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Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.

Bogen SL, Pan W, Gibeau CR, Lahue BR, Ma Y, Nair LG, Seigel E, Shipps GW Jr, Tian Y, Wang Y, Lin Y, Liu M, Liu S, Mirza A, Wang X, Lipari P, Seidel-Dugan C, Hicklin DJ, Bishop WR, Rindgen D, Nomeir A, Prosise W, Reichert P, Scapin G, Strickland C, Doll RJ.

ACS Med Chem Lett. 2016 Jan 20;7(3):324-9. doi: 10.1021/acsmedchemlett.5b00472. eCollection 2016 Mar 10.


Antiangiogenic therapy--evolving view based on clinical trial results.

Jayson GC, Hicklin DJ, Ellis LM.

Nat Rev Clin Oncol. 2012 Feb 14;9(5):297-303. doi: 10.1038/nrclinonc.2012.8. Review.


SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors.

Basso AD, Liu M, Gray K, Tevar S, Lee S, Liang L, Ponery A, Smith EB, Monsma FJ Jr, Yu T, Zhang Y, Kerekes AD, Esposite S, Xiao Y, Tagat JR, Hicklin DJ, Kirschmeier P.

Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. doi: 10.1007/s00280-011-1568-1. Epub 2011 Feb 5.


SCH 2047069, a novel oral kinesin spindle protein inhibitor, shows single-agent antitumor activity and enhances the efficacy of chemotherapeutics.

Basso AD, Liu M, Dai C, Gray K, Nale L, Tevar S, Lee S, Liang L, Ponery A, Yaremko B, Smith E, Tang H, Sheth PR, Siddiqui MA, Hicklin DJ, Kirschmeier P.

Mol Cancer Ther. 2010 Nov;9(11):2993-3002. doi: 10.1158/1535-7163.MCT-10-0548. Epub 2010 Oct 26.


Resistance to Targeted Therapies: Refining Anticancer Therapy in the Era of Molecular Oncology.

Ellis LM, Hicklin DJ.

Clin Cancer Res. 2009 Dec 15;15(24):7471-7478.


Prioritization of EGFR/IGF-IR/VEGFR2 combination targeted therapies utilizing cancer models.

Tonra JR, Corcoran E, Deevi DS, Steiner P, Kearney J, Li H, Ludwig DL, Zhu Z, Witte L, Surguladze D, Hicklin DJ.

Anticancer Res. 2009 Jun;29(6):1999-2007.


Vascular endothelial growth factor receptor 2 (VEGFR-2) functions to promote uterine decidual angiogenesis during early pregnancy in the mouse.

Douglas NC, Tang H, Gomez R, Pytowski B, Hicklin DJ, Sauer CM, Kitajewski J, Sauer MV, Zimmermann RC.

Endocrinology. 2009 Aug;150(8):3845-54. doi: 10.1210/en.2008-1207. Epub 2009 Apr 30.


In vivo method for establishing synergy between antibodies to epidermal growth factor receptor and vascular endothelial growth factor receptor-2.

Tonra JR, Prewett M, Corcoran E, Hicklin DJ, Zhu Z.

Methods Mol Biol. 2009;525:545-57, xv. doi: 10.1007/978-1-59745-554-1_30.


Anti-epidermal growth factor receptor monoclonal antibody cetuximab inhibits EGFR/HER-2 heterodimerization and activation.

Patel D, Bassi R, Hooper A, Prewett M, Hicklin DJ, Kang X.

Int J Oncol. 2009 Jan;34(1):25-32.


Enhanced suppression of melanoma tumor growth and metastasis by combined therapy with anti-VEGF receptor and anti-TYRP-1/gp75 monoclonal antibodies.

Patel D, Bassi R, Hooper AT, Sun H, Huber J, Hicklin DJ, Kang X.

Anticancer Res. 2008 Sep-Oct;28(5A):2679-86.


Pathways mediating resistance to vascular endothelial growth factor-targeted therapy.

Ellis LM, Hicklin DJ.

Clin Cancer Res. 2008 Oct 15;14(20):6371-5. doi: 10.1158/1078-0432.CCR-07-5287. Review.


