Fármacos epigenéticos dirigidos a HDAC, HAT, PRMT, DNMT
Análisis computacional
– Química y Biología de retinoides – Síntesis estereocontroladas de carotenoides y polienos relacionados – Diseño y síntesis de moduladores epigenéticos base de productos naturales – Análisis computacional de procesos catalíticos organometálicos; reacciones concertadas pericíclicas y Otros
2017
2018
2019
2020
Artículos Científicos
Alvarez R, de Lera AR. Natural polyenic macrolactams and polycyclic derivatives generated by transannular pericyclic reactions: optimized biogenesis challenging chemical synthesis. Nat Prod Rep. 2021;38(6):1136–220. PMID: 33283831. DOI: 10.1039/d0np00050g. http://www.ncbi.nlm.nih.gov/pubmed/33283831 +Pubmed+DOI
Areal A, Domínguez M, Vendrig P, Alvarez S, Álvarez R, de Lera ÁR. Total Synthesis of Homo- and Heterodimeric Bispyrrolidinoindoline Dioxopiperazine Natural Products. J Nat Prod. 2021;84(6):1725–37. PMID: 34019401. DOI: 10.1021/acs.jnatprod.0c01273. http://www.ncbi.nlm.nih.gov/pubmed/34019401 +Pubmed+DOI
Böhm V, Lietz G, Olmedilla-Alonso B, Phelan D, Reboul E, Bánati D, Borel P, Corte-Real J, de Lera AR, Desmarchelier C, Dulinska-Litewka J, Landrier J-F, Milisav I, Nolan J, Porrini M, Riso P, Roob JM, Valanou E, Wawrzyniak A, Winklhofer-Roob BM, Rühl R, Bohn T. From carotenoid intake to carotenoid blood and tissue concentrations – implications for dietary intake recommendations. Nutr Rev. 2021;79(5):544–73. PMID: 32766681. DOI: 10.1093/nutrit/nuaa008. http://www.ncbi.nlm.nih.gov/pubmed/32766681 +Pubmed+DOI
Kr??el W, Rivas A, Szklenar M, Ciancia M, Alvarez R, de Lera AR, Rühl R. Vitamin A5/X, a New Food to Lipid Hormone Concept for a Nutritional Ligand to Control RXR-Mediated Signaling. Nutrients. 2021 Mar;13(3) PMID: 33809241. DOI: 10.3390/nu13030925. http://www.ncbi.nlm.nih.gov/pubmed/33809241 +Pubmed+DOI
Krzy?osiak A, Podle?ny-Drabiniok A, Vaz B, Alvarez R, Rühl R, de Lera AR, Kr??el W. Vitamin A5/X controls stress-adaptation and prevents depressive-like behaviors in a mouse model of chronic stress. Neurobiol Stress. 2021 Nov;15:100375. PMID: 34401411. DOI: 10.1016/j.ynstr.2021.100375. http://www.ncbi.nlm.nih.gov/pubmed/34401411 +Pubmed+DOI
Lucas R, Mihály J, Gericke J, de Lera AR, Alvarez S, Veleczki Z, Tör?csik D, Rühl R. Topical Vitamin D Receptor Antagonist/Partial-Agonist Treatment Induces Epidermal Hyperproliferation via RAR? Signaling Pathways. Dermatology. 2021;237(2):197–203. PMID: 32866959. DOI: 10.1159/000508334. http://www.ncbi.nlm.nih.gov/pubmed/32866959 +Pubmed+DOI
Vaz B, Martínez C, Cruz F, Denis JG, de Lera ÁR, Aurrecoechea JM, Álvarez R. Palladium-Catalyzed Aminocyclization-Coupling Cascades: Preparation of Dehydrotryptophan Derivatives and Computational Study. J Org Chem. 2021 Jul;86(13):8766–85. PMID: 34125552. DOI: 10.1021/acs.joc.1c00636. http://www.ncbi.nlm.nih.gov/pubmed/34125552 +Pubmed+DOI
Artículos Científicos
Cala L, Villar P, de Lera ÁR, Fañanás FJ, Álvarez R, Rodríguez F. Multicomponent and multicatalytic asymmetric synthesis of furo[2,3-b]pyrrole derivatives: further insights into the mode of action of chiral phosphoric acid catalysts. Chem Sci. 2020 Aug;11(34):9181–90. PMID: 34094194. DOI: 10.1039/d0sc03342a. http://www.ncbi.nlm.nih.gov/pubmed/34094194 +Pubmed+DOI
Catalán M, Castro-Castillo V, Gajardo-de la Fuente J, Aguilera J, Ferreira J, Ramires-Fernandez R, Olmedo I, Molina-Berríos A, Palominos C, Valencia M, Domínguez M, Souto JA, Jara JA. Continuous flow synthesis of lipophilic cations derived from benzoic acid as new cytotoxic chemical entities in human head and neck carcinoma cell lines. RSC Med Chem. 2020 Oct;11(10):1210–25. PMID: 33479625. DOI: 10.1039/d0md00153h. http://www.ncbi.nlm.nih.gov/pubmed/33479625 +Pubmed+DOI
