Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 65

1.

Reversible dual inhibitor against G9a and DNMT1 improves human iPSC derivation enhancing MET and facilitating transcription factor engagement to the genome.

Rodriguez-Madoz JR, San Jose-Eneriz E, Rabal O, Zapata-Linares N, Miranda E, Rodriguez S, Porciuncula A, Vilas-Zornoza A, Garate L, Segura V, Guruceaga E, Agirre X, Oyarzabal J, Prosper F.

PLoS One. 2017 Dec 27;12(12):e0190275. doi: 10.1371/journal.pone.0190275. eCollection 2017.

2.

Targeting the anion exchanger 2 with specific peptides as a new therapeutic approach in B lymphoid neoplasms.

Celay J, Lozano T, Concepcion AR, Beltrán E, Rudilla F, García-Barchino MJ, Robles EF, Rabal O, de Miguel I, Panizo C, Casares N, Oyarzabal J, Prieto J, Medina JF, Lasarte JJ, Martínez-Climent JÁ.

Haematologica. 2017 Nov 30. pii: haematol.2017.175687. doi: 10.3324/haematol.2017.175687. [Epub ahead of print]

3.

Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB2 Receptors.

Martínez-Pinilla E, Varani K, Reyes-Resina I, Angelats E, Vincenzi F, Ferreiro-Vera C, Oyarzabal J, Canela EI, Lanciego JL, Nadal X, Navarro G, Borea PA, Franco R.

Front Pharmacol. 2017 Oct 23;8:744. doi: 10.3389/fphar.2017.00744. eCollection 2017.

4.

Blockage of FOXP3 transcription factor dimerization and FOXP3/AML1 interaction inhibits T regulatory cell activity: sequence optimization of a peptide inhibitor.

Lozano T, Gorraiz M, Lasarte-Cía A, Ruiz M, Rabal O, Oyarzabal J, Hervás-Stubbs S, Llopiz D, Sarobe P, Prieto J, Casares N, Lasarte JJ.

Oncotarget. 2017 May 13;8(42):71709-71724. doi: 10.18632/oncotarget.17845. eCollection 2017 Sep 22.

5.

Identification of LAG3 high affinity aptamers by HT-SELEX and Conserved Motif Accumulation (CMA).

Soldevilla MM, Hervas S, Villanueva H, Lozano T, Rabal O, Oyarzabal J, Lasarte JJ, Bendandi M, Inoges S, López-Díaz de Cerio A, Pastor F.

PLoS One. 2017 Sep 21;12(9):e0185169. doi: 10.1371/journal.pone.0185169. eCollection 2017.

6.

Dual epigenetic modifiers for cancer therapy.

José-Enériz ES, Rabal O, Agirre X, Oyarzabal J, Prosper F.

Mol Cell Oncol. 2017 Jun 20;4(4):e1342748. doi: 10.1080/23723556.2017.1342748. eCollection 2017.

PMID:
28868353
7.

Inducing heat shock protein 70 expression provides a robust antithrombotic effect with minimal bleeding risk.

Allende M, Molina E, Lecumberri R, Sanchez-Arias JA, Ugarte A, Guruceaga E, Oyarzabal J, Hermida J.

Thromb Haemost. 2017 Aug 30;117(9):1722-1729. doi: 10.1160/TH17-02-0108. Epub 2017 Jul 27.

PMID:
28837204
8.

GPR55: A therapeutic target for Parkinson's disease?

Celorrio M, Rojo-Bustamante E, Fernández-Suárez D, Sáez E, Estella-Hermoso de Mendoza A, Müller CE, Ramírez MJ, Oyarzábal J, Franco R, Aymerich MS.

Neuropharmacology. 2017 Oct;125:319-332. doi: 10.1016/j.neuropharm.2017.08.017. Epub 2017 Aug 12.

PMID:
28807673
9.

CM352 Reduces Brain Damage and Improves Functional Recovery in a Rat Model of Intracerebral Hemorrhage.