VEGF-targeted therapy: mechanisms of anti-tumour activity.

Ellis LM, Hicklin DJ.

Nat Rev Cancer. 2008 Aug;8(8):579-91. doi: 10.1038/nrc2403. Epub 2008 Jul 3. Review.


Effect of molecular therapeutics on liver regeneration in a murine model.

Van Buren G 2nd, Yang AD, Dallas NA, Gray MJ, Lim SJ, Xia L, Fan F, Somcio R, Wu Y, Hicklin DJ, Ellis LM.

J Clin Oncol. 2008 Apr 10;26(11):1836-42. doi: 10.1200/JCO.2007.11.6566.


Cetuximab-induced anaphylaxis and IgE specific for galactose-alpha-1,3-galactose.

Chung CH, Mirakhur B, Chan E, Le QT, Berlin J, Morse M, Murphy BA, Satinover SM, Hosen J, Mauro D, Slebos RJ, Zhou Q, Gold D, Hatley T, Hicklin DJ, Platts-Mills TA.

N Engl J Med. 2008 Mar 13;358(11):1109-17. doi: 10.1056/NEJMoa074943.


Generation and characterization of a therapeutic human antibody to melanoma antigen TYRP1.

Patel D, Balderes P, Lahiji A, Melchior M, Ng S, Bassi R, Wu Y, Griffith H, Jimenez X, Ludwig DL, Hicklin DJ, Kang X.

Hum Antibodies. 2007;16(3-4):127-36.


HIF-1alpha regulates epithelial inflammation by cell autonomous NFkappaB activation and paracrine stromal remodeling.

Scortegagna M, Cataisson C, Martin RJ, Hicklin DJ, Schreiber RD, Yuspa SH, Arbeit JM.

Blood. 2008 Apr 1;111(7):3343-54. doi: 10.1182/blood-2007-10-115758. Epub 2008 Jan 16.


Tumors established with cell lines selected for oxaliplatin resistance respond to oxaliplatin if combined with cetuximab.

Prewett M, Deevi DS, Bassi R, Fan F, Ellis LM, Hicklin DJ, Tonra JR.

Clin Cancer Res. 2007 Dec 15;13(24):7432-40.


Monoclonal antibody cetuximab binds to and down-regulates constitutively activated epidermal growth factor receptor vIII on the cell surface.

Patel D, Lahiji A, Patel S, Franklin M, Jimenez X, Hicklin DJ, Kang X.

Anticancer Res. 2007 Sep-Oct;27(5A):3355-66.


Regulation of cyclooxygenase-2 (COX-2) expression in human pancreatic carcinoma cells by the insulin-like growth factor-I receptor (IGF-IR) system.

Stoeltzing O, Liu W, Fan F, Wagner C, Stengel K, Somcio RJ, Reinmuth N, Parikh AA, Hicklin DJ, Ellis LM.

Cancer Lett. 2007 Dec 18;258(2):291-300. Epub 2007 Oct 22.


Inhibitory activity of cetuximab on epidermal growth factor receptor mutations in non small cell lung cancers.

Doody JF, Wang Y, Patel SN, Joynes C, Lee SP, Gerlak J, Rolser RL, Li Y, Steiner P, Bassi R, Hicklin DJ, Hadari YR.

Mol Cancer Ther. 2007 Oct;6(10):2642-51. Epub 2007 Oct 3.


Review: monoclonal antibodies to the vascular endothelial growth factor receptor-2 in cancer therapy.

Youssoufian H, Hicklin DJ, Rowinsky EK.

Clin Cancer Res. 2007 Sep 15;13(18 Pt 2):5544s-5548s. Review.


Suppression of Ewing's sarcoma tumor growth, tumor vessel formation, and vasculogenesis following anti vascular endothelial growth factor receptor-2 therapy.

Zhou Z, Bolontrade MF, Reddy K, Duan X, Guan H, Yu L, Hicklin DJ, Kleinerman ES.

Clin Cancer Res. 2007 Aug 15;13(16):4867-73.


