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Items: 38

1.

RG7386, a Novel Tetravalent FAP-DR5 Antibody, Effectively Triggers FAP-Dependent, Avidity-Driven DR5 Hyperclustering and Tumor Cell Apoptosis.

Brünker P, Wartha K, Friess T, Grau-Richards S, Waldhauer I, Koller CF, Weiser B, Majety M, Runza V, Niu H, Packman K, Feng N, Daouti S, Hosse RJ, Mössner E, Weber TG, Herting F, Scheuer W, Sade H, Shao C, Liu B, Wang P, Xu G, Vega-Harring S, Klein C, Bosslet K, Umaña P.

Mol Cancer Ther. 2016 May;15(5):946-57. doi: 10.1158/1535-7163.MCT-15-0647. Epub 2016 Apr 1.

2.

Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy.

Zhang Z, Ding Q, Liu JJ, Zhang J, Jiang N, Chu XJ, Bartkovitz D, Luk KC, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.

Bioorg Med Chem. 2014 Aug 1;22(15):4001-9. doi: 10.1016/j.bmc.2014.05.072. Epub 2014 Jun 11.

PMID:
24997575
3.

Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.

Zhang Z, Chu XJ, Liu JJ, Ding Q, Zhang J, Bartkovitz D, Jiang N, Karnachi P, So SS, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev L, Graves B.

ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. doi: 10.1021/ml400359z. eCollection 2014 Feb 13.

4.

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.

Vu B, Wovkulich P, Pizzolato G, Lovey A, Ding Q, Jiang N, Liu JJ, Zhao C, Glenn K, Wen Y, Tovar C, Packman K, Vassilev L, Graves B.

ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. doi: 10.1021/ml4000657. eCollection 2013 May 9.

5.

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.

6.

Discovery of siRNA lipid nanoparticles to transfect suspension leukemia cells and provide in vivo delivery capability.

He W, Bennett MJ, Luistro L, Carvajal D, Nevins T, Smith M, Tyagi G, Cai J, Wei X, Lin TA, Heimbrook DC, Packman K, Boylan JF.

Mol Ther. 2014 Feb;22(2):359-370. doi: 10.1038/mt.2013.210. Epub 2013 Sep 3.

7.

RG7212 anti-TWEAK mAb inhibits tumor growth through inhibition of tumor cell proliferation and survival signaling and by enhancing the host antitumor immune response.

Yin X, Luistro L, Zhong H, Smith M, Nevins T, Schostack K, Hilton H, Lin TA, Truitt T, Biondi D, Wang X, Packman K, Rosinski J, Berkofsky-Fessler W, Tang JP, Pant S, Geho D, Vega-Harring S, Demario M, Levitsky H, Simcox M.

Clin Cancer Res. 2013 Oct 15;19(20):5686-98. doi: 10.1158/1078-0432.CCR-13-0405. Epub 2013 Aug 23.

8.

Stapled α-helical peptide drug development: a potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy.

Chang YS, Graves B, Guerlavais V, Tovar C, Packman K, To KH, Olson KA, Kesavan K, Gangurde P, Mukherjee A, Baker T, Darlak K, Elkin C, Filipovic Z, Qureshi FZ, Cai H, Berry P, Feyfant E, Shi XE, Horstick J, Annis DA, Manning AM, Fotouhi N, Nash H, Vassilev LT, Sawyer TK.

Proc Natl Acad Sci U S A. 2013 Sep 3;110(36):E3445-54. doi: 10.1073/pnas.1303002110. Epub 2013 Aug 14.

9.

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.

Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B.

J Med Chem. 2013 Jul 25;56(14):5979-83. doi: 10.1021/jm400487c. Epub 2013 Jul 16.

PMID:
23808545
10.

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.

11.

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.

12.

BRAFV600E negatively regulates the AKT pathway in melanoma cell lines.

Chen B, Tardell C, Higgins B, Packman K, Boylan JF, Niu H.