de Lera AR, Ganesan A. Two-hit wonders: The expanding universe of multitargeting epigenetic agents. Curr Opin Chem Biol. 2020;57:135–54. PMID: 32784072. DOI: 10.1016/j.cbpa.2020.05.009. http://www.ncbi.nlm.nih.gov/pubmed/32784072 +Pubmed+DOI
García P, Lorenzo P, de Lera AR. Natural ligands of RXR receptors. Methods Enzymol. 2020;637:209–34. PMID: 32359646. DOI: 10.1016/bs.mie.2020.02.006. http://www.ncbi.nlm.nih.gov/pubmed/32359646 +Pubmed+DOI
Gavalás-Olea A, Sanz N, Riobó P, Garrido JL, Vaz B. Enzymatic synthesis and characterization of chlorophyllide derivatives as possible internal standards for pigment chromatographic analysis. Algal Res. 2020 Mar;46:101688. DOI: 10.1016/j.algal.2019.101688. https://doi.org/10.1016/j.algal.2019.101688 +DOI
Rivas A, Areal A, Mora P, Álvarez R, de Lera AR. Synthesis of Symmetrical and Nonsymmetrical Polyenes by Iterative and Bidirectional Palladium-Catalyzed Cross-Coupling Reactions. Chemistry. 2020 Oct;26(60):13543–67. PMID: 32267574. DOI: 10.1002/chem.202000624. http://www.ncbi.nlm.nih.gov/pubmed/32267574 +Pubmed+DOI
Rivas A, Pequerul R, Barracco V, Domínguez M, López S, Jiménez R, Parés X, Alvarez R, Farrés J, de Lera AR. Synthesis of C11-to-C14 methyl-shifted all-trans-retinal analogues and their activities on human aldo-keto reductases. Org Biomol Chem. 2020;18(25):4788–801. PMID: 32530010. DOI: 10.1039/d0ob01084g. http://www.ncbi.nlm.nih.gov/pubmed/32530010 +Pubmed+DOI
Souto JA, Sarno F, Nebbioso A, Papulino C, Álvarez R, Lombino J, Perricone U, Padova A, Altucci L, de Lera ÁR. A New Family of Jumonji C Domain-Containing KDM Inhibitors Inspired by Natural Product Purpurogallin. Front Chem. 2020;8:312. PMID: 32523934. DOI: 10.3389/fchem.2020.00312. http://www.ncbi.nlm.nih.gov/pubmed/32523934 +Pubmed+DOI
Villar P, Pérez-Temprano MH, Casares JA, Álvarez R, Espinet P. Experimental and DFT Study of the [AuAr(AsPh 3 )]-Catalyzed cis/trans Isomerization of [PdAr 2 (AsPh 3 ) 2 ] (Ar = C 6 F 5 or C 6 Cl 2 F 3 ): Alternative Mechanisms and Its Switch upon Pt for Pd Substitution. Organometallics. 2020 Jun;39(12):2295–303. DOI: 10.1021/acs.organomet.0c00245. https://doi.org/10.1021/acs.organomet.0c00245 +DOI
Wang JY, Jamil M, Lin P-Y, Ota T, Fiorilli V, Novero M, Zarban RA, Kountche BA, Takahashi I, Martínez C, Lanfranco L, Bonfante P, de Lera AR, Asami T, Al-Babili S. Efficient Mimics for Elucidating Zaxinone Biology and Promoting Agricultural Applications. Mol Plant. 2020;13(11):1654–61. PMID: 32835886. DOI: 10.1016/j.molp.2020.08.009. http://www.ncbi.nlm.nih.gov/pubmed/32835886 +Pubmed+DOI
Capítulos de libro
García P, Lorenzo P, de Lera AR. Natural ligands of RXR receptors. Methods Enzymol. 2020;637:209–34. PMID: 32359646. DOI: 10.1016/bs.mie.2020.02.006. http://www.ncbi.nlm.nih.gov/pubmed/32359646 +DOI
Artículos Científicos
Aydemir G, Domínguez M, de Lera AR, Mihaly J, Tör?csik D, Rühl R. Apo-14´-Carotenoic Acid Is a Novel Endogenous and Bioactive Apo-Carotenoid. Nutrients. 2019 Sep;11(9):2084. DOI: 10.3390/nu11092084. https://www.mdpi.com/2072-6643/11/9/2084 +DOI
González-Pérez AB, Villar P, de Lera AR. A Computational Study of Model Parent Systems and Reported Aza-(Iso)Nazarov/Aza-(Iso)Piancatelli Electrocyclic Reactions. European J Org Chem. 2019 Apr;2019(14):2539–51. DOI: 10.1002/ejoc.201900103. http://doi.wiley.com/10.1002/ejoc.201900103 +DOI
Kr??el W, Rühl R, de Lera AR. Alternative retinoid X receptor (RXR) ligands. Mol Cell Endocrinol. 2019 Jul;491:110436. PMID: 31026478. DOI: 10.1016/j.mce.2019.04.016. http://www.ncbi.nlm.nih.gov/pubmed/31026478 +Pubmed+DOI
Rivas A, Alvarez R, de Lera AR. Stereocontrolled synthesis and configurational assignment of (R)-all-trans-11,12-dihydro-3-hydroxyretinol. Tetrahedron Lett. 2019 Aug;60(35):150972. DOI: 10.1016/j.tetlet.2019.150972. https://linkinghub.elsevier.com/retrieve/pii/S0040403919307233 +DOI
