograft model.

Higgins B, Kolinsky K, Linn M, Adames V, Zhang YE, Moisa C, Dugan U, Heimbrook D, Packman K.

Anticancer Res. 2007 Jul-Aug;27(4B):2279-87.

18.

In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.

DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D.

Mol Cancer Ther. 2006 Nov;5(11):2644-58.

19.

Antitumor activity of HER1/EGFR tyrosine kinase inhibitor erlotinib, alone and in combination with CPT-11 (irinotecan) in human colorectal cancer xenograft models.

Chen J, Smith M, Kolinsky K, Adames V, Mehta N, Fritzky L, Rashed M, Wheeldon E, Linn M, Higgins B.

Cancer Chemother Pharmacol. 2007 Apr;59(5):651-9. Epub 2006 Aug 26.

PMID:
16937104
20.

Preclinical evaluation of tumor microvascular response to a novel antiangiogenic/antitumor agent RO0281501 by dynamic contrast-enhanced MRI at 1.5 T.

Muruganandham M, Lupu M, Dyke JP, Matei C, Linn M, Packman K, Kolinsky K, Higgins B, Koutcher JA.

Mol Cancer Ther. 2006 Aug;5(8):1950-7.

21.

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

McDermott LA, Higgins B, Simcox M, Luk KC, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Liu JJ, Konzelmann F, Zhang Z, Flynn T, Morales O, Chen Y.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.

PMID:
16460940
22.

Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.

Tovar C, Rosinski J, Filipovic Z, Higgins B, Kolinsky K, Hilton H, Zhao X, Vu BT, Qing W, Packman K, Myklebost O, Heimbrook DC, Vassilev LT.

Proc Natl Acad Sci U S A. 2006 Feb 7;103(6):1888-93. Epub 2006 Jan 27.

23.

RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.

McDermott LA, Simcox M, Higgins B, Nevins T, Kolinsky K, Smith M, Yang H, Li JK, Chen Y, Ke J, Mallalieu N, Egan T, Kolis S, Railkar A, Gerber L, Luk KC.

Bioorg Med Chem. 2005 Aug 15;13(16):4835-41.

PMID:
15953730
24.

Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models.

Higgins B, Kolinsky K, Smith M, Beck G, Rashed M, Adames V, Linn M, Wheeldon E, Gand L, Birnboeck H, Hoffmann G.

Anticancer Drugs. 2004 Jun;15(5):503-12.

PMID:
15166626
25.

Interleukin-12 antagonist activity of mouse interleukin-12 p40 homodimer in vitro and in vivo.

Gately MK, Carvajal DM, Connaughton SE, Gillessen S, Warrier RR, Kolinsky KD, Wilkinson VL, Dwyer CM, Higgins GF Jr, Podlaski FJ, Faherty DA, Familletti PC, Stern AS, Presky DH.

Ann N Y Acad Sci. 1996 Oct 31;795:1-12.

PMID:
8958912
26.

Inhibition of interleukin 1 (IL-1) binding and bioactivity in vitro and modulation of acute inflammation in vivo by IL-1 receptor antagonist and anti-IL-1 receptor monoclonal antibody.

McIntyre KW, Stepan GJ, Kolinsky KD, Benjamin WR, Plocinski JM, Kaffka KL, Campen CA, Chizzonite RA, Kilian PL.

J Exp Med. 1991 Apr 1;173(4):931-9.

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