A vascular endothelial growth factor receptor-2 inhibitor enhances antitumor immunity through an immune-based mechanism.

Manning EA, Ullman JG, Leatherman JM, Asquith JM, Hansen TR, Armstrong TD, Hicklin DJ, Jaffee EM, Emens LA.

Clin Cancer Res. 2007 Jul 1;13(13):3951-9.


Detecting vascular changes in tumour xenografts using micro-ultrasound and micro-ct following treatment with VEGFR-2 blocking antibodies.

Cheung AM, Brown AS, Cucevic V, Roy M, Needles A, Yang V, Hicklin DJ, Kerbel RS, Foster FS.

Ultrasound Med Biol. 2007 Aug;33(8):1259-68. Epub 2007 Apr 30.


Promoting angiogenesis to a fault.

Hicklin DJ.

Nat Biotechnol. 2007 Mar;25(3):300-2. No abstract available.


Tumor growth inhibition with cetuximab and chemotherapy in non-small cell lung cancer xenografts expressing wild-type and mutated epidermal growth factor receptor.

Steiner P, Joynes C, Bassi R, Wang S, Tonra JR, Hadari YR, Hicklin DJ.

Clin Cancer Res. 2007 Mar 1;13(5):1540-51.


Tyrosine kinase receptor RON in human pancreatic cancer: expression, function, and validation as a target.

Camp ER, Yang A, Gray MJ, Fan F, Hamilton SR, Evans DB, Hooper AT, Pereira DS, Hicklin DJ, Ellis LM.

Cancer. 2007 Mar 15;109(6):1030-9.


Neonatal hypoxic preconditioning involves vascular endothelial growth factor.

Laudenbach V, Fontaine RH, Medja F, Carmeliet P, Hicklin DJ, Gallego J, Leroux P, Marret S, Gressens P.

Neurobiol Dis. 2007 Apr;26(1):243-52. Epub 2007 Jan 13.


VEGFR-1 and -2 regulate inflammation, myocardial angiogenesis, and arteriosclerosis in chronically rejecting cardiac allografts.

Raisky O, Nykänen AI, Krebs R, Hollmén M, Keränen MA, Tikkanen JM, Sihvola R, Alhonen L, Salven P, Wu Y, Hicklin DJ, Alitalo K, Koskinen PK, Lemström KB.

Arterioscler Thromb Vasc Biol. 2007 Apr;27(4):819-25. Epub 2007 Feb 8.


Insulin-like growth factor-I receptor signaling blockade combined with radiation.

Allen GW, Saba C, Armstrong EA, Huang SM, Benavente S, Ludwig DL, Hicklin DJ, Harari PM.

Cancer Res. 2007 Feb 1;67(3):1155-62.


Simultaneous blockade of VEGFR-1 and VEGFR-2 activation is necessary to efficiently inhibit experimental melanoma growth and metastasis formation.

Gille J, Heidenreich R, Pinter A, Schmitz J, Boehme B, Hicklin DJ, Henschler R, Breier G.

Int J Cancer. 2007 May 1;120(9):1899-908.


Cooperative and redundant roles of VEGFR-2 and VEGFR-3 signaling in adult lymphangiogenesis.

Goldman J, Rutkowski JM, Shields JD, Pasquier MC, Cui Y, Schmökel HG, Willey S, Hicklin DJ, Pytowski B, Swartz MA.

FASEB J. 2007 Apr;21(4):1003-12. Epub 2007 Jan 8. Erratum in: FASEB J. 2007 Jun;21(8):1942.


Targeting the vascular endothelial growth factor pathway in the treatment of human malignancy.

Tonra JR, Hicklin DJ.

Immunol Invest. 2007;36(1):3-23. Review.


Vascular endothelial growth factor plays a major role in development of experimental obliterative bronchiolitis.

Krebs R, Hollmén ME, Tikkanen JM, Wu Y, Hicklin DJ, Koskinen PK, Lemström KB.

Transplant Proc. 2006 Dec;38(10):3266-7.


Anti-vascular endothelial growth factor receptor-1 antagonist antibody as a therapeutic agent for cancer.