Rivas A, Pérez-Revenga V, Alvarez R, de Lera AR. Bidirectional Hiyama-Denmark Cross-Coupling Reactions of Bissilyldeca-1,3,5,7,9-pentaenes for the Synthesis of Symmetrical and Non-Symmetrical Carotenoids. Chemistry. 2019 Nov;25(63):14399–407. PMID: 31456273. DOI: 10.1002/chem.201903080. https://onlinelibrary.wiley.com/doi/abs/10.1002/chem.201903080 +Pubmed+DOI
Sarceda S, Souto JA, Otero D, de Lera ÁR, Domínguez M, Álvarez R. Improved synthesis of key fragments for the preparation of natural product incednine. Tetrahedron. 2019 Oct;75(43):130604. DOI: 10.1016/j.tet.2019.130604. https://doi.org/10.1016/j.tet.2019.130604 +DOI
Villar P, González-Pérez AB, de Lera AR. Deciphering the Origin of Enantioselectivity on the Cis-Cyclopropanation of Styrene with Enantiopure Di-chloro,Di-gold(I)-SEGPHOS Carbenoids Generated from Propargylic Esters. J Org Chem. 2019 Jun;84(12):7664–73. PMID: 31095390. DOI: 10.1021/acs.joc.9b00250. http://www.ncbi.nlm.nih.gov/pubmed/31095390 +Pubmed+DOI
Villar P, Guillade L, González-Pérez AB, de Lera AR. Computational studies on the formation of aza-oxypentadienyl intermediates from alkylidene oxaziridines and keteneimine oxides and their conversion to 1,5-dihydropyrrolones. Int J Quantum Chem. 2019 Feb;119(4):e25796. DOI: 10.1002/qua.25796. http://doi.wiley.com/10.1002/qua.25796 +DOI
Capítulos de libro
Martínez C, Souto JA, de Lera AR. Ligand Design for Modulation of RXR Functions. In: Ray S (ed.). RETINOID AND REXINOID SIGNALING: METHODS AND PROTOCOLS. NJ, USA: HUMANA PRESS INC; 2019. p. 51–72. ISBN: 978-1-4939-9585-1; 978-1-4939-9584-4. http://link.springer.com/10.1007/978-1-4939-9585-1_4 +DOI
Artículos Científicos
Cruz F, Vaz B, Vilar U, Ortega A, Madich Y, Álvarez R, Aurrecoechea JM. Regioselective Palladium-Catalyzed Heterocyclization–Sonogashira Coupling Cascades from 2-Alkynylbenzamides and Terminal Alkynes: Experimental and DFT Studies. Organometallics. 2018 Nov;37(21):3813–26. DOI: 10.1021/acs.organomet.8b00519. http://pubs.acs.org/doi/10.1021/acs.organomet.8b00519 +DOI
Domínguez M, Pequerul R, Alvarez R, Giménez-Dejoz J, Birta E, Porté S, Rühl R, Parés X, Farrés J, de Lera AR. Synthesis of apocarotenoids by acyclic cross metathesis and characterization as substrates for human retinaldehyde dehydrogenases. Tetrahedron. 2018 May;74(21):2567–74. DOI: 10.1016/j.tet.2018.03.050. https://linkinghub.elsevier.com/retrieve/pii/S0040402018303235 +DOI
Franci G, Folliero V, Cammarota M, Zannella C, Sarno F, Schiraldi C, de Lera AR, Altucci L, Galdiero M. Epigenetic modulator UVI5008 inhibits MRSA by interfering with bacterial gyrase. Sci Rep. Springer US; 2018 Sep;8(1):13117. PMID: 30177735. DOI: 10.1038/s41598-018-31135-9. http://dx.doi.org/10.1038/s41598-018-31135-9 +Pubmed+DOI
Gavalas-Olea A, Luis Garrido J, Riobo P, Alvarez S, Vaz B. Mass Spectrometry of Algal Chlorophyll c Compounds. Curr Org Chem. 2018 May;22(9):836–41. DOI: 10.2174/1385272821666170919155604. http://www.eurekaselect.com/155707/article +DOI
Guillade L, Sarno F, Tarhonskaya H, Nebbioso A, Alvarez S, Kawamura A, Schofield CJ, Altucci L, de Lera ÁR. Synthesis and Biological Evaluation of Tripartin, a Putative KDM4 Natural Product Inhibitor, and 1-Dichloromethylinden-1-ol Analogues. ChemMedChem. 2018;13(18):1949–56. PMID: 30047603. DOI: 10.1002/cmdc.201800377. http://www.ncbi.nlm.nih.gov/pubmed/30047603 +Pubmed+DOI
Rühl R, Krezel W, de Lera AR. 9-Cis-13,14-dihydroretinoic acid, a new endogenous mammalian ligand of retinoid X receptor and the active ligand of a potential new vitamin A category: vitamin A5. Nutr Rev. 2018 Dec;76(12):929–41. PMID: 30358857. DOI: 10.1093/nutrit/nuy057. http://www.ncbi.nlm.nih.gov/pubmed/30358857 +Pubmed+DOI
Artículos Científicos
Alonso I, Alvarez R, de Lera ÁR. Indole-Indole Ullmann Cross-Coupling for C Ar -N Bond Formation: Total Synthesis of (-)-Aspergilazine A. European J Org Chem. 2017 Sep;2017(33):4948–54. DOI: 10.1002/ejoc.201700842. IF2017: 2.882; Q2. http://doi.wiley.com/10.1002/ejoc.201700842 +DOI
