epitron

Publications

2009 2008 2007 2006 2005 2004 2003 2002 2001 2000

   2009

Modulating Retinoid X Receptor with a Series of (E)-3-[4-Hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic Acids and Their 4-Alkoxy Isomers.
Efrén Pérez Santín, Pierre Germain, Fabien Quillard, Harshal Khanwalkar, Fátima Rodríguez-Barrios, Hinrich Gronemeyer, Ángel R. de Lera and William Bourguet
J. Med. Chem. 2009, 52(10), 3150–3158.

Retinoid Receptor Subtype-Selective Modulators Through Synthetic Modifications of RARγ Agonists.
Susana Álvarez, Rosana Álvarez, Harshal Khanwalkar, Pierre Germain, Géraldine Lemaire, Fátima Rodríguez-Barrios, Hinrich Gronemeyer, Ángel R. de Lera
Bioorganic & Medicinal Chemistry, 2009, 17(13), 4345-4359.

Highly Potent Naphthofuran-Based Retinoic Acid Receptor Agonists
Efrén Pérez Santín, Harshal Khanwalkar, Johannes Voegel, Pascal Collette, Pascale Mauvais, Hinrich Gronemeyer, Ángel R. de Lera
ChemMedChem, 2009, 4(5), 780-791.

Pyrazine Arotinoids with Inverse Agonist Activities on the Retinoid and Rexinoid Receptors
José García, Harshal Khanwalkar, Raquel Pereira, Cathie Erb, Johannes J. Voegel, Pascal Collette, Pascale Mauvais, William Bourguet, Hinrich Gronemeyer, Ángel R. de Lera.
ChemBioChem, 2009, 10(7), 1252-1259.

Mechanism of the Gold-Catalyzed Rearrangement of (3-Acyloxyprop-1-ynyl)oxiranes: A Dual Role of the Catalyst
Adán González Pérez, Carlos Silva López, José Marco-Contelles, Olalla Nieto Faza, Elena Soriano, and Angel R. de Lera
J. Org. Chem., 2009, 74(9), 2982–2991.

Regio-, Peri-, and Torquoselectivity in Hydroxy Heptatrienyl Cation Electrocyclizations: The Iso/Homo-Nazarov Reaction
Olalla Nieto Faza, Carlos Silva López, Rosana álvarez, and ángel R. de Lera
Chem. Eur. J. 2009, 15(8), 1944 - 1956

The C-C Reductive Elimination in Palladium Complexes, and the Role of Coupling Additives. A DFT Study Supported by Experiment.
Martín Pérez-Rodríguez, Ataualpa A. C. Braga, Max Garcia-Melchor, Mónica H. Pérez-Temprano, Juan A. Casares,Gregori Ujaque, Angel R. de Lera,Rosana álvarez, Feliu Maseras and Pablo Espinet
J. Am. Chem. Soc. 2009, 131(10), 3650-3657

Palladium-Catalyzed Sequential Oxidative Cyclization/Coupling of 2-Alkynylphenols and Alkenes: A Direct Entry into 3-Alkenylbenzofurans"
Martínez, Claudio; Aurrecoechea, José; álvarez, Rosana.
Org Lett 2009, 11 (5), pp 1083–1086

Aldo-keto reductases from the AKR1B subfamily: Retinoid specificity and control of cellular retinoic acid levels.
Xavier Ruiz; Oriol Gallego.; Albert Ardèvol.; Armando Moro.; Marta Domínguez.; Susana Alvarez.; Rosana Alvarez.; Angel R de Lera.; Carme Rovira.; Ignacio Fita.; Xavier Parés.; Jaume Farrés
Chemico-Biological Interactions 2009, 178(1-3) 171–177

Structural Coupling of 11-cis-7-Methyl-retinal and Amino Acids at the Ligand Binding Pocket of Rhodopsin.
Mònica Aguilà, Darwin Toledo, Margarita Morillo, Marta Dominguez, Belén Vaz, Rosana Alvarez, Angel R. de Lera, Pere Garriga.
Photochemistry and Photobiology 2009, 85(2) March/April, 485-493

Highly Twisted Adamantyl Arotinoids: Synthesis, Antiproliferative Effects and RXR Transactivation Profiles
Santiago Pérez-Rodríguez, Maria A. Ortiz, Raquel Pereira, Fátima Rodríguez-Barrios, Angel R. de Lera and F. Javier Piedrafita
European Journal of Medicinal Chemistry, 2009, in press, online 1-13

   2008

NOVEL DERIVATIVES OF PSAMMAPLIN A, A METHOD FOR THEIR SYNTHESIS AND THEIR USE FOR THE PREVENTION OR TREATMENT OF CANCER
Gronemeyer, Hinrich; Altucci, Lucia; De Lera, Angel; Stunnenberg, Hendrik Gerard.
PCT/IB2008/001887 (pub. 2008/10/23), WO2008125988-56pp .

