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Items: 40

1.

Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.

Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J.

Eur J Med Chem. 2019 Apr 15;168:87-109. doi: 10.1016/j.ejmech.2019.02.022. Epub 2019 Feb 19.

PMID:
30802730
2.

Identification of novel PI3K inhibitors through a scaffold hopping strategy.

Martínez González S, Hernández AI, Álvarez RM, Rodríguez A, Ramos-Lima F, Bischoff JR, Albarrán MI, Cebriá A, Hernández-Encinas E, García-Arocha J, Cebrián D, Blanco-Aparicio C, Pastor J.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4794-4799. doi: 10.1016/j.bmcl.2017.09.059. Epub 2017 Sep 30.

PMID:
29017786
3.

Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.

Martínez González S, Rodríguez-Arístegui S, Hernández AI, Varela C, González Cantalapiedra E, Álvarez RM, Rodríguez Hergueta A, Bischoff JR, Albarrán MI, Cebriá A, Cendón E, Cebrián D, Alfonso P, Pastor J.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2536-2543. doi: 10.1016/j.bmcl.2017.03.090. Epub 2017 Apr 2.

PMID:
28404374
4.

PIM kinases as potential therapeutic targets in a subset of peripheral T cell lymphoma cases.

Martín-Sánchez E, Odqvist L, Rodríguez-Pinilla SM, Sánchez-Beato M, Roncador G, Domínguez-González B, Blanco-Aparicio C, García Collazo AM, Cantalapiedra EG, Fernández JP, Curiel del Olmo S, Pisonero H, Madureira R, Almaraz C, Mollejo M, Alves FJ, Menárguez J, González-Palacios F, Rodríguez-Peralto JL, Ortiz-Romero PL, Real FX, García JF, Bischoff JR, Piris MA.

PLoS One. 2014 Nov 11;9(11):e112148. doi: 10.1371/journal.pone.0112148. eCollection 2014.

5.

Fragment-hopping-based discovery of a novel chemical series of proto-oncogene PIM-1 kinase inhibitors.

Saluste G, Albarran MI, Alvarez RM, Rabal O, Ortega MA, Blanco C, Kurz G, Salgado A, Pevarello P, Bischoff JR, Pastor J, Oyarzabal J.

PLoS One. 2012;7(10):e45964. doi: 10.1371/journal.pone.0045964. Epub 2012 Oct 24.

6.

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Martínez González S, Hernández AI, Varela C, Lorenzo M, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán MI, Alfonso P, García-Serelde B, Mateos G, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Blanco-Aparicio C, Pastor J.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5208-14. doi: 10.1016/j.bmcl.2012.06.093. Epub 2012 Jul 4.

PMID:
22819764
7.

Simultaneous inhibition of pan-phosphatidylinositol-3-kinases and MEK as a potential therapeutic strategy in peripheral T-cell lymphomas.

Martín-Sánchez E, Rodríguez-Pinilla SM, Sánchez-Beato M, Lombardía L, Domínguez-González B, Romero D, Odqvist L, García-Sanz P, Wozniak MB, Kurz G, Blanco-Aparicio C, Mollejo M, Alves FJ, Menárguez J, González-Palacios F, Rodríguez-Peralto JL, Ortiz-Romero PL, García JF, Bischoff JR, Piris MA.

Haematologica. 2013 Jan;98(1):57-64. doi: 10.3324/haematol.2012.068510. Epub 2012 Jul 16.

8.

Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases.

Granda TG, Cebrián D, Martínez S, Anguita PV, López EC, Link W, Merino T, Pastor J, Serelde BG, Peregrina S, Palacios I, Albarran MI, Cebriá A, Lorenzo M, Alonso P, Fominaya J, López AR, Bischoff JR.

Invest New Drugs. 2013 Feb;31(1):66-76. doi: 10.1007/s10637-012-9835-5. Epub 2012 May 24.

PMID:
22623067
9.

Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.

Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J.

Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. doi: 10.1016/j.bmcl.2012.03.090. Epub 2012 Mar 29.

PMID:
22520259
10.

Pten positively regulates brown adipose function, energy expenditure, and longevity.

Ortega-Molina A, Efeyan A, Lopez-Guadamillas E, Muñoz-Martin M, Gómez-López G, Cañamero M, Mulero F, Pastor J, Martinez S, Romanos E, Mar Gonzalez-Barroso M, Rial E, Valverde AM, Bischoff JR, Serrano M.

