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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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


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.


Elevated MDM2 boosts the apoptotic activity of p53-MDM2 binding inhibitors by facilitating MDMX degradation.

Xia M, Knezevic D, Tovar C, Huang B, Heimbrook DC, Vassilev LT.

Cell Cycle. 2008 Jun 1;7(11):1604-12. Epub 2008 Mar 17.


A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage.

Daouti S, Li WH, Qian H, Huang KS, Holmgren J, Levin W, Reik L, McGady DL, Gillespie P, Perrotta A, Bian H, Reidhaar-Olson JF, Bliss SA, Olivier AR, Sergi JA, Fry D, Danho W, Ritland S, Fotouhi N, Heimbrook D, Niu H.

Cancer Res. 2008 Feb 15;68(4):1162-9. doi: 10.1158/0008-5472.CAN-07-2349.


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.


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.


Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.

Vassilev LT, Tovar C, Chen S, Knezevic D, Zhao X, Sun H, Heimbrook DC, Chen L.

Proc Natl Acad Sci U S A. 2006 Jul 11;103(28):10660-5. Epub 2006 Jul 3.


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.


Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.

Fraley ME, Garbaccio RM, Arrington KL, Hoffman WF, Tasber ES, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Fernandes C, Schaber MD, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Shu C, Torrent M, Heimbrook DC, Kohl NE, Huber HE, Hartman GD.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1775-9. Epub 2006 Jan 24.


Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.

Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1780-3. Epub 2006 Jan 24.


Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.

Bell IM, Stirdivant SM, Ahern J, Culberson JC, Darke PL, Dinsmore CJ, Drakas RA, Gallicchio SN, Graham SL, Heimbrook DC, Hall DL, Hua J, Kett NR, Kim AS, Kornienko M, Kuo LC, Munshi SK, Quigley AG, Reid JC, Trotter BW, Waxman LH, Williams TM, Zartman CB.

Biochemistry. 2005 Jul 12;44(27):9430-40.


Activation of p53 by MDM2 antagonists can protect proliferating cells from mitotic inhibitors.

Carvajal D, Tovar C, Yang H, Vu BT, Heimbrook DC, Vassilev LT.

Cancer Res. 2005 Mar 1;65(5):1918-24.


Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.

Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD.

J Med Chem. 2004 Dec 2;47(25):6363-72.


Phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis.

Thompson T, Tovar C, Yang H, Carvajal D, Vu BT, Xu Q, Wahl GM, Heimbrook DC, Vassilev LT.

J Biol Chem. 2004 Dec 17;279(51):53015-22. Epub 2004 Oct 6.


A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo.

Sepp-Lorenzino L, Rands E, Mao X, Connolly B, Shipman J, Antanavage J, Hill S, Davis L, Beck S, Rickert K, Coll K, Ciecko P, Fraley M, Hoffman W, Hartman G, Heimbrook D, Gibbs J, Kohl N, Thomas K.

Cancer Res. 2004 Jan 15;64(2):751-6.


3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB.

J Med Chem. 2002 Jun 6;45(12):2388-409.


Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.

Lobell RB, Omer CA, Abrams MT, Bhimnathwala HG, Brucker MJ, Buser CA, Davide JP, deSolms SJ, Dinsmore CJ, Ellis-Hutchings MS, Kral AM, Liu D, Lumma WC, Machotka SV, Rands E, Williams TM, Graham SL, Hartman GD, Oliff AI, Heimbrook DC, Kohl NE.

Cancer Res. 2001 Dec 15;61(24):8758-68.


Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.

Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM.

J Med Chem. 2001 Aug 30;44(18):2933-49.


Anions modulate the potency of geranylgeranyl-protein transferase I inhibitors.

Huber HE, Robinson RG, Watkins A, Nahas DD, Abrams MT, Buser CA, Lobell RB, Patrick D, Anthony NJ, Dinsmore CJ, Graham SL, Hartman GD, Lumma WC, Williams TM, Heimbrook DC.

J Biol Chem. 2001 Jul 6;276(27):24457-65. Epub 2001 Mar 26.


Therapeutic intervention and signaling.

Heimbrook DC, Oliff A.

Curr Opin Cell Biol. 1998 Apr;10(2):284-8. Review.


Oncogene products as therapeutic targets for cancer.

Huang PS, Heimbrook DC.

Curr Opin Oncol. 1997 Jan;9(1):94-100. Review.


Cloning and mutagenesis of the p110 alpha subunit of human phosphoinositide 3'-hydroxykinase.

Stirdivant SM, Ahern J, Conroy RR, Barnett SF, Ledder LM, Oliff A, Heimbrook DC.

Bioorg Med Chem. 1997 Jan;5(1):65-74.


Interfacial catalysis by phosphoinositide 3'-hydroxykinase.