Derivatives of psammaplin A, a method for their synthesis and their use for the prevention or treatment of cancer
Gronemeyer, Hinrich; De Lera, Angel; Altucci, Lucia.
Eur. Pat. Appl. 07290253.9 (published 2008/09/03, Bulletin 2008/36), EP1964835A1-32pp .

Expedient Total Syntheses of WIN 64745 and WIN 64821
Carlos Pérez-Balado and Angel R. de Lera
Org Lett. 2008 Sep 4;10(17):3701-4.

New retinoid chemotypes: 9-cis-Retinoic acid analogs with hydrophobic rings derived from terpenes as selective RAR agonists.
Susana Álvarez, Yolanda Pazos-Randulfe, Harshal Khanwalkar, Pierre Germain, Rosana Álvarez, Hinrich Gronemeyer, and ángel R. de Lera.
Bioorg Med Chem. 2008 Nov 15;16(22):9719-28.

Stereoselective Stille Coupling of Enantiopure Haloallenes and Alkenylstannanes for the Synthesis of Allenyl Carotenoids. Experimental and Computational Studies
BelénVaz, Raquél Pereira, Martín Pérez, Rosana Álvarez, Angel R de Lera.
J. Org. Chem., 2008, 73(17), 6534-6541.

Nuclear receptor ligand binding domains: reduction of helix H12 dynamics to favor crystallization
Virginie Nahoum, Alexandra Lipski, Fabien Quillard, Jean-François Guichou, Yvan Boublik, Efrén Pérez, Pierre Germain, Angel R. de Lera, and William Bourguet
Acta Cryst. Sect. F , 2008, F64, 614-616.

Inhibition of IκB Kinaseβ and Anticancer Activities of Novel Chalcone Adamantyl Arotinoids
Paula Lorenzo, Rosana Alvarez, Maria A. Ortiz, Susana Alvarez, F. Javier Piedrafita and Angel R. de Lera
J. Med. Chem., 51 (17), 5431–5440, 2008.

The Associative Transmetalation in the Stille Cross-Coupling Reaction to Form Dienes: Theoretical Insights into the Open Pathway.
Rosana Álvarez, Martín Pérez, Olalla Nieto Faza and Angel R. de Lera.
Organometallics, 27 (14), 3378–3389, 2008.

Synthesis of Novel Benzamides Related to Anacardic Acid and Their Histone Acetyltransferase (HAT) Inhibitory Activities
José A. Souto, Mariarosaria Conte, Rosana Álvarez, Angela Nebbioso, Vincenzo Carafa, Lucia Altucci, and Angel R. de Lera
ChemMedChem, Volume 3 Issue 9, Pages 1435 - 1442, 2008.

Isomer-specific effects of conjugated linoleic acid on gene expression in RAW 264.7
Yunkyoung Lee, Jerry T. Thompson, Angel R. de Lera and John P. Vanden Heuvel
J. Nutrit. Biochem., 2008, Available online 6 November 2008, xx (2008) xxx–xxx

Photochromic polymer films based on a 14-F bacteriorhodopsin derivative
Anna Druzhko , Rosana Álvarez and Angel R. de Lera
J. Biomater. Sci. Polymer Edn, Vol. 19, No. 12, pp. 1585-1595 (2008)

Retinoic acid inhibits Human Herpesvirus 8 replication.
Elisabetta Caselli, Galvan Monica, Fabio Santoni, Susana Alvarez, Angel R. de Lera, Diana Ivanova, Hinrich Gronemeyer, Arnaldo Caruso, Massimo Guidoboni, Enzo Cassai, Riccardo Dolcetti, and Dario Di Luca
Antiviral Therapy 2008, 13(2): 199-209

Stereospecificity of Retinol Saturase: Absolute Configuration, Synthesis and Biological Evaluation of Dihydroretinoids.
Alexander R. Moise, Marta Domínguez, Susana Alvarez, Rosana Alvarez, Michael Schupp, Ana G. Cristancho, Philip D. Kiser, Angel R. de Lera, Mitchell A. Lazar, Krzysztof Palczewski
J. Am. Chem. Soc., 2008, 130(4), 1154-1155.

Characterization of the Switch in the Mechanism of an Intramolecular Diels-Alder Reaction.
Silva Lopez, Carlos; Nieto Faza, Olalla; de Lera, Angel R..
Journal of Organic Chemistry (2008), 73(2), 467-473.

Mechanistic Insights into the Stereocontrolled Synthesis of Hexahydropyrrolo[2,3-b]indoles by Electrophilic Activation of Tryptophan Derivatives.
Silva Lopez, Carlos; Perez-Balado, Carlos; Rodriguez-Grana, Paula; de Lera, Angel R..
Organic Letters, 10 (1), 77 -80, 2008.

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   2007

Structural basis for the high all-trans retinaldehydr reductase activity of the tumor marker AKR1B10
Oriol Gallego, F. Xavier Ruiz, Albert Ardèvol, Marta Domínguez, Rosana Alvarez, Angel R. de Lera, Carme Rovira, Jaume Farrés, Ignacio Fita and Xavier Parés
Proceedings of the National Academy of Sciences of the United States of America, (2007), 104(52), 20764

Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function.
Nahoum, Virginie; Perez, Efren; Germain, Pierre; Rodriguez-Barrios, Fatima; Manzo, Fabio; Kammerer, Sabrina; Lemaire, Geraldine; Hirsch, Oliver; Royer, Catherine A.; Gronemeyer, Hinrich; de Lera, Angel R.; Bourguet, William.
Proceedings of the National Academy of Sciences of the United States of America (2007), 104(44), 17323-17328.

Deuterium exchange and mass spectrometry reveal the interaction differences of two synthetic modulators of RXRa LBD.
Yan, Xuguang; Perez, Efren; Leid, Mark; Schimerlik, Michael I.; De Lera, Angel R.; Deinzer, Max L.
Protein Science (2007), 16(11), 2491-2501.

Rapid, nongenomic actions of retinoic acid on phosphatidylinositol-3-kinase signaling pathway mediated by the retinoic acid receptor.
Masia, Susana; Alvarez, Susana; de Lera, Angel R.; Barettino, Domingo.
Molecular Endocrinology (2007), 21(10), 2391-2402.

RAR and RXR modulation in cancer and metabolic disease.
Altucci, Lucia; Leibowitz, Mark D.; Ogilvie, Kathleen M.; de Lera, Angel R.; Gronemeyer, Hinrich.
Nature Reviews Drug Discovery (2007), 6(10), 793-810.

Design of selective nuclear receptor modulators: RAR and RXR as a case study.
de Lera, Angel R.; Bourguet, William; Altucci, Lucia; Gronemeyer, Hinrich.
Nature Reviews Drug Discovery (2007), 6(10), 811-820.

Feijoa sellowiana derived natural Flavone exerts anti-cancer action displaying HDAC inhibitory activities.
Bontempo, Paola; Mita, Luigi; Miceli, Marco; Doto, Antonella; Nebbioso, Angela; De Bellis, Floriana; Conte, Mariarosaria; Minichiello, Annunziata; Manzo, Fabio; Carafa, Vincenzo; Basile, Adriana; Rigano, Daniela; Sorbo, Sergio; Castaldo Cobianchi, Rosa; Schiavone, Ettore Mariano; Ferrara, Felicetto; De Simone, Mariacarla; Vietri, MariaTeresa; Cioffi, Michele; Sica, Vincenzo; Bresciani, Francesco; de Lera, Angel R.; Altucci, Lucia; Molinari, Anna Maria.
International Journal of Biochemistry & Cell Biology (2007), 39(10), 1902-1914.

Structure, function and modulation of retinoic acid receptor beta, a tumor suppressor.
Alvarez, Susana; Germain, Pierre; Alvarez, Rosana; Rodriguez-Barrios, Fatima; Gronemeyer, Hinrich; De Lera, Angel R..
International Journal of Biochemistry & Cell Biology (2007), 39(7-8), 1406-1415.

Electrocyclic ring opening of cis-bicyclo[m.n.0]alkenes: the anti-Woodward-Hoffmann quest.
Lopez, Carlo Silva; Faza, Olalla Nieto; de Lera, Angel R..
Chemistry--A European Journal (2007), 13(17), 5009-5017.

A density functional theory study of the stille cross-coupling via associative transmetalation. The role of ligands and coordinating solvents.
Alvarez, Rosana; Faza, Olalla Nieto; de Lera, Angel R.; Cardenas, Diego J.
Advanced Synthesis & Catalysis (2007), 349(6), 887-906.

Pseudopericyclic design drives antara-antara [1,5] methylene sigmatropic shifts from a stepwise to a concerted mechanism.
Lopez, Carlos Silva; Faza, Olalla Nieto; Souto, Jose A.; Alvarez, Rosana; De Lera, Angel R..
Journal of Computational Chemistry (2007), 28(8), 1411-1416.

Bimetallic Intermediates in the Formation of Nucleophilic Allenylzincs from Allenylpalladiums: A DFT Study.
Alvarez, Rosana; De Lera, Angel R.; Aurrecoechea, Jose M.; Durana, Aritz.
Organometallics (2007), 26(11), 2799-2802.

Bispyridinium Dienes: Histone Deacetylase Inhibitors with Selective Activities.
Perez-Balado, Carlos; Nebbioso, Angela; Rodriguez-Grana, Paula; Minichiello, Annunziata; Miceli, Marco; Altucci, Lucia; de Lera, Angel R..
Journal of Medicinal Chemistry (2007), 50(10), 2497-2505.

Cyclopent-2-en-1-one derivatives as PPAR modulators, their preparation, pharmaceutical and cosmetic compositions, and uses thereof.
De Lera, Angel Rodriguez; Otero Cabredo, Maria Paz.
PCT Int. Appl. (2007), 63pp. WO2007029121 A2 20070315

Sulfoxide-Induced Stereoselection in [1,5]-Sigmatropic Hydrogen Shifts of Vinylallenes. A Computational Study.
Faza, Olalla Nieto; Lopez, Carlos Silva; de Lera, Angel R..
Journal of Organic Chemistry (2007), 72(7), 2617-2624.

Total synthesis of peridinin and related C37-norcarotenoid butenolides.
Vaz, Belen; Dominguez, Marta; Alvarez, Rosana; de Lera, Angel R..
Chemistry--A European Journal (2007), 13(4), 1273-1290.

Preparation of cyclopent-2-en-1-one derivatives as PPAR modulators and their use in cosmetic and pharmaceutical compositions.
De Lera, Angel Rodriguez; Otero, Cabredo Maria Paz.
Fr. Demande (2007), 56pp. FR2888846 A1 20070126

Specificity of Zebrafish Retinol Saturase: Formation of All-trans-13,14-dihydroretinol and All-trans-7,8-dihydroretinol.
Moise, Alexander R.; Isken, Andrea; Dominguez, Marta; De Lera, Angel R.; Von Lintig, Johannes; Palczewski, Krzysztof.
Biochemistry (2007), 46(7), 1811-1820.

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   2006

International union of pharmacology. LXIII. Retinoid X receptors.
Germain, Pierre; Chambon, Pierre; Eichele, Gregor; Evans, Ronald M.; Lazar, Mitchell A.; Leid, Mark; De Lera, Angel R.; Lotan, Reuben; Mangelsdorf, David J.; Gronemeyer, Hinrich.
Pharmacological Reviews (2006), 58(4), 750-772.

International union of pharmacology. LX. Retinoic acid receptors.
Germain, Pierre; Chambon, Pierre; Eichele, Gregor; Evans, Ronald M.; Lazar, Mitchell A.; Leid, Mark; De Lera, Angel R.; Lotan, Reuben; Mangelsdorf, David J.; Gronemeyer, Hinrich.
Pharmacological Reviews (2006), 58(4), 712-725.

Insights into the mechanism of the site-selective sequential palladium-catalyzed cross-coupling reactions of dibromothiophenes/dibromothiazoles and arylboronic acids. Synthesis of PPARb /d agonists.
Pereira, Raquel; Furst, Audrey; Iglesias, Beatriz; Germain, Pierre; Gronemeyer, Hinrich; de Lera, Angel R..
Organic & Biomolecular Chemistry (2006), 4(24), 4514-4525.

