PubMed

A phase I trial of UCN-01 and prednisone in patients with refractory solid tumors and lymphomas.

Kummar S, Gutierrez ME, Gardner ER, Figg WD, Melillo G, Dancey J, Sausville EA, Conley BA, Murgo AJ, Doroshow JH.

Cancer Chemother Pharmacol. 2009 Nov 6. [Epub ahead of print]PMID: 19894051 [PubMed - as supplied by publisher]Related articles

Clinical pharmacokinetics and exposure-toxicity relationship of a folate-Vinca alkaloid conjugate EC145 in cancer patients.

Li J, Sausville EA, Klein PJ, Morgenstern D, Leamon CP, Messmann RA, LoRusso P.

J Clin Pharmacol. 2009 Dec;49(12):1467-76. Epub 2009 Oct 16.PMID: 19837906 [PubMed - in process]Related articles

Biodistribution of HPMA copolymer-aminohexylgeldanamycin-RGDfK conjugates for prostate cancer drug delivery.

Borgman MP, Aras O, Geyser-Stoops S, Sausville EA, Ghandehari H.

Mol Pharm. 2009 Nov-Dec;6(6):1836-47.PMID: 19743884 [PubMed - in process]Related articles

Mitochondrial function as an emerging 'target of interest' for cancer treatment.

Sausville EA.

Curr Opin Investig Drugs. 2009 Jun;10(6):523-5. No abstract available. PMID: 19513940 [PubMed - indexed for MEDLINE]Related articles

Targetable HPMA copolymer-aminohexylgeldanamycin conjugates for prostate cancer therapy.

Borgman MP, Ray A, Kolhatkar RB, Sausville EA, Burger AM, Ghandehari H.

Pharm Res. 2009 Jun;26(6):1407-18. Epub 2009 Feb 19.PMID: 19225872 [PubMed - indexed for MEDLINE]Related articles

Phospho-p70S6K/p85S6K and cdc2/cdk1 are novel targets for diffuse large B-cell lymphoma combination therapy.

Zhao MY, Auerbach A, D'Costa AM, Rapoport AP, Burger AM, Sausville EA, Stass SA, Jiang F, Sands AM, Aguilera N, Zhao XF.

Clin Cancer Res. 2009 Mar 1;15(5):1708-20. Epub 2009 Feb 17.PMID: 19223503 [PubMed - indexed for MEDLINE]Related articles

Preclinical studies of vorinostat (suberoylanilide hydroxamic acid) combined with cytosine arabinoside and etoposide for treatment of acute leukemias.

Shiozawa K, Nakanishi T, Tan M, Fang HB, Wang WC, Edelman MJ, Carlton D, Gojo I, Sausville EA, Ross DD.

Clin Cancer Res. 2009 Mar 1;15(5):1698-707. Epub 2009 Feb 17.PMID: 19223502 [PubMed - indexed for MEDLINE]Related articles

A mechanistic perspective of monoclonal antibodies in cancer therapy beyond target-related effects.

Strome SE, Sausville EA, Mann D.

Oncologist. 2007 Sep;12(9):1084-95. Review.PMID: 17914078 [PubMed - indexed for MEDLINE]Related articlesFree article

Inhibition of mitochondrial respiration as a source of adaphostin-induced reactive oxygen species and cytotoxicity.

Le SB, Hailer MK, Buhrow S, Wang Q, Flatten K, Pediaditakis P, Bible KC, Lewis LD, Sausville EA, Pang YP, Ames MM, Lemasters JJ, Holmuhamedov EL, Kaufmann SH.

J Biol Chem. 2007 Mar 23;282(12):8860-72. Epub 2007 Jan 9.PMID: 17213201 [PubMed - indexed for MEDLINE]Related articlesFree article

Phase 1 and pharmacologic study of MS-275, a histone deacetylase inhibitor, in adults with refractory and relapsed acute leukemias.

Gojo I, Jiemjit A, Trepel JB, Sparreboom A, Figg WD, Rollins S, Tidwell ML, Greer J, Chung EJ, Lee MJ, Gore SD, Sausville EA, Zwiebel J, Karp JE.

Blood. 2007 Apr 1;109(7):2781-90.PMID: 17179232 [PubMed - indexed for MEDLINE]Related articlesFree article

Molecular mechanism of adaphostin-mediated G1 arrest in prostate cancer (PC-3) cells: signaling events mediated by hepatocyte growth factor receptor, c-Met, and p38 MAPK pathways.

Mukhopadhyay I, Sausville EA, Doroshow JH, Roy KK.

J Biol Chem. 2006 Dec 8;281(49):37330-44. Epub 2006 Sep 6.PMID: 16956884 [PubMed - indexed for MEDLINE]Related articlesFree article

Respecting cancer drug transportability: a basis for successful lead selection.

Sausville EA.

J Natl Cancer Inst. 2006 Aug 16;98(16):1098-9. No abstract available. PMID: 16912257 [PubMed - indexed for MEDLINE]Related articlesFree article

The TSC2/mTOR pathway drives endothelial cell transformation induced by the Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor.

Sodhi A, Chaisuparat R, Hu J, Ramsdell AK, Manning BD, Sausville EA, Sawai ET, Molinolo A, Gutkind JS, Montaner S.

Cancer Cell. 2006 Aug;10(2):133-43.PMID: 16904612 [PubMed - indexed for MEDLINE]Related articles

Contributions of human tumor xenografts to anticancer drug development.

Sausville EA, Burger AM.

Cancer Res. 2006 Apr 1;66(7):3351-4, discussion 3354. Review.PMID: 16585151 [PubMed - indexed for MEDLINE]Related articlesFree article

Factors affecting the pharmacokinetic profile of MS-275, a novel histone deacetylase inhibitor, in patients with cancer.

Acharya MR, Karp JE, Sausville EA, Hwang K, Ryan Q, Gojo I, Venitz J, Figg WD, Sparreboom A.

Invest New Drugs. 2006 Sep;24(5):367-75.PMID: 16583304 [PubMed - indexed for MEDLINE]Related articles

Ligand-directed surface profiling of human cancer cells with combinatorial peptide libraries.

Kolonin MG, Bover L, Sun J, Zurita AJ, Do KA, Lahdenranta J, Cardó-Vila M, Giordano RJ, Jaalouk DE, Ozawa MG, Moya CA, Souza GR, Staquicini FI, Kunyiasu A, Scudiero DA, Holbeck SL, Sausville EA, Arap W, Pasqualini R.

Cancer Res. 2006 Jan 1;66(1):34-40.PMID: 16397212 [PubMed - indexed for MEDLINE]Related articlesFree article

Preclinical modeling of combination treatments: fantasy or requirement?

Decker S, Sausville EA.

Ann N Y Acad Sci. 2005 Nov;1059:61-9. Review.PMID: 16382044 [PubMed - indexed for MEDLINE]Related articles

Differential gene expression as a potential classifier of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole-sensitive and -insensitive cell lines.

Wallqvist A, Connelly J, Sausville EA, Covell DG, Monks A.

Mol Pharmacol. 2006 Mar;69(3):737-48. Epub 2005 Dec 6.PMID: 16332985 [PubMed - indexed for MEDLINE]Related articlesFree article

Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells.

Brantley E, Antony S, Kohlhagen G, Meng L, Agama K, Stinson SF, Sausville EA, Pommier Y.

Cancer Chemother Pharmacol. 2006 Jul;58(1):62-72. Epub 2005 Dec 6.PMID: 16331501 [PubMed - indexed for MEDLINE]Related articles

Mammalian target of rapamycin, a molecular target in squamous cell carcinomas of the head and neck.

Amornphimoltham P, Patel V, Sodhi A, Nikitakis NG, Sauk JJ, Sausville EA, Molinolo AA, Gutkind JS.

Cancer Res. 2005 Nov 1;65(21):9953-61.PMID: 16267020 [PubMed - indexed for MEDLINE]Related articlesFree article

Histone deacetylase inhibitor pharmacodynamic analysis by multiparameter flow cytometry.

Chung EJ, Lee S, Sausville EA, Ryan Q, Karp JE, Gojo I, Telford WG, Lee MJ, Kong HS, Trepel JB.

Ann Clin Lab Sci. 2005 Autumn;35(4):397-406.PMID: 16254255 [PubMed - indexed for MEDLINE]Related articles

Cell cycle regulatory kinase modulators: interim progress and issues.

Sausville EA.

Curr Top Med Chem. 2005;5(12):1109-17. Review.PMID: 16248786 [PubMed - indexed for MEDLINE]Related articles

Transcriptional profiling identifies altered intracellular labile iron homeostasis as a contributing factor to the toxicity of adaphostin: decreased vascular endothelial growth factor secretion is independent of hypoxia-inducible factor-1 regulation.

Hose C, Kaur G, Sausville EA, Monks A.

Clin Cancer Res. 2005 Sep 1;11(17):6370-81.PMID: 16144942 [PubMed - indexed for MEDLINE]Related articlesFree article

Benzodithiophenes induce differentiation and apoptosis in human leukemia cells.

Jing Y, Hellinger N, Xia L, Monks A, Sausville EA, Zelent A, Waxman S.

Cancer Res. 2005 Sep 1;65(17):7847-55.PMID: 16140954 [PubMed - indexed for MEDLINE]Related articlesFree article

Adaphostin and other anticancer drugs quench the fluorescence of mitochondrial potential probes.

Le SB, Holmuhamedov EL, Narayanan VL, Sausville EA, Kaufmann SH.

Cell Death Differ. 2006 Jan;13(1):151-9.PMID: 16052237 [PubMed - indexed for MEDLINE]Related articlesFree article

Interspecies differences in plasma protein binding of MS-275, a novel histone deacetylase inhibitor.

Acharya MR, Sparreboom A, Sausville EA, Conley BA, Doroshow JH, Venitz J, Figg WD.

Cancer Chemother Pharmacol. 2006 Feb;57(3):275-81. Epub 2005 Jul 19.PMID: 16028097 [PubMed - indexed for MEDLINE]Related articles

Inhibition of nuclear factor-kappaB and target genes during combined therapy with proteasome inhibitor bortezomib and reirradiation in patients with recurrent head-and-neck squamous cell carcinoma.

Van Waes C, Chang AA, Lebowitz PF, Druzgal CH, Chen Z, Elsayed YA, Sunwoo JB, Rudy SF, Morris JC, Mitchell JB, Camphausen K, Gius D, Adams J, Sausville EA, Conley BA.

Int J Radiat Oncol Biol Phys. 2005 Dec 1;63(5):1400-12. Epub 2005 Jul 11.PMID: 16005577 [PubMed - indexed for MEDLINE]Related articles

Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance.

Glaze ER, Lambert AL, Smith AC, Page JG, Johnson WD, McCormick DL, Brown AP, Levine BS, Covey JM, Egorin MJ, Eiseman JL, Holleran JL, Sausville EA, Tomaszewski JE.

Cancer Chemother Pharmacol. 2005 Dec;56(6):637-47. Epub 2005 Jun 29.PMID: 15986212 [PubMed - indexed for MEDLINE]Related articles

Making bad cells go good: the promise of epigenetic therapy.

Sausville EA, Carducci MA.

J Clin Oncol. 2005 Jun 10;23(17):3875-6. Review. No abstract available. PMID: 15946932 [PubMed - indexed for MEDLINE]Related articles

Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma.

Ryan QC, Headlee D, Acharya M, Sparreboom A, Trepel JB, Ye J, Figg WD, Hwang K, Chung EJ, Murgo A, Melillo G, Elsayed Y, Monga M, Kalnitskiy M, Zwiebel J, Sausville EA.

J Clin Oncol. 2005 Jun 10;23(17):3912-22. Epub 2005 Apr 25.PMID: 15851766 [PubMed - indexed for MEDLINE]Related articles

Atiprimod is an inhibitor of cancer cell proliferation and angiogenesis.

Shailubhai K, Dheer S, Picker D, Kaur G, Sausville EA, Jacob GS.

J Exp Ther Oncol. 2004 Dec;4(4):267-79.PMID: 15844657 [PubMed - indexed for MEDLINE]Related articles

Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models.

Smith V, Sausville EA, Camalier RF, Fiebig HH, Burger AM.

Cancer Chemother Pharmacol. 2005 Aug;56(2):126-37. Epub 2005 Apr 20.PMID: 15841378 [PubMed - indexed for MEDLINE]Related articles

In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative.

Hollingshead M, Alley M, Burger AM, Borgel S, Pacula-Cox C, Fiebig HH, Sausville EA.

Cancer Chemother Pharmacol. 2005 Aug;56(2):115-25. Epub 2005 Mar 25.PMID: 15791458 [PubMed - indexed for MEDLINE]Related articles

Review of UCN-01 development: a lesson in the importance of clinical pharmacology.

Fuse E, Kuwabara T, Sparreboom A, Sausville EA, Figg WD.

J Clin Pharmacol. 2005 Apr;45(4):394-403. Review.PMID: 15778420 [PubMed - indexed for MEDLINE]Related articles

Cytotoxicity of RH1: NAD(P)H:quinone acceptor oxidoreductase (NQO1)-independent oxidative stress and apoptosis induction.

Tudor G, Alley M, Nelson CM, Huang R, Covell DG, Gutierrez P, Sausville EA.

Anticancer Drugs. 2005 Apr;16(4):381-91.PMID: 15746574 [PubMed - indexed for MEDLINE]Related articles

Homology model of the CDK1/cyclin B complex.

McGrath CF, Pattabiraman N, Kellogg GE, Lemcke T, Kunick C, Sausville EA, Zaharevitz DW, Gussio R.

J Biomol Struct Dyn. 2005 Apr;22(5):493-502.PMID: 15702922 [PubMed - indexed for MEDLINE]Related articlesFree article

Indifferently pursued or unowned drugs: who should lead where companies do not tread?

Sausville EA.

J Clin Oncol. 2005 Mar 20;23(9):1796-8. Epub 2005 Feb 7. No abstract available. PMID: 15699475 [PubMed - indexed for MEDLINE]Related articles

Synthesis, structure-activity relationship, and p210(bcr-abl) protein tyrosine kinase activity of novel AG 957 analogs.

Kaur G, Narayanan VL, Risbood PA, Hollingshead MG, Stinson SF, Varma RK, Sausville EA.

Bioorg Med Chem. 2005 Mar 1;13(5):1749-61.PMID: 15698792 [PubMed - indexed for MEDLINE]Related articles

Geldanamycin analogs.

Sausville EA.

J Chemother. 2004 Nov;16 Suppl 4:68-9. Review.PMID: 15688614 [PubMed - indexed for MEDLINE]Related articles

Target selection issues in drug discovery and development.

Sausville EA.

J Chemother. 2004 Nov;16 Suppl 4:16-8. Review.PMID: 15688602 [PubMed - indexed for MEDLINE]Related articles

Cytotoxicities of three rebeccamycin derivatives in the National Cancer Institute screening of 60 human tumor cell lines.

Moreau P, Holbeck S, Prudhomme M, Sausville EA.

Anticancer Drugs. 2005 Feb;16(2):145-50.PMID: 15655411 [PubMed - indexed for MEDLINE]Related articles

The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces NF-kappaB activity in drug-sensitive MCF-7 cells.

Brantley E, Patel V, Stinson SF, Trapani V, Hose CD, Ciolino HP, Yeh GC, Gutkind JS, Sausville EA, Loaiza-Pérez AI.

Anticancer Drugs. 2005 Feb;16(2):137-43.PMID: 15655410 [PubMed - indexed for MEDLINE]Related articles

In vivo models for experimental therapeutics relevant to human cancer.

Gitler MS, Sausville EA, Hollingshead M, Shoemaker R.

Cancer Res. 2004 Nov 15;64(22):8478-80. No abstract available. PMID: 15548722 [PubMed - indexed for MEDLINE]Related articlesFree article

Transcription profiling of gene expression in drug discovery and development: the NCI experience.

Sausville EA, Holbeck SL.

Eur J Cancer. 2004 Nov;40(17):2544-9. Review.PMID: 15541957 [PubMed - indexed for MEDLINE]Related articles

7-hydroxystaurosporine (UCN-01) inhibition of Akt Thr308 but not Ser473 phosphorylation: a basis for decreased insulin-stimulated glucose transport.

Kondapaka SB, Zarnowski M, Yver DR, Sausville EA, Cushman SW.

Clin Cancer Res. 2004 Nov 1;10(21):7192-8.PMID: 15534092 [PubMed - indexed for MEDLINE]Related articlesFree article

Effects of alpha1-acid glycoprotein on the clinical pharmacokinetics of 7-hydroxystaurosporine.

Sparreboom A, Chen H, Acharya MR, Senderowicz AM, Messmann RA, Kuwabara T, Venzon DJ, Murgo AJ, Headlee D, Sausville EA, Figg WD.

Clin Cancer Res. 2004 Oct 15;10(20):6840-6.PMID: 15501960 [PubMed - indexed for MEDLINE]Related articlesFree article

Components of the cell death machine and drug sensitivity of the National Cancer Institute Cell Line Panel.

Svingen PA, Loegering D, Rodriquez J, Meng XW, Mesner PW Jr, Holbeck S, Monks A, Krajewski S, Scudiero DA, Sausville EA, Reed JC, Lazebnik YA, Kaufmann SH.

Clin Cancer Res. 2004 Oct 15;10(20):6807-20.PMID: 15501957 [PubMed - indexed for MEDLINE]Related articlesFree article

The broad-range cyclin-dependent kinase inhibitor UCN-01 induces apoptosis in colon carcinoma cells through transcriptional suppression of the Bcl-x(L) protein.

Bhonde MR, Hanski ML, Magrini R, Moorthy D, Müller A, Sausville EA, Kohno K, Wiegand P, Daniel PT, Zeitz M, Hanski C.

Oncogene. 2005 Jan 6;24(1):148-56.PMID: 15467762 [PubMed - indexed for MEDLINE]Related articles

Adaphostin-induced apoptosis in CLL B cells is associated with induction of oxidative stress and exhibits synergy with fludarabine.

Shanafelt TD, Lee YK, Bone ND, Strege AK, Narayanan VL, Sausville EA, Geyer SM, Kaufmann SH, Kay NE.

Blood. 2005 Mar 1;105(5):2099-106. Epub 2004 Sep 23.PMID: 15388586 [PubMed - indexed for MEDLINE]Related articlesFree article

Optimizing target selection and development strategy in cancer treatment: the next wave.

Sausville EA.

Curr Med Chem Anticancer Agents. 2004 Sep;4(5):445-7. Review.PMID: 15379701 [PubMed - indexed for MEDLINE]Related articles