Rodríguez JA, Sobrino T, López-Arias E, Ugarte A, Sánchez-Arias JA, Vieites-Prado A, de Miguel I, Oyarzabal J, Páramo JA, Campos F, Orbe J, Castillo J.

J Am Heart Assoc. 2017 Jun 1;6(6). pii: e006042. doi: 10.1161/JAHA.117.006042.

10.

Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.

San José-Enériz E, Agirre X, Rabal O, Vilas-Zornoza A, Sanchez-Arias JA, Miranda E, Ugarte A, Roa S, Paiva B, Estella-Hermoso de Mendoza A, Alvarez RM, Casares N, Segura V, Martín-Subero JI, Ogi FX, Soule P, Santiveri CM, Campos-Olivas R, Castellano G, de Barrena MGF, Rodriguez-Madoz JR, García-Barchino MJ, Lasarte JJ, Avila MA, Martinez-Climent JA, Oyarzabal J, Prosper F.

Nat Commun. 2017 May 26;8:15424. doi: 10.1038/ncomms15424.

11.

LimTox: a web tool for applied text mining of adverse event and toxicity associations of compounds, drugs and genes.

Cañada A, Capella-Gutierrez S, Rabal O, Oyarzabal J, Valencia A, Krallinger M.

Nucleic Acids Res. 2017 Jul 3;45(W1):W484-W489. doi: 10.1093/nar/gkx462.

12.

Information Retrieval and Text Mining Technologies for Chemistry.

Krallinger M, Rabal O, Lourenço A, Oyarzabal J, Valencia A.

Chem Rev. 2017 Jun 28;117(12):7673-7761. doi: 10.1021/acs.chemrev.6b00851. Epub 2017 May 5. Review.

PMID:
28475312
13.

Impact of Scaffold Exploration on Novel Dual-Acting Histone Deacetylases and Phosphodiesterase 5 Inhibitors for the Treatment of Alzheimer's Disease.

Sánchez-Arias JA, Rabal O, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, Ugarte A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J.

ACS Chem Neurosci. 2017 Mar 15;8(3):638-661. doi: 10.1021/acschemneuro.6b00370. Epub 2016 Dec 27.

PMID:
27936591
14.

In Silico Aptamer Docking Studies: From a Retrospective Validation to a Prospective Case Study-TIM3 Aptamers Binding.

Rabal O, Pastor F, Villanueva H, Soldevilla MM, Hervas-Stubbs S, Oyarzabal J.

Mol Ther Nucleic Acids. 2016 Oct 18;5(10):e376. doi: 10.1038/mtna.2016.84.

15.

Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.

Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J.

J Med Chem. 2016 Oct 13;59(19):8967-9004. Epub 2016 Sep 27.

PMID:
27606546
16.

A First-in-Class Small-Molecule that Acts as a Dual Inhibitor of HDAC and PDE5 and that Rescues Hippocampal Synaptic Impairment in Alzheimer's Disease Mice.

Cuadrado-Tejedor M, Garcia-Barroso C, Sánchez-Arias JA, Rabal O, Pérez-González M, Mederos S, Ugarte A, Franco R, Segura V, Perea G, Oyarzabal J, Garcia-Osta A.

Neuropsychopharmacology. 2017 Jan;42(2):524-539. doi: 10.1038/npp.2016.163. Epub 2016 Aug 23.

17.

The Markyt visualisation, prediction and benchmark platform for chemical and gene entity recognition at BioCreative/CHEMDNER challenge.

Pérez-Pérez M, Pérez-Rodríguez G, Rabal O, Vazquez M, Oyarzabal J, Fdez-Riverola F, Valencia A, Krallinger M, Lourenço A.

Database (Oxford). 2016 Aug 19;2016. pii: baw120. doi: 10.1093/database/baw120. Print 2016.

18.

Two Affinity Sites of the Cannabinoid Subtype 2 Receptor Identified by a Novel Homogeneous Binding Assay.

Martínez-Pinilla E, Rabal O, Reyes-Resina I, Zamarbide M, Navarro G, Sánchez-Arias JA, de Miguel I, Lanciego JL, Oyarzabal J, Franco R.

J Pharmacol Exp Ther. 2016 Sep;358(3):580-7. doi: 10.1124/jpet.116.234948. Epub 2016 Jun 29.

19.

Fatty acid amide hydrolase inhibition for the symptomatic relief of Parkinson's disease.

Celorrio M, Fernández-Suárez D, Rojo-Bustamante E, Echeverry-Alzate V, Ramírez MJ, Hillard CJ, López-Moreno JA, Maldonado R, Oyarzábal J, Franco R, Aymerich MS.

Brain Behav Immun. 2016 Oct;57:94-105. doi: 10.1016/j.bbi.2016.06.010. Epub 2016 Jun 16.

PMID:
27318096
20.

Hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk.

Allende M, Molina E, Guruceaga E, Tamayo I, González-Porras JR, Gonzalez-López TJ, Toledo E, Rabal O, Ugarte A, Roldán V, Rivera J, Oyarzabal J, Montes R, Hermida J.

Cardiovasc Res. 2016 Jun 1;110(3):309-18. doi: 10.1093/cvr/cvw049. Epub 2016 Mar 14.

PMID:
26976620
21.

Pharmacokinetic investigation of sildenafil using positron emission tomography and determination of its effect on cerebrospinal fluid cGMP levels.

Gómez-Vallejo V, Ugarte A, García-Barroso C, Cuadrado-Tejedor M, Szczupak B, Dopeso-Reyes IG, Lanciego JL, García-Osta A, Llop J, Oyarzabal J, Franco R.

J Neurochem. 2016 Jan;136(2):403-15. doi: 10.1111/jnc.13454.

22.

Concomitant histone deacetylase and phosphodiesterase 5 inhibition synergistically prevents the disruption in synaptic plasticity and it reverses cognitive impairment in a mouse model of Alzheimer's disease.

Cuadrado-Tejedor M, Garcia-Barroso C, Sanzhez-Arias J, Mederos S, Rabal O, Ugarte A, Franco R, Pascual-Lucas M, Segura V, Perea G, Oyarzabal J, Garcia-Osta A.

Clin Epigenetics. 2015 Oct 8;7:108. doi: 10.1186/s13148-015-0142-9. eCollection 2015.

23.

Inhibition of FOXP3/NFAT Interaction Enhances T Cell Function after TCR Stimulation.

Lozano T, Villanueva L, Durántez M, Gorraiz M, Ruiz M, Belsúe V, Riezu-Boj JI, Hervás-Stubbs S, Oyarzábal J, Bandukwala H, Lourenço AR, Coffer PJ, Sarobe P, Prieto J, Casares N, Lasarte JJ.

J Immunol. 2015 Oct 1;195(7):3180-9. doi: 10.4049/jimmunol.1402997. Epub 2015 Aug 31.

24.

The CHEMDNER corpus of chemicals and drugs and its annotation principles.

Krallinger M, Rabal O, Leitner F, Vazquez M, Salgado D, Lu Z, Leaman R, Lu Y, Ji D, Lowe DM, Sayle RA, Batista-Navarro RT, Rak R, Huber T, Rocktäschel T, Matos S, Campos D, Tang B, Xu H, Munkhdalai T, Ryu KH, Ramanan SV, Nathan S, Žitnik S, Bajec M, Weber L, Irmer M, Akhondi SA, Kors JA, Xu S, An X, Sikdar UK, Ekbal A, Yoshioka M, Dieb TM, Choi M, Verspoor K, Khabsa M, Giles CL, Liu H, Ravikumar KE, Lamurias A, Couto FM, Dai HJ, Tsai RT, Ata C, Can T, Usié A, Alves R, Segura-Bedmar I, Martínez P, Oyarzabal J, Valencia A.