Álvarez R, Vilar U, Madich Y, Aurrecoechea JM. On the regiochemical differences between Pd-catalyzed heterocyclization-allylation and -arylation reactions of alkynylbenzamides: preparation of 4-allyl-isochromen-1-imines and computational study. Org Biomol Chem. 2017 Oct;15(40):8594–605. PMID: 28979956. DOI: 10.1039/c7ob02117h. IF2017: 3.423; Q2. http://www.ncbi.nlm.nih.gov/pubmed/28979956 +Pubmed+DOI
Carvalho JE, Theodosiou M, Chen J, Chevret P, Alvarez S, De Lera AR, Laudet V, Croce JC, Schubert M. Lineage-specific duplication of amphioxus retinoic acid degrading enzymes (CYP26) resulted in sub-functionalization of patterning and homeostatic roles. BMC Evol Biol. BMC Evolutionary Biology; 2017 Jan;17(1):24. PMID: 28103795. DOI: 10.1186/s12862-016-0863-1. IF2017: 3.027; Q2. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5247814/pdf/12862_2016_Article_863.pdf +Pubmed+DOI
del Pozo J, Pérez-Iglesias M, Álvarez R, Lledós A, Casares JA, Espinet P. Speciation of ZnMe 2 , ZnMeCl, and ZnCl 2 in Tetrahydrofuran (THF), and Its Influence on Mechanism Calculations of Catalytic Processes. ACS Catal. 2017 May;7(5):3575–83. DOI: 10.1021/acscatal.6b03636. IF2017: 11.384; D1. http://pubs.acs.org/doi/10.1021/acscatal.6b03636 +DOI
Dominguez M, Alvarez S, de Lera AR. Natural and Structure-based RXR Ligand Scaffolds and Their Functions. Curr Top Med Chem. 2017 Jan;17(6):631–62. PMID: 27320335. DOI: 10.2174/1568026616666160617072521. IF2017: 3.374; Q2. http://www.ncbi.nlm.nih.gov/pubmed/27320335 +Pubmed+DOI
Gallego S, Lorenzo P, Alvarez R, de Lera AR. Total synthesis of naturally occurring (+)-psychotriasine and the related tetrahydro-?-carboline, dimeric tryptamines with NC connectivities. Tetrahedron Lett. 2017 Jan;58(3):210–2. DOI: 10.1016/j.tetlet.2016.12.003. IF2017: 2.125; Q2. http://linkinghub.elsevier.com/retrieve/pii/S004040391631629X +DOI
González-Pérez AB, Grechkin A, de Lera ÁR. Rearrangement of vinyl allene oxide geometric isomers to cyclopentenones. Further computational insights with biologically relevant model systems. Org Biomol Chem. 2017 Mar;15(13):2846–55. PMID: 28286893. DOI: 10.1039/c6ob02791a. IF2017: 3.423; Q2. http://www.ncbi.nlm.nih.gov/pubmed/28286893 +Pubmed+DOI
Guillade L, González-Pérez AB, de Lera ÁR. Synthesis of the octahydronaphthalene core of nahuoic acid A via a B(C6F5)3-catalyzed intramolecular Diels-Alder (IMDA) reaction. Org Biomol Chem. 2017 Sep;15(35):7430–8. PMID: 28831488. DOI: 10.1039/c7ob01665d. IF2017: 3.423; Q2. http://www.ncbi.nlm.nih.gov/pubmed/28831488 +Pubmed+DOI
Iturrioz-Rodríguez N, González-Domínguez E, González-Lavado E, Marín-Caba L, Vaz B, Pérez-Lorenzo M, Correa-Duarte MA, Fanarraga ML. A Biomimetic Escape Strategy for Cytoplasm Invasion by Synthetic Particles. Angew Chem Int Ed Engl. 2017 Oct;56(44):13736–40. PMID: 28873280. DOI: 10.1002/anie.201707769. IF2017: 12.102; D1. http://www.ncbi.nlm.nih.gov/pubmed/28873280 +Pubmed+DOI
Landrier J-F, Kasiri E, Karkeni E, Mihály J, Béke G, Weiss K, Lucas R, Aydemir G, Salles J, Walrand S, de Lera AR, Rühl R. Reduced adiponectin expression after high-fat diet is associated with selective up-regulation of ALDH1A1 and further retinoic acid receptor signaling in adipose tissue. FASEB J. 2017;31(1):203–11. PMID: 27729412. DOI: 10.1096/fj.201600263RR. IF2017: 5.595; D1. http://www.ncbi.nlm.nih.gov/pubmed/27729412 +Pubmed+DOI
Ruiz FX, Crespo I, Álvarez S, Porté S, Giménez-Dejoz J, Cousido-Siah A, Mitschler A, de Lera ÁR, Parés X, Podjarny A, Farrés J. Structural basis for the inhibition of AKR1B10 by the C3 brominated TTNPB derivative UVI2008. Chem Biol Interact. 2017 Oct;276:174–81. PMID: 28161411. DOI: 10.1016/j.cbi.2017.01.026. IF2017: 3.296; Q2. http://www.ncbi.nlm.nih.gov/pubmed/28161411 +Pubmed+DOI
Artículos Científicos