Cell Metab. 2012 Mar 7;15(3):382-94. doi: 10.1016/j.cmet.2012.02.001.

11.

Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.

Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Alvarez RM, García AB, Lorenzo M, Rivero V, Oyarzabal J, Rabal O, Bischoff JR, Albarrán M, Cebriá A, Alfonso P, Link W, Fominaya J, Pastor J.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. doi: 10.1016/j.bmcl.2012.01.074. Epub 2012 Jan 28.

PMID:
22325943
12.

PIM2 inhibition as a rational therapeutic approach in B-cell lymphoma.

Gómez-Abad C, Pisonero H, Blanco-Aparicio C, Roncador G, González-Menchén A, Martinez-Climent JA, Mata E, Rodríguez ME, Muñoz-González G, Sánchez-Beato M, Leal JF, Bischoff JR, Piris MA.

Blood. 2011 Nov 17;118(20):5517-27. doi: 10.1182/blood-2011-03-344374. Epub 2011 Sep 21.

13.

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

Toledo LI, Murga M, Zur R, Soria R, Rodriguez A, Martinez S, Oyarzabal J, Pastor J, Bischoff JR, Fernandez-Capetillo O.

Nat Struct Mol Biol. 2011 Jun;18(6):721-7. doi: 10.1038/nsmb.2076. Epub 2011 May 8.

14.

Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition.

Blanco-Aparicio C, Collazo AM, Oyarzabal J, Leal JF, Albarán MI, Lima FR, Pequeño B, Ajenjo N, Becerra M, Alfonso P, Reymundo MI, Palacios I, Mateos G, Quiñones H, Corrionero A, Carnero A, Pevarello P, Lopez AR, Fominaya J, Pastor J, Bischoff JR.

Cancer Lett. 2011 Jan 28;300(2):145-53. doi: 10.1016/j.canlet.2010.09.016. Epub 2010 Nov 3.

PMID:
21051136
15.

HDAC inhibitors induce cell cycle arrest, activate the apoptotic extrinsic pathway and synergize with a novel PIM inhibitor in Hodgkin lymphoma-derived cell lines.

Martín-Sánchez E, Sánchez-Beato M, Rodríguez ME, Sánchez-Espiridión B, Gómez-Abad C, Bischoff JR, Piris MA, García-Orad A, García JF.

Br J Haematol. 2011 Feb;152(3):352-6. doi: 10.1111/j.1365-2141.2010.08401.x. Epub 2010 Oct 19. No abstract available.

PMID:
20955406
16.

Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A, Fominaya J, Pastor J, Bischoff JR.

J Med Chem. 2010 Sep 23;53(18):6618-28. doi: 10.1021/jm1005513.

PMID:
20722422
17.

An integrated one-step system to extract, analyze and annotate all relevant information from image-based cell screening of chemical libraries.

Rabal O, Link W, Serelde BG, Bischoff JR, Oyarzabal J.

Mol Biosyst. 2010 Apr;6(4):711-20. doi: 10.1039/b919830j. Epub 2010 Jan 21.

PMID:
20237649
18.

Vorinostat interferes with the signaling transduction pathway of T-cell receptor and synergizes with phosphoinositide-3 kinase inhibitors in cutaneous T-cell lymphoma.

Wozniak MB, Villuendas R, Bischoff JR, Aparicio CB, Martínez Leal JF, de La Cueva P, Rodriguez ME, Herreros B, Martin-Perez D, Longo MI, Herrera M, Piris MA, Ortiz-Romero PL.

Haematologica. 2010 Apr;95(4):613-21. doi: 10.3324/haematol.2009.013870. Epub 2010 Feb 4.

19.

Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases.

Link W, Oyarzabal J, Serelde BG, Albarran MI, Rabal O, Cebriá A, Alfonso P, Fominaya J, Renner O, Peregrina S, Soilán D, Ceballos PA, Hernández AI, Lorenzo M, Pevarello P, Granda TG, Kurz G, Carnero A, Bischoff JR.

J Biol Chem. 2009 Oct 9;284(41):28392-400. doi: 10.1074/jbc.M109.038984. Epub 2009 Aug 18.

20.

CDK inhibitors in cancer therapy: what is next?

Malumbres M, Pevarello P, Barbacid M, Bischoff JR.

Trends Pharmacol Sci. 2008 Jan;29(1):16-21. Epub 2007 Dec 4.

PMID:
18054800
21.