J Cheminform. 2015 Jan 19;7(Suppl 1 Text mining for chemistry and the CHEMDNER track):S2. doi: 10.1186/1758-2946-7-S1-S2. eCollection 2015.

25.

CHEMDNER: The drugs and chemical names extraction challenge.

Krallinger M, Leitner F, Rabal O, Vazquez M, Oyarzabal J, Valencia A.

J Cheminform. 2015 Jan 19;7(Suppl 1 Text mining for chemistry and the CHEMDNER track):S1. doi: 10.1186/1758-2946-7-S1-S1. eCollection 2015.

26.

Design, synthesis, and biological evaluation of novel matrix metalloproteinase inhibitors as potent antihemorrhagic agents: from hit identification to an optimized lead.

Orbe J, Sánchez-Arias JA, Rabal O, Rodríguez JA, Salicio A, Ugarte A, Belzunce M, Xu M, Wu W, Tan H, Ma H, Páramo JA, Oyarzabal J.

J Med Chem. 2015 Mar 12;58(5):2465-88. doi: 10.1021/jm501940y. Epub 2015 Feb 25.

PMID:
25686153
27.

Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage.

Orbe J, Rodríguez JA, Sánchez-Arias JA, Salicio A, Belzunce M, Ugarte A, Chang HC, Rabal O, Oyarzabal J, Páramo JA.

J Med Chem. 2015 Apr 9;58(7):2941-57. doi: 10.1021/jm501939z. Epub 2015 Feb 25.

PMID:
25686022
28.

Novel Scaffold FingerPrint (SFP): applications in scaffold hopping and scaffold-based selection of diverse compounds.

Rabal O, Amr FI, Oyarzabal J.

J Chem Inf Model. 2015 Jan 26;55(1):1-18. doi: 10.1021/ci500542e. Epub 2015 Jan 13.

PMID:
25558803
29.

Decreased levels of guanosine 3', 5'-monophosphate (cGMP) in cerebrospinal fluid (CSF) are associated with cognitive decline and amyloid pathology in Alzheimer's disease.

Ugarte A, Gil-Bea F, García-Barroso C, Cedazo-Minguez Á, Ramírez MJ, Franco R, García-Osta A, Oyarzabal J, Cuadrado-Tejedor M.

Neuropathol Appl Neurobiol. 2015 Jun;41(4):471-82. doi: 10.1111/nan.12203.

PMID:
25488891
30.

Phosphodiesterase inhibition in cognitive decline.

García-Barroso C, Ugarte A, Martínez M, Rico AJ, Lanciego JL, Franco R, Oyarzabal J, Cuadrado-Tejedor M, García-Osta A.

J Alzheimers Dis. 2014;42 Suppl 4:S561-73. doi: 10.3233/JAD-141341. Review.

PMID:
25125473
31.

Monoacylglycerol lipase inhibitor JZL184 is neuroprotective and alters glial cell phenotype in the chronic MPTP mouse model.

Fernández-Suárez D, Celorrio M, Riezu-Boj JI, Ugarte A, Pacheco R, González H, Oyarzabal J, Hillard CJ, Franco R, Aymerich MS.

Neurobiol Aging. 2014 Nov;35(11):2603-2616. doi: 10.1016/j.neurobiolaging.2014.05.021. Epub 2014 May 28.

PMID:
24973119
32.

Discovery of selective ligands for telomeric RNA G-quadruplexes (TERRA) through 19F-NMR based fragment screening.

Garavís M, López-Méndez B, Somoza A, Oyarzabal J, Dalvit C, Villasante A, Campos-Olivas R, González C.

ACS Chem Biol. 2014 Jul 18;9(7):1559-66. doi: 10.1021/cb500100z. Epub 2014 May 28.

PMID:
24837572
33.

Epigenetic drugs in Alzheimer's disease.

Cuadrado-Tejedor M, Oyarzabal J, Lucas MP, Franco R, García-Osta A.

Biomol Concepts. 2013 Oct;4(5):433-45. doi: 10.1515/bmc-2013-0012. Review.