Wu Y, Zhong Z, Huber J, Bassi R, Finnerty B, Corcoran E, Li H, Navarro E, Balderes P, Jimenez X, Koo H, Mangalampalli VR, Ludwig DL, Tonra JR, Hicklin DJ.

Clin Cancer Res. 2006 Nov 1;12(21):6573-84.


Therapy-induced acute recruitment of circulating endothelial progenitor cells to tumors.

Shaked Y, Ciarrocchi A, Franco M, Lee CR, Man S, Cheung AM, Hicklin DJ, Chaplin D, Foster FS, Benezra R, Kerbel RS.

Science. 2006 Sep 22;313(5794):1785-7.


Therapeutic implications of a human neutralizing antibody to the macrophage-stimulating protein receptor tyrosine kinase (RON), a c-MET family member.

O'Toole JM, Rabenau KE, Burns K, Lu D, Mangalampalli V, Balderes P, Covino N, Bassi R, Prewett M, Gottfredsen KJ, Thobe MN, Cheng Y, Li Y, Hicklin DJ, Zhu Z, Waltz SE, Hayman MJ, Ludwig DL, Pereira DS.

Cancer Res. 2006 Sep 15;66(18):9162-70.


Vascular endothelial growth factor overexpression by soft tissue sarcoma cells: implications for tumor growth, metastasis, and chemoresistance.

Zhang L, Hannay JA, Liu J, Das P, Zhan M, Nguyen T, Hicklin DJ, Yu D, Pollock RE, Lev D.

Cancer Res. 2006 Sep 1;66(17):8770-8.


Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases.

Lesslie DP, Summy JM, Parikh NU, Fan F, Trevino JG, Sawyer TK, Metcalf CA, Shakespeare WC, Hicklin DJ, Ellis LM, Gallick GE.

Br J Cancer. 2006 Jun 5;94(11):1710-7.


The vascular endothelial growth factor receptor (VEGFR-1) supports growth and survival of human breast carcinoma.

Wu Y, Hooper AT, Zhong Z, Witte L, Bohlen P, Rafii S, Hicklin DJ.

Int J Cancer. 2006 Oct 1;119(7):1519-29.


Cytokine-mediated deployment of SDF-1 induces revascularization through recruitment of CXCR4+ hemangiocytes.

Jin DK, Shido K, Kopp HG, Petit I, Shmelkov SV, Young LM, Hooper AT, Amano H, Avecilla ST, Heissig B, Hattori K, Zhang F, Hicklin DJ, Wu Y, Zhu Z, Dunn A, Salari H, Werb Z, Hackett NR, Crystal RG, Lyden D, Rafii S.

Nat Med. 2006 May;12(5):557-67. Epub 2006 Apr 30. Erratum in: Nat Med. 2006 Aug;12(8):978.


Synergistic antitumor effects of combined epidermal growth factor receptor and vascular endothelial growth factor receptor-2 targeted therapy.

Tonra JR, Deevi DS, Corcoran E, Li H, Wang S, Carrick FE, Hicklin DJ.

Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2197-207.


Targeted anti-vascular endothelial growth factor receptor-2 therapy leads to short-term and long-term impairment of vascular function and increase in tumor hypoxia.

Franco M, Man S, Chen L, Emmenegger U, Shaked Y, Cheung AM, Brown AS, Hicklin DJ, Foster FS, Kerbel RS.

Cancer Res. 2006 Apr 1;66(7):3639-48.


VEGF receptor 2 blockade leads to renal cyst formation in mice.

McGrath-Morrow S, Cho C, Molls R, Burne-Taney M, Haas M, Hicklin DJ, Tuder R, Rabb H.

Kidney Int. 2006 May;69(10):1741-8.


Strategies for delaying or treating in vivo acquired resistance to trastuzumab in human breast cancer xenografts.

du Manoir JM, Francia G, Man S, Mossoba M, Medin JA, Viloria-Petit A, Hicklin DJ, Emmenegger U, Kerbel RS.

Clin Cancer Res. 2006 Feb 1;12(3 Pt 1):904-16.

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