Bazhin A V, Bleul T, de Lera AR, Werner J, Rühl R. Relationship Between All-trans-13,14-Dihydro Retinoic Acid and Pancreatic Adenocarcinoma. Pancreas. 2016 Jul;45(6):e29-31. PMID: 27295537. DOI: 10.1097/MPA.0000000000000601. IF2016: 2.967; Q2. http://www.ncbi.nlm.nih.gov/pubmed/27295537 +Pubmed+DOI
de Lera AR, Ganesan A. Epigenetic polypharmacology: from combination therapy to multitargeted drugs. Clin Epigenetics. Clinical Epigenetics; 2016 Oct;8(1):105. PMID: 27752293. DOI: 10.1186/s13148-016-0271-9. IF2016: 4.987; Q1. http://www.ncbi.nlm.nih.gov/pubmed/27752293 +Pubmed+DOI
de Lera ÁR, Krezel W, Rühl R. An Endogenous Mammalian Retinoid X Receptor Ligand, At Last! ChemMedChem. 2016 May;11(10):1027–37. PMID: 27151148. DOI: 10.1002/cmdc.201600105. IF2016: 3.225; Q2. http://www.ncbi.nlm.nih.gov/pubmed/27151148 +Pubmed+DOI
del Pozo J, Salas G, Álvarez R, Casares JA, Espinet P. The Negishi Catalysis: Full Study of the Complications in the Transmetalation Step and Consequences for the Coupling Products. Organometallics. 2016 Oct;35(20):3604–11. DOI: 10.1021/acs.organomet.6b00660. IF2016: 3.862; Q1. http://pubs.acs.org/doi/10.1021/acs.organomet.6b00660 +DOI
Galván A, González-Pérez AB, Álvarez R, de Lera AR, Fañanás FJ, Rodríguez F. Exploiting the Multidentate Nature of Chiral Disulfonimides in a Multicomponent Reaction for the Asymmetric Synthesis of Pyrrolo[1,2-a]indoles: A Remarkable Case of Enantioinversion. Angew Chem Int Ed Engl. 2016 Mar;55(10):3428–32. PMID: 26833640. DOI: 10.1002/anie.201511231. IF2016: 11.994; D1. http://www.ncbi.nlm.nih.gov/pubmed/26833640 +Pubmed+DOI
García-García C, Ortiz-Rojano L, Álvarez S, Álvarez R, Ribagorda M, Carreño MC. Friedel-Crafts Alkylation of Indoles with p-Quinols: The Role of Hydrogen Bonding of Water for the Desymmetrization of the Cyclohexadienone System. Org Lett. 2016 May;18(9):2224–7. PMID: 27088217. DOI: 10.1021/acs.orglett.6b00781. IF2016: 6.579; D1. http://www.ncbi.nlm.nih.gov/pubmed/27088217 +Pubmed+DOI
Gavalás-Olea A, Álvarez S, Riobó P, Rodríguez F, Garrido JL, Vaz B. 19,19´-Diacyloxy Signature: An Atypical Level of Structural Evolution in Carotenoid Pigments. Org Lett. 2016 Sep;18(18):4642–5. PMID: 27583572. DOI: 10.1021/acs.orglett.6b02272. IF2016: 6.579; D1. http://www.ncbi.nlm.nih.gov/pubmed/27583572 +Pubmed+DOI
Gutierrez-Mazariegos J, Nadendla EK, Studer RA, Alvarez S, de Lera AR, Kuraku S, Bourguet W, Schubert M, Laudet V. Evolutionary diversification of retinoic acid receptor ligand-binding pocket structure by molecular tinkering. R Soc open Sci. 2016 Mar;3(3):150484. PMID: 27069642. DOI: 10.1098/rsos.150484. IF2016: 2.243; Q2. http://www.ncbi.nlm.nih.gov/pubmed/27069642 +Pubmed+DOI
Mihály J, Gericke J, Lucas R, de Lera AR, Alvarez S, Tör?csik D, Rühl R. TSLP expression in the skin is mediated via RAR?-RXR pathways. Immunobiology. 2016 Feb;221(2):161–5. PMID: 26531761. DOI: 10.1016/j.imbio.2015.09.013. IF2016: 2.720; Q3. http://www.ncbi.nlm.nih.gov/pubmed/26531761 +Pubmed+DOI
Vaz B, Alvarez R, de Lera AR. Stereocontrolled synthesis of ( S )-9- cis – and ( S )-11- cis -13,14-dihydroretinoic acid. Tetrahedron. 2016 Jul;72(27–28):3898–904. DOI: 10.1016/j.tet.2016.05.006. IF2016: 2.651; Q2. http://linkinghub.elsevier.com/retrieve/pii/S0040402016303787 +DOI
Artículos Científicos
Álvarez S, Lieb M, Martínez C, Khanwalkar H, Rodríguez-Barrios F, Álvarez R, Gronemeyer H, de Lera AR. Modulation of Retinoic Acid Receptor Subtypes by 5- and 8-Substituted (Naphthalen-2-yl)-based Arotinoids. ChemMedChem. 2015 Aug;10(8):1378–91. PMID: 26012882. DOI: 10.1002/cmdc.201500150. IF2015: 2.980; Q2. http://www.ncbi.nlm.nih.gov/pubmed/26012882 +Pubmed+DOI
Bertrand S, Aldea D, Oulion S, Subirana L, de Lera AR, Somorjai I, Escriva H. Evolution of the Role of RA and FGF Signals in the Control of Somitogenesis in Chordates. Brand T (ed.). PLoS One. Public Library of Science; 2015 Sep;10(9):e0136587. PMID: 26371756. DOI: 10.1371/journal.pone.0136587. IF2015: 3.057; Q1. http://www.ncbi.nlm.nih.gov/pubmed/26371756 +Pubmed+DOI
