Research papers
- Conformational diversity in class C GPCR positive allosteric modulation
Cannone G., Berto L., Malhaire F., Ferguson G., Fouillen A., Balor S., Font-Ingles J., Llebaria A., Goudet C., Kotecha A., Vinothkumar K.R., Lebon G.
Nature Communications 2025 Jan 13: 16: 619
- Hemithioindigo-based histone deacetylase inhibitors induce a light-dependent anticancer effect
Josa-Culleré L., Aira Rodríguez C., Llebaria A.
Eur. J. Med. Chem. 2024 Dec 5: 279:116846 - A 'double-edged' role for type-5 metabotropic glutamate receptors in pain disclosed by light-sensitive drugs
Notartomaso S, Antenucci N, Mazzitelli M, Rovira X, Boccella S, Ricciardi F, Liberatore F, Gomez-Santacana X, Imbriglio T, Cannella M, Zussy C, Luongo L, Maione S, Goudet C, Battaglia G, Llebaria A, Nicoletti F, Neugebauer V.
Elife. 2024 Aug 22: 13:e94931
- Photoswitchable positive allosteric modulators of metabotropic glutamate receptor 4 to improve selectivity
Panarello S, González-Díez A, Berizzi A E, Malhaire F, Borràs-Tudurí R, Rovira X, Serra C, Prézeau L, Pin J P, Goudet C, Llebaria A, Gómez-Santacana X.
iSCIENCE. 2024 Jun 21: 27(6)110123
- Boosting the Impact of EFMC Young Scientists Network Through the Creation of Working Groups
Mari M, Lanthier C, Proj M, Donckele E J, Josa-Culleré L, Goncharenko K, Leroy S, Matagne B, McKenna S M, Borsari C
ChemMedChem, 2024 May 22
- Identification of differential biological activity and synergy between the PARP inhibitor rucaparib and its major metabolite
Hu H, Serra C, Zhang W, Scrivo A, Fernandez-Carasa I, Consiglio A, Aytes A, Pujana M A, Llebaria A, Antolin A A .
Cell Chem Biol. 2024 May 16; 31(5):973-988.e4
- Optical Control of Adenosine A2A Receptor Using Istradefylline Photosensitivity
Dumazer A, Gómez-Santacana X, Malhaire F, Jopling C, Maurel D, Lebon G, Llebaria A, Goudet C.
ACS Chem. Neurosci. 2024 Jan 26: 15(3) 645–655
- Design and validation of a low-cost photomodulator for in vivo photoactivation of a mGluR5 inhibitor
Ajieren H, Fox A, Biggs E, Albors O, Llebaria A, Irazoqui P.
Biomed Eng Lett. 2023 Dec 4;14(2):245-254
- Mitochondria-targeted melatonin photorelease supports the presence of melatonin MT1 receptors in mitochondria inhibiting respiration
Somalo-Barranco G, Pagano Zottola AC, Abdulrahman AO, El Zein RM, Cannich A, Muñoz L, Serra C, Oishi A, Marsicano G, Masri B, Bellocchio L, Llebaria A, Jockers R.
Cell Chem Biol. 2023 Aug 17;30(8):920-932.e7
- The antioxidant l-Ergothioneine prevents cystine lithiasis in the Slc7a9-/- mouse model of cystinuria.
Mayayo-Vallverdú C, López de Heredia M, Prat E, González L, Espino Guarch M, Vilches C, Muñoz L, Asensi MA, Serra C, Llebaria A, Casado M, Artuch R, Garrabou G, Garcia-Roves PM, Pallardó FV, Nunes V.
Redox Biol. 2023 Aug;64:102801
- A Novel Family of Lysosomotropic Tetracyclic Compounds for Treating Leukemia
Carbó JM, Cornet-Masana JM, Cuesta-Casanovas L, Delgado-Martínez J, Banús-Mulet A, Clément-Demange L, Serra C, Catena J, Llebaria A, Esteve J, Risueño RM.
Cancers (Basel). 2023 Mar 22;15(6):1912
- Controlled Histone Deacetylase Inhibitors for Targeted Cancer Therapy
Josa-Culleré L, Llebaria A.
J Med Chem. 2023 Feb 9;66(3):1909-1927
- Photopharmacological manipulation of amygdala metabotropic glutamate receptor mGlu4 alleviates neuropathic pain
Pereira V, Arias JA, Llