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Zalypsis: a novel marine-derived compound with potent antimyeloma activity that reveals high sensitivity of malignant plasma cells to DNA double-strand breaks.

Ocio EM, Maiso P, Chen X, Garayoa M, Alvarez-Fernández S, San-Segundo L, Vilanova D, López-Corral L, Montero JC, Hernández-Iglesias T, de Alava E, Galmarini C, Avilés P, Cuevas C, San-Miguel JF, Pandiella A.

Blood. 2009 Apr 16;113(16):3781-91. doi: 10.1182/blood-2008-09-177774. Epub 2008 Nov 19. Erratum in: Blood. 2010 Jul 8;116(1):151.


Zalypsis has in vitro activity in acute myeloid blasts and leukemic progenitor cells through the induction of a DNA damage response.

Colado E, Paíno T, Maiso P, Ocio EM, Chen X, Alvarez-Fernández S, Gutiérrez NC, Martín-Sánchez J, Flores-Montero J, San Segundo L, Garayoa M, Fernández-Lázaro D, Vidriales MB, Galmarini CM, Avilés P, Cuevas C, Pandiella A, San-Miguel JF.

Haematologica. 2011 May;96(5):687-95. doi: 10.3324/haematol.2010.036400. Epub 2011 Feb 17.


D-501036, a novel selenophene-based triheterocycle derivative, exhibits potent in vitro and in vivo antitumoral activity which involves DNA damage and ataxia telangiectasia-mutated nuclear protein kinase activation.

Juang SH, Lung CC, Hsu PC, Hsu KS, Li YC, Hong PC, Shiah HS, Kuo CC, Huang CW, Wang YC, Huang L, Chen TS, Chen SF, Fu KC, Hsu CL, Lin MJ, Chang CJ, Ashendel CL, Chan TC, Chou KM, Chang JY.

Mol Cancer Ther. 2007 Jan;6(1):193-202.


Oxaliplatin-induced gamma-H2AX activation via both p53-dependent and -independent pathways but is not associated with cell cycle arrest in human colorectal cancer cells.

Chiu SJ, Lee YJ, Hsu TS, Chen WS.

Chem Biol Interact. 2009 Dec 10;182(2-3):173-82. doi: 10.1016/j.cbi.2009.08.019. Epub 2009 Sep 6.


Atypical retinoids ST1926 and CD437 are S-phase-specific agents causing DNA double-strand breaks: significance for the cytotoxic and antiproliferative activity.

Valli C, Paroni G, Di Francesco AM, Riccardi R, Tavecchio M, Erba E, Boldetti A, Gianni' M, Fratelli M, Pisano C, Merlini L, Antoccia A, Cenciarelli C, Terao M, Garattini E.

Mol Cancer Ther. 2008 Sep;7(9):2941-54. doi: 10.1158/1535-7163.MCT-08-0419.


KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling.

Feng R, Ma H, Hassig CA, Payne JE, Smith ND, Mapara MY, Hager JH, Lentzsch S.

Mol Cancer Ther. 2008 Jun;7(6):1494-505. doi: 10.1158/1535-7163.MCT-08-0183.


Aplidin, a marine organism-derived compound with potent antimyeloma activity in vitro and in vivo.

Mitsiades CS, Ocio EM, Pandiella A, Maiso P, Gajate C, Garayoa M, Vilanova D, Montero JC, Mitsiades N, McMullan CJ, Munshi NC, Hideshima T, Chauhan D, Aviles P, Otero G, Faircloth G, Mateos MV, Richardson PG, Mollinedo F, San-Miguel JF, Anderson KC.

Cancer Res. 2008 Jul 1;68(13):5216-25. doi: 10.1158/0008-5472.CAN-07-5725.


p53 induction, cell cycle checkpoints, and apoptosis in DNAPK-deficient scid mice.

Gurley KE, Kemp CJ.

Carcinogenesis. 1996 Dec;17(12):2537-42.


E2F1 uses the ATM signaling pathway to induce p53 and Chk2 phosphorylation and apoptosis.

Powers JT, Hong S, Mayhew CN, Rogers PM, Knudsen ES, Johnson DG.

Mol Cancer Res. 2004 Apr;2(4):203-14.


CPT21, a novel compound with anti-proliferative effect against gastric cancer cell SGC7901.

Zhang B, Luo Y, Weng Q, He Q, Lu W, Yang B.

Invest New Drugs. 2008 Dec;26(6):517-24. doi: 10.1007/s10637-008-9120-9. Epub 2008 Feb 19.


The insulin-like growth factor-I receptor inhibitor NVP-AEW541 provokes cell cycle arrest and apoptosis in multiple myeloma cells.

Maiso P, Ocio EM, Garayoa M, Montero JC, Hofmann F, García-Echeverría C, Zimmermann J, Pandiella A, San Miguel JF.

Br J Haematol. 2008 May;141(4):470-82. doi: 10.1111/j.1365-2141.2008.07049.x. Epub 2008 Mar 12.


Bendamustine induces G2 cell cycle arrest and apoptosis in myeloma cells: the role of ATM-Chk2-Cdc25A and ATM-p53-p21-pathways.

Gaul L, Mandl-Weber S, Baumann P, Emmerich B, Schmidmaier R.

J Cancer Res Clin Oncol. 2008 Feb;134(2):245-53. Epub 2007 Jul 25.


PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity.

Leal JF, Martínez-Díez M, García-Hernández V, Moneo V, Domingo A, Bueren-Calabuig JA, Negri A, Gago F, Guillén-Navarro MJ, Avilés P, Cuevas C, García-Fernández LF, Galmarini CM.

Br J Pharmacol. 2010 Nov;161(5):1099-110. doi: 10.1111/j.1476-5381.2010.00945.x.


The selective Aurora B kinase inhibitor AZD1152 is a potential new treatment for multiple myeloma.

Evans RP, Naber C, Steffler T, Checkland T, Maxwell CA, Keats JJ, Belch AR, Pilarski LM, Lai R, Reiman T.

Br J Haematol. 2008 Feb;140(3):295-302. Epub 2007 Dec 10.


Novel genotoxicity assays identify norethindrone to activate p53 and phosphorylate H2AX.

Gallmeier E, Winter JM, Cunningham SC, Kahn SR, Kern SE.

Carcinogenesis. 2005 Oct;26(10):1811-20. Epub 2005 May 19.


Activation of ataxia telangiectasia mutated by DNA strand break-inducing agents correlates closely with the number of DNA double strand breaks.

Ismail IH, Nyström S, Nygren J, Hammarsten O.

J Biol Chem. 2005 Feb 11;280(6):4649-55. Epub 2004 Nov 15.


Generation of S phase-dependent DNA double-strand breaks by Cr(VI) exposure: involvement of ATM in Cr(VI) induction of gamma-H2AX.

Ha L, Ceryak S, Patierno SR.

Carcinogenesis. 2004 Nov;25(11):2265-74. Epub 2004 Jul 29.


Generation of replication-dependent double-strand breaks by the novel N2-G-alkylator S23906-1.

Léonce S, Kraus-Berthier L, Golsteyn RM, David-Cordonnier MH, Tardy C, Lansiaux A, Poindessous V, Larsen AK, Pierré A.

Cancer Res. 2006 Jul 15;66(14):7203-10.

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