delPozo J, Gioria E, Casares JA, Álvarez R, Espinet P. Organometallic Nucleophiles and Pd: What Makes ZnMe 2 Different? Is Au Like Zn? Organometallics. American Chemical Society; 2015 Jul;34(13):3120–8. DOI: 10.1021/acs.organomet.5b00329. IF2015: 4.186; Q1. http://pubs.acs.org/doi/abs/10.1021/acs.organomet.5b00329 +DOI
Denis JG, Franci G, Altucci L, Aurrecoechea JM, de Lera ÁR, Álvarez R. Synthesis of 7-alkylidene-7,12-dihydroindolo[3,2-d]benzazepine-6-(5H)-ones (7-alkylidene-paullones) by N-cyclization-oxidative Heck cascade and characterization as sirtuin modulators. Org Biomol Chem. 2015 Mar;13(9):2800–10. PMID: 25604354. DOI: 10.1039/c4ob02493a. IF2015: 3.559; Q1. http://www.ncbi.nlm.nih.gov/pubmed/25604354 +Pubmed+DOI
Galván A, Calleja J, González-Pérez AB, Álvarez R, de Lera AR, Fañanás FJ, Rodríguez F. Stereoselective [3+2] Carbocyclization of Indole-Derived Imines and Electron-Rich Alkenes: A Divergent Synthesis of Cyclopenta[b]indole or Tetrahydroquinoline Derivatives. Chemistry. WILEY?VCH Verlag; 2015 Nov;21(47):16769–74. PMID: 26440995. DOI: 10.1002/chem.201503044. IF2015: 5.771; Q1. http://www.ncbi.nlm.nih.gov/pubmed/26440995 +Pubmed+DOI
Madich Y, Álvarez R, Aurrecoechea JM. Palladium-Catalyzed 6- endo -Selective Oxycyclization-Alkene Addition Cascades of ortho -Alkynylarylcarboxamides and ?,?-Unsaturated Carbonyl Compounds. European J Org Chem. WILEY?VCH Verlag; 2015 Oct;2015(28):6298–305. DOI: 10.1002/ejoc.201500797. IF2015: 3.068; Q2. http://doi.wiley.com/10.1002/ejoc.201500797 +DOI
Rühl R, Krzy?osiak A, Niewiadomska-Cimicka A, Rochel N, Szeles L, Vaz B, Wietrzych-Schindler M, Álvarez S, Szklenar M, Nagy L, de Lera AR, Kr??el W. 9-cis-13,14-Dihydroretinoic Acid Is an Endogenous Retinoid Acting as RXR Ligand in Mice. PLoS Genet. 2015 Jun;11(6):e1005213. PMID: 26030625. DOI: 10.1371/journal.pgen.1005213. IF2015: 6.661; D1. http://www.ncbi.nlm.nih.gov/pubmed/26030625 +Pubmed+DOI
Ruiz FX, Cousido-Siah A, Porté S, Domínguez M, Crespo I, Rechlin C, Mitschler A, de Lera ÁR, Martín MJ, de la Fuente JÁ, Klebe G, Parés X, Farrés J, Podjarny A. Structural Determinants of the Selectivity of 3-Benzyluracil-1-acetic Acids toward Human Enzymes Aldose Reductase and AKR1B10. ChemMedChem. 2015 Dec;10(12):1989–2003. PMID: 26549844. DOI: 10.1002/cmdc.201500393. IF2015: 2.980; Q2. http://www.ncbi.nlm.nih.gov/pubmed/26549844 +Pubmed+DOI
Vaz B, Fontán N, Castiñeira M, Álvarez R, de Lera ÁR. Synthesis of labile all-trans-7,8,7´,8´-bis-acetylenic carotenoids by bi-directional Horner-Wadsworth-Emmons condensation. Org Biomol Chem. 2015 Mar;13(10):3024–31. PMID: 25622142. DOI: 10.1039/c4ob02144d. IF2015: 3.559; Q1. http://www.ncbi.nlm.nih.gov/pubmed/25622142 +Pubmed+DOI
Vaz B, Salgueiriño V, Pérez-Lorenzo M, Correa-Duarte MA. Enhancing the Exploitation of Functional Nanomaterials through Spatial Confinement: The Case of Inorganic Submicrometer Capsules. Langmuir. 2015 Aug;31(32):8745–55. PMID: 25736568. DOI: 10.1021/acs.langmuir.5b00098. IF2015: 3.993; Q1. http://www.ncbi.nlm.nih.gov/pubmed/25736568 +Pubmed+DOI
Zheng G, Kaefer K, Mourdikoudis S, Polavarapu L, Vaz B, Cartmell SE, Bouleghlimat A, Buurma NJ, Yate L, de Lera ÁR, Liz-Marzán LM, Pastoriza-Santos I, Pérez-Juste J. Palladium Nanoparticle-Loaded Cellulose Paper: A Highly Efficient, Robust, and Recyclable Self-Assembled Composite Catalytic System. J Phys Chem Lett. 2015 Jan;6(2):230–8. PMID: 26263455. DOI: 10.1021/jz5024948. IF2015: 8.539; D1. http://www.ncbi.nlm.nih.gov/pubmed/26263455 +Pubmed+DOI
Artículos Científicos
Álvarez R, Vaz B, Gronemeyer H, de Lera ÁR. Functions, therapeutic applications, and synthesis of retinoids and carotenoids. Chem Rev. 2014 Jan;114(1):1–125. PMID: 24266866. DOI: 10.1021/cr400126u. IF: 46.568; Q1. http://www.ncbi.nlm.nih.gov/pubmed/24266866 +Pubmed+DOI