PLoS One. 2012;7(8):e42598. doi: 10.1371/journal.pone.0042598. Epub 2012 Aug 3.

13.

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.

14.

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.

15.

Allosteric antibody inhibition of human hepsin protease.

Koschubs T, Dengl S, Dürr H, Kaluza K, Georges G, Hartl C, Jennewein S, Lanzendörfer M, Auer J, Stern A, Huang KS, Packman K, Gubler U, Kostrewa D, Ries S, Hansen S, Kohnert U, Cramer P, Mundigl O.

Biochem J. 2012 Mar 15;442(3):483-94. doi: 10.1042/BJ20111317.

PMID:
22132769
16.

Identification of the MEK1(F129L) activating mutation as a potential mechanism of acquired resistance to MEK inhibition in human cancers carrying the B-RafV600E mutation.

Wang H, Daouti S, Li WH, Wen Y, Rizzo C, Higgins B, Packman K, Rosen N, Boylan JF, Heimbrook D, Niu H.

Cancer Res. 2011 Aug 15;71(16):5535-45. doi: 10.1158/0008-5472.CAN-10-4351. Epub 2011 Jun 24.

17.

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
18.

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.

19.

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.

20.

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.

21.

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.

22.

Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties.

Luistro L, He W, Smith M, Packman K, Vilenchik M, Carvajal D, Roberts J, Cai J, Berkofsky-Fessler W, Hilton H, Linn M, Flohr A, Jakob-Røtne R, Jacobsen H, Glenn K, Heimbrook D, Boylan JF.

Cancer Res. 2009 Oct 1;69(19):7672-80. doi: 10.1158/0008-5472.CAN-09-1843. Epub 2009 Sep 22. Erratum in: Cancer Res. 2012 Apr 15;72(8):2151.

23.

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.

24.

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.

25.

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.

26.

Mesenchymal stem cells in early entry of breast cancer into bone marrow.

Corcoran KE, Trzaska KA, Fernandes H, Bryan M, Taborga M, Srinivas V, Packman K, Patel PS, Rameshwar P.

PLoS One. 2008 Jun 25;3(6):e2563. doi: 10.1371/journal.pone.0002563.

27.

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.

28.

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.

29.

Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.

Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N.

J Med Chem. 2006 Nov 2;49(22):6549-60.

PMID:
17064073
30.

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.

31.

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.

32.
33.

Antiandrogen-induced cell death in LNCaP human prostate cancer cells.

Lee EC, Zhan P, Schallhom R, Packman K, Tenniswood M.

Cell Death Differ. 2003 Jul;10(7):761-71.

34.

Efficacy of Vitamin D compounds to modulate estrogen receptor negative breast cancer growth and invasion.

Flanagan L, Packman K, Juba B, O'Neill S, Tenniswood M, Welsh J.

J Steroid Biochem Mol Biol. 2003 Feb;84(2-3):181-92.

PMID:
12711002
35.

Induction of invasive phenotype by Casodex in hormone-sensitive prostate cancer cells.

Zhan P, Lee EC, Packman K, Tenniswood M.

J Steroid Biochem Mol Biol. 2002 Dec;83(1-5):101-11.

PMID:
12650706
36.

Vitamin D(3) receptor ablation alters mammary gland morphogenesis.

Zinser G, Packman K, Welsh J.

Development. 2002 Jul;129(13):3067-76.

37.

Increased plasminogen activator and type IV collagenase activity in invasive follicular thyroid carcinoma cells.

Packman KS, Demeure MJ, Doffek KM, Wilson SD.

Surgery. 1995 Dec;118(6):1011-6; discussion 1016-7.

PMID:
7491516
38.

Indications for parathyroidectomy and extent of treatment for patients with secondary hyperparathyroidism.

Packman KS, Demeure MJ.

Surg Clin North Am. 1995 Jun;75(3):465-82. Review.

PMID:
7747253

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