Barnett SF, Ledder LM, Stirdivant SM, Ahern J, Conroy RR, Heimbrook DC.

Biochemistry. 1995 Oct 31;34(43):14254-62.


An SH3 domain is required for the mitogenic activity of microinjected phospholipase C-gamma 1.

Huang PS, Davis L, Huber H, Goodhart PJ, Wegrzyn RE, Oliff A, Heimbrook DC.

FEBS Lett. 1995 Jan 30;358(3):287-92.


Phase I clinical study of the recombinant oncotoxin TP40 in superficial bladder cancer.

Goldberg MR, Heimbrook DC, Russo P, Sarosdy MF, Greenberg RE, Giantonio BJ, Linehan WM, Walther M, Fisher HA, Messing E, et al.

Clin Cancer Res. 1995 Jan;1(1):57-61.


Cloning and characterization of E2F-2, a novel protein with the biochemical properties of transcription factor E2F.

Ivey-Hoyle M, Conroy R, Huber HE, Goodhart PJ, Oliff A, Heimbrook DC.

Mol Cell Biol. 1993 Dec;13(12):7802-12.


Transcription factor E2F binds DNA as a heterodimer.

Huber HE, Edwards G, Goodhart PJ, Patrick DR, Huang PS, Ivey-Hoyle M, Barnett SF, Oliff A, Heimbrook DC.

Proc Natl Acad Sci U S A. 1993 Apr 15;90(8):3525-9.


Protein domains governing interactions between E2F, the retinoblastoma gene product, and human papillomavirus type 16 E7 protein.

Huang PS, Patrick DR, Edwards G, Goodhart PJ, Huber HE, Miles L, Garsky VM, Oliff A, Heimbrook DC.

Mol Cell Biol. 1993 Feb;13(2):953-60.


Retinoblastoma protein binding properties are dependent on 4 cysteine residues in the protein binding pocket.

Stirdivant SM, Ahern JD, Oliff A, Heimbrook DC.

J Biol Chem. 1992 Jul 25;267(21):14846-51.


Human papillomavirus type 16 E7 protein inhibits DNA binding by the retinoblastoma gene product.

Stirdivant SM, Huber HE, Patrick DR, Defeo-Jones D, McAvoy EM, Garsky VM, Oliff A, Heimbrook DC.

Mol Cell Biol. 1992 May;12(5):1905-14.


Purification and characterization of a functionally homogeneous 60-kDa species of the retinoblastoma gene product.

Edwards GM, Huber HE, DeFeo-Jones D, Vuocolo G, Goodhart PJ, Maigetter RZ, Sanyal G, Oliff A, Heimbrook DC.

J Biol Chem. 1992 Apr 25;267(12):7971-4. Erratum in: J Biol Chem 1992 Jul 5;267(19):13780.


Characterization of functional HPV-16 E7 protein produced in Escherichia coli.

Patrick DR, Zhang K, Defeo-Jones D, Vuocolo GR, Maigetter RZ, Sardana MK, Oliff A, Heimbrook DC.

J Biol Chem. 1992 Apr 5;267(10):6910-5.


Activity of a recombinant transforming growth factor-alpha-Pseudomonas exotoxin hybrid protein against primary human tumor colony-forming units.

Von Hoff DD, Marshall MH, Heimbrook DC, Stirdivant SM, Ahern JD, Herbert WK, Maigetter RZ, Oliff A.

Invest New Drugs. 1992 Apr;10(1):17-22.


Specific N-methylations of HPV-16 E7 peptides alter binding to the retinoblastoma suppressor protein.

Jones RE, Heimbrook DC, Huber HE, Wegrzyn RJ, Rotberg NS, Stauffer KJ, Lumma PK, Garsky VM, Oliff A.

J Biol Chem. 1992 Jan 15;267(2):908-12.


Expression of growth factor-toxin fusion proteins.

Edwards GM, Defeo-Jones D, Stirdivant SM, Heimbrook DC, Oliff A.

Targeted Diagn Ther. 1992;7:425-37. Review. No abstract available.


Gastrin releasing peptide antagonists with improved potency and stability.

Heimbrook DC, Saari WS, Balishin NL, Fisher TW, Friedman A, Kiefer DM, Rotberg NS, Wallen JW, Oliff A.

J Med Chem. 1991 Jul;34(7):2102-7.


Biological activity of a transforming growth factor-alpha--Pseudomonas exotoxin fusion protein in vitro and in vivo.

Heimbrook DC, Stirdivant SM, Ahern JD, Balishin NL, Patrick DR, Edwards GM, Defeo-Jones D, FitzGerald DJ, Pastan I, Oliff A.

J Ind Microbiol. 1991 Apr;7(3):203-7.


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