Calleja J, González-Pérez AB, de Lera ÁR, Álvarez R, Fañanás FJ, Rodríguez F. Enantioselective synthesis of hexahydrofuro[3,2-c] quinolines through a multicatalytic and multicomponent process. A new “aromatic sandwich” model for BINOL-phosphoric acid catalyzed reactions. Chem Sci. The Royal Society of Chemistry; 2014 Feb;5(3):996–1007. DOI: 10.1039/C3SC52891J. IF: 9.211; Q1. http://pubs.rsc.org/en/content/articlehtml/2014/sc/c3sc52891j +DOI
Cousido-Siah A, Ruiz FX, Mitschler A, Porté S, de Lera ÁR, Martín MJ, Manzanaro S, de la Fuente JA, Terwesten F, Betz M, Klebe G, Farrés J, Parés X, Podjarny A. Identification of a novel polyfluorinated compound as a lead to inhibit the human enzymes aldose reductase and AKR1B10: structure determination of both ternary complexes and implications for drug design. Acta Crystallogr D Biol Crystallogr. 2014 Mar;70(Pt 3):889–903. PMID: 24598757. DOI: 10.1107/S1399004713033452. IF: 2.674; Q1. http://www.ncbi.nlm.nih.gov/pubmed/24598757 +Pubmed+DOI
Fenollosa R, Garcia-Rico E, Alvarez S, Alvarez R, Yu X, Rodriguez I, Carregal-Romero S, Villanueva C, Garcia-Algar M, Rivera-Gil P, de Lera AR, Parak WJ, Meseguer F, Alvarez-Puebla RA. Silicon particles as trojan horses for potential cancer therapy. J Nanobiotechnology. 2014 Jan;12:35. PMID: 25223512. DOI: 10.1186/s12951-014-0035-7. IF: 4.115; Q1. http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=4428529&tool=pmcentrez&rendertype=abstract +Pubmed+DOI
García-Rodríguez J, Pérez-Rodríguez S, Ortiz MA, Pereira R, de Lera AR, Piedrafita FJ. Inhibition of I?B kinase-? and I?B kinase-? by heterocyclic adamantyl arotinoids. Bioorg Med Chem. 2014 Feb;22(4):1285–302. PMID: 24457093. DOI: 10.1016/j.bmc.2014.01.006. IF: 2.793; Q2. http://www.ncbi.nlm.nih.gov/pubmed/24457093 +Pubmed+DOI
González-Pérez AB, Grechkin A, de Lera AR. A unifying mechanism for the rearrangement of vinyl allene oxide geometric isomers to cyclopentenones. Org Biomol Chem. 2014 Oct;12(39):7694–701. PMID: 24942560. DOI: 10.1039/c4ob00562g. IF: 3.562; Q1. http://www.ncbi.nlm.nih.gov/pubmed/24942560 +Pubmed+DOI
Koop D, Chen J, Theodosiou M, Carvalho JE, Alvarez S, de Lera AR, Holland LZ, Schubert M. Roles of retinoic acid and Tbx1/10 in pharyngeal segmentation: amphioxus and the ancestral chordate condition. Evodevo. 2014 Jan;5(1):36. PMID: 25664163. DOI: 10.1186/2041-9139-5-36. IF: 3.034; Q2. http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=4320481&tool=pmcentrez&rendertype=abstract +Pubmed+DOI
Lorenzo P, Álvarez R, de Lera ÁR. Total synthesis and structural revision of (+)-cristatumin C. J Nat Prod. 2014 Feb;77(2):421–3. PMID: 24437951. DOI: 10.1021/np400969u. IF: 3.798; Q1. http://www.ncbi.nlm.nih.gov/pubmed/24437951 +Pubmed+DOI
Lorenzo P, Álvarez R, de Lera ÁR. Total Synthesis and Structural Revision of (-)-Protubonine A and (-)-Protubonine B. European J Org Chem. 2014 Apr;2014(12):2557–64. DOI: 10.1002/ejoc.201400029. IF: 3.065; Q1. http://doi.wiley.com/10.1002/ejoc.201400029 +DOI
Madich Y, Álvarez R, Aurrecoechea JM. Palladium-Catalyzed Regioselective 5- exo – O -Cyclization/Oxidative Heck Cascades from o -Alkynylbenzamides and Electron-Deficient Alkenes. European J Org Chem. 2014 Oct;2014(28):6263–71. DOI: 10.1002/ejoc.201402709. IF: 3.065; Q1. http://doi.wiley.com/10.1002/ejoc.201402709 +DOI
Martínez C, Lieb M, Alvarez S, Rodríguez-Barrios F, Alvarez R, Khanwalkar H, Gronemeyer H, de Lera AR. Dual RXR Agonists and RAR Antagonists Based on the Stilbene Retinoid Scaffold. ACS Med Chem Lett. 2014 May;5(5):533–7. PMID: 24900875. DOI: 10.1021/ml400521f. IF: 3.120; Q1. http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=4027779&tool=pmcentrez&rendertype=abstract +Pubmed+DOI
Código
PID2019-107855RB-I00
Título