The role of the 11-cis-retinal ring methyl substituents in visual pigment formation.
Dominguez, Marta; Alvarez, Rosana; Perez, Martin; Palczewski, Krzysztof; de Lera, Angel R..
ChemBioChem (2006), 7(11), 1815-1825.

A methyl group at C7 of 11-cis-retinal allows chromophore formation but affects rhodopsin activation.
Bosch, Laia; Cordomi, Arnau; Dominguez, Marta; Toledo, Darwin; Morillo, Margarita; Perez, Juan J.; Alvarez, Rosana; de Lera, Angel R.; Garriga, Pere.
Vision Research (2006), 46(27), 4472-4481.

Activity of alcohol dehydrogenase with 11-cis-retinoids and distribution of ADH4 in ocular tissues.
Porte, Sergio; Martras, Silvia; Martinez, Susana E.; Alvarez, Rosana; Gallego, Oriol; Dominguez, Marta; Duester, Gregg; de Lera, Angel R.; Farres, Jaume; Pares, Xavier.
Enzymology and Molecular Biology of Carbonyl Metabolism--12, [International Meeting], 12th, Burlington, VT, United States, July 6-11, 2004 (2006), Meeting Date 2004, 200-207.

The Stille Reaction in the Synthesis of the C37-Norcarotenoid Butenolide Pyrrhoxanthin. Scope and Limitations.
Vaz, Belen; Dominguez, Marta; Alvarez, Rosana; de Lera, Angel R..
Journal of Organic Chemistry (2006), 71(16), 5914-5920.

Cycloisomerization of Activated (2E,4Z)-Heptatrienoate and Its Relevance to Crispatene (Bio)synthesis. A Case of Concerted and Stepwise Uncertainty.
Lopez, Carlos Silva; Faza, Olalla Nieto; Alvarez, Rosana; de Lera, Angel R..
Journal of Organic Chemistry (2006), 71(12), 4497-4501.

Computational Study and Analysis of the Kinetic Isotope Effects of the Rearrangement of cis-Bicyclo[4.2.0]oct-7-ene to cis,cis-Cycloocta-1,3-diene.
Silva Lopez, Carlos; Nieto Faza, Olalla; De Lera, Angel R..
Organic Letters (2006), 8(10), 2055-2058.

Natural and synthetic retinoids: structural bases and biological effects of potential clinical relevance for the prevention and treatment of infection-driven tumors.
Dolcetti, Riccardo; Di Luca, Dario; de Lera, Angel R..
Anti-Infective Agents in Medicinal Chemistry (2006), 5(1), 85-103.

Mechanism of the Gold(I)-Catalyzed Rautenstrauch Rearrangement: A Center-to-Helix-to-Center Chirality Transfer.
Nieto Faza, Olalla; Silva Lopez, Carlos; Alvarez, Rosana; De Lera, Angel R..
Journal of the American Chemical Society (2006), 128(7), 2434-2437.

Computation of vertical excitation energies of retinal and analogs: Scope and limitations.
Lopez, Carlos Silva; Faza, Olalla Nieto; Estevez, Susana Lopez; De Lera, Angel R..
Journal of Computational Chemistry (2006), 27(1), 116-123.

Synthesis of enantiopure C3- and C4-hydroxyretinals and their enzymatic reduction by ADH8 from Xenopus laevis.
Dominguez, Marta; Alvarez, Rosana; Borras, Emma; Farres, Jaume; Pares, Xavier; De Lera, Angel R..
Organic & Biomolecular Chemistry (2006), 4(1), 155-164.

Computational Characterization of a Complete Palladium-Catalyzed Cross-Coupling Process: The Associative Transmetalation in the Stille Reaction.
Alvarez, Rosana; Nieto Faza, Olalla; Silva Lopez, Carlos; de Lera, Angel R..
Organic Letters (2006), 8(1), 35-38.

Synthesis of the PPARb /d -selective agonist GW501516 and C4-thiazole-substituted analogs.
Pereira, Raquel; Gaudon, Claudine; Iglesias, Beatriz; Germain, Pierre; Gronemeyer, Hinrich; de Lera, Angel R..
Bioorganic & Medicinal Chemistry Letters (2006), 16(1), 49-54.


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