PMID:
25436752
34.

Biologically relevant chemical space navigator: from patent and structure-activity relationship analysis to library acquisition and design.

Rabal O, Oyarzabal J.

J Chem Inf Model. 2012 Dec 21;52(12):3123-37. doi: 10.1021/ci3004539. Epub 2012 Dec 5.

PMID:
23176522
35.

Phosphodiesterases as therapeutic targets for Alzheimer's disease.

García-Osta A, Cuadrado-Tejedor M, García-Barroso C, Oyarzábal J, Franco R.

ACS Chem Neurosci. 2012 Nov 21;3(11):832-44. doi: 10.1021/cn3000907. Epub 2012 Oct 1. Review.

36.

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.

37.

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
38.

Tadalafil crosses the blood-brain barrier and reverses cognitive dysfunction in a mouse model of AD.

García-Barroso C, Ricobaraza A, Pascual-Lucas M, Unceta N, Rico AJ, Goicolea MA, Sallés J, Lanciego JL, Oyarzabal J, Franco R, Cuadrado-Tejedor M, García-Osta A.

Neuropharmacology. 2013 Jan;64:114-23. doi: 10.1016/j.neuropharm.2012.06.052. Epub 2012 Jul 7.

PMID:
22776546
39.

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
40.

Using novel descriptor accounting for ligand-receptor interactions to define and visually explore biologically relevant chemical space.

Rabal O, Oyarzabal J.

J Chem Inf Model. 2012 May 25;52(5):1086-102. doi: 10.1021/ci200627v. Epub 2012 Apr 19.

PMID:
22486368
41.

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
42.

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.

Pastor J, Oyarzabal J, Saluste G, Alvarez RM, Rivero V, Ramos F, Cendón E, Blanco-Aparicio C, Ajenjo N, Cebriá A, Albarrán MI, Cebrián D, Corrionero A, Fominaya J, Montoya G, Mazzorana M.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1591-7. doi: 10.1016/j.bmcl.2011.12.130. Epub 2012 Jan 5.

PMID:
22266039
43.

Defining the mechanism of action of 4-phenylbutyrate to develop a small-molecule-based therapy for Alzheimer's disease.

Cuadrado-Tejedor M, García-Osta A, Ricobaraza A, Oyarzabal J, Franco R.

Curr Med Chem. 2011;18(36):5545-53. Review.

PMID:
22172064
44.

Conformational selection versus induced fit in kinases: the case of PI3K-γ.

D'Abramo M, Rabal O, Oyarzabal J, Gervasio FL.

Angew Chem Int Ed Engl. 2012 Jan 16;51(3):642-6. doi: 10.1002/anie.201103264. Epub 2011 Dec 1. No abstract available.

PMID:
22135005
45.

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.

46.

Computational medicinal chemistry in fragment-based drug discovery: what, how and when.

Rabal O, Urbano-Cuadrado M, Oyarzabal J.

Future Med Chem. 2011 Jan;3(1):95-134. doi: 10.4155/fmc.10.277. Review.

PMID:
21428828
47.

Centralizing discovery information: from logistics to knowledge at a public organization.

Urbano-Cuadrado M, Rabal O, Oyarzabal J.

Comb Chem High Throughput Screen. 2011 Jul;14(6):429-49.

PMID:
21143181
48.

Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Cid JM, Duvey G, Cluzeau P, Nhem V, Macary K, Raux A, Poirier N, Muller J, Boléa C, Finn T, Poli S, Epping-Jordan M, Chamelot E, Derouet F, Girard F, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, Lavreysen H, Linares ML, Oehlrich D, Oyarzábal J, Tresadern G, Trabanco AA, Andrés JI, Le Poul E, Imogai H, Lutjens R, Rocher JP.

ACS Chem Neurosci. 2010 Dec 15;1(12):788-95. doi: 10.1021/cn1000638. Epub 2010 Aug 23.

49.

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
50.

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

Supplemental Content

Loading ...
Support Center