Síntesis estereocontrolada de productos naturales poliénicos bioactivos con potencial terapéutico y mecanismos biogenéticos pericíclicos
Financiador
Ministerio de Ciencia e Innovación
Tipo
Individual
Duración
2020 – 2023
IP
Ángel Rodríguez de Lera
Código
ED481B-2018/022
Título
Design and Stereocontrolled Total Synthesis of Macrotermycins A-D
Financiador
Consellería de Cultura, Educación e Ordenación Universitaria
Tipo
Individual
Duración
2018 – 2020
IP
Paula Lorenzo Fernández
Código
ED431C 2017/61-GRC
Título
Consolidación y estructuración de unidades de investigación competitivas del SUG. Grupos de Referencia Competitiva
Financiador
Axencia Galega de Innovación
Tipo
Individual
Duración
2017 – 2020
IP
Ángel Rodríguez de Lera
Código
MICINN-SAF2016-77620-R
Título
Retinoides y Moduladores Epigeneticos Inspirados en la Estructura de Productos Naturales: Desarrollo y Aplicaciones
Financiador
Ministerio de Economía y Competitividad
Tipo
Individual
Duración
2017 – 2019
IP
Ángel Rodríguez de Lera
Código
MICINN-CTQ2015-68794-P
Título
Desarrollo de Reacciones en Cascada Catalizadas por Paladio: Estudio ComputaCional y Aplicaciones en Sintesis de Heterociclos
Financiador
Ministerio de Ciencia e Innovación
Tipo
Individual
Duración
2016 – 2018
IP
Rosana Álvarez Rodríguez
Código
IJCI-2014-19146
Título
Enabling Technologies In Synthesis
Financiador
Ministerio de Economía y Competitividad
Tipo
Individual
Duración
2016 – 2018
IP
Jose Antonio Souto Salgado
Código
POS-B/2016/007-PR
Título
Fluoroalkylation Of (hetero)aryl Halides By Au-pd Synergistic Catalysis
Financiador
Consellería de Cultura, Educación e Ordenación Universitaria
Tipo
Individual
Duración
2016 – 2018
IP
Patricia García Domínguez
Código
SAF2013-48397-R
Título
Síntesis de nuevos moduladores de enzimas epigenéticas inspirados en la estructura de productos naturales
Financiador
Ministerio de Economía y Competitividad
Tipo
Individual
Duración
2014 – 2016
IP
Ángel Rodríguez de Lera
Código
CTQ2012-37734-C02-01
Título
Reacciones divergentes a través de cascadas heterociclación/acoplamiento catalizadas por paladio: Regioselectividad, quimioselectividad, y aplicaciones sintéticas.
Financiador
Ministerio de Economía y Competitividad
Tipo
Coordinado
Duración
2013 – 2015
IP
Ángel Rodríguez de Lera
Código
GRC2013-007
Título
Consolidación y estructuración de unidades de investigación competitivas del SUG. Grupos de Referencia Competitiva.
Financiador
Consellería de Cultura, Educación e Ordenación Universitaria
Tipo
Individual
Duración
2013 – 2016
IP
Ángel Rodríguez de Lera
Código
CN 2012/273 – INB1
Título
Contribución a un mellor coñecemento das patoloxías dende unha perspectiva multidisciplinar – Agrupación Estratégica para la Investigación en Biomedicina – INBIOMED
Financiador
Consellería de Cultura, Educación e Ordenación Universitaria
Tipo
Coordinado
Duración
2012 – 2015
IP
Ángel Rodríguez de Lera
Código
SAF2010-17935
Título
Diseño y Síntesis de Nuevos Moduladores de Enzimas Epigenéticas con Actividad Anticancerosa
Financiador
Ministerio de Economía y Competitividad
Tipo
Individual
Duración
2011 – 2014
IP
Ángel Rodríguez de Lera
Título
On the boundaries of computational organic chemistry: From pericyclic to enantioselective cyclizations and transition metal catalysed reactions
UVIGO, Universite de Strasbourg, University of Debrecen
Referencia
WO2018091937 (HU1600629 N/Ref. 2017/P1600629)
Fch. Prioridad
28/02/2008
Fch. Concesión
Título
Novel derivatives of psammaplin a, a method for their synthesis and their use for the prevention or treatment of cancer
Titular
Centre National de la Recherche Scientifique [FR], Universite De Strasbourg, Institut Nationa de la Sante et de la Recherche Medicale (INSERM)[FR], UVIGO, Seconda Universit A Degli Studi Di Napoli [IT], Radboud University Nijmegen [NL]
Referencia
WO2008IB01887
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