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittalà V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14.

PMID:
16290148
22.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C.

J Med Chem. 2005 Apr 21;48(8):2944-56. Erratum in: J Med Chem. 2005 Jul 28;48(15):5058.

PMID:
15828833
23.

The STE20 kinase HGK is broadly expressed in human tumor cells and can modulate cellular transformation, invasion, and adhesion.

Wright JH, Wang X, Manning G, LaMere BJ, Le P, Zhu S, Khatry D, Flanagan PM, Buckley SD, Whyte DB, Howlett AR, Bischoff JR, Lipson KE, Jallal B.

Mol Cell Biol. 2003 Mar;23(6):2068-82.

24.

Requirement for PAK4 in the anchorage-independent growth of human cancer cell lines.

Callow MG, Clairvoyant F, Zhu S, Schryver B, Whyte DB, Bischoff JR, Jallal B, Smeal T.

J Biol Chem. 2002 Jan 4;277(1):550-8. Epub 2001 Oct 19.

25.

BIRinging chromosomes through cell division--and survivin' the experience.

Reed JC, Bischoff JR.

Cell. 2000 Sep 1;102(5):545-8. Review. No abstract available.

26.

The Aurora/Ipl1p kinase family: regulators of chromosome segregation and cytokinesis.

Bischoff JR, Plowman GD.

Trends Cell Biol. 1999 Nov;9(11):454-9. Review.

PMID:
10511710
27.

A homologue of Drosophila aurora kinase is oncogenic and amplified in human colorectal cancers.

Bischoff JR, Anderson L, Zhu Y, Mossie K, Ng L, Souza B, Schryver B, Flanagan P, Clairvoyant F, Ginther C, Chan CS, Novotny M, Slamon DJ, Plowman GD.

EMBO J. 1998 Jun 1;17(11):3052-65.

28.

An adenovirus mutant that replicates selectively in p53-deficient human tumor cells.

Bischoff JR, Kirn DH, Williams A, Heise C, Horn S, Muna M, Ng L, Nye JA, Sampson-Johannes A, Fattaey A, McCormick F.

Science. 1996 Oct 18;274(5286):373-6.

PMID:
8832876
29.

Transcriptional activation of the human proliferating-cell nuclear antigen promoter by p53.

Morris GF, Bischoff JR, Mathews MB.

Proc Natl Acad Sci U S A. 1996 Jan 23;93(2):895-9.

30.

Signal transduction by Ras-like GTPases: a potential target for anticancer drugs.

Spaargaren M, Bischoff JR, McCormick F.

Gene Expr. 1995;4(6):345-56. Review.

31.
32.

The Ras-related protein R-ras interacts directly with Raf-1 in a GTP-dependent manner.

Spaargaren M, Martin GA, McCormick F, Fernandez-Sarabia MJ, Bischoff JR.

Biochem J. 1994 Jun 1;300 ( Pt 2):303-7.

33.

Bcl-2 associates with the ras-related protein R-ras p23.

Fernandez-Sarabia MJ, Bischoff JR.

Nature. 1993 Nov 18;366(6452):274-5.

PMID:
8232588
34.

Human p53 inhibits growth in Schizosaccharomyces pombe.

Bischoff JR, Casso D, Beach D.

Mol Cell Biol. 1992 Apr;12(4):1405-11.

35.

p34cdc2-mediated phosphorylation at T124 inhibits nuclear import of SV-40 T antigen proteins.

Jans DA, Ackermann MJ, Bischoff JR, Beach DH, Peters R.

J Cell Biol. 1991 Dec;115(5):1203-12.

36.

A complex containing p34cdc2 and cyclin B phosphorylates the nuclear lamin and disassembles nuclei of clam oocytes in vitro.

Dessev G, Iovcheva-Dessev C, Bischoff JR, Beach D, Goldman R.

J Cell Biol. 1991 Feb;112(4):523-33.

37.

Intermediate filament reorganization during mitosis is mediated by p34cdc2 phosphorylation of vimentin.

Chou YH, Bischoff JR, Beach D, Goldman RD.

Cell. 1990 Sep 21;62(6):1063-71.

PMID:
2169348
38.

Human p53 is phosphorylated by p60-cdc2 and cyclin B-cdc2.

Bischoff JR, Friedman PN, Marshak DR, Prives C, Beach D.

Proc Natl Acad Sci U S A. 1990 Jun;87(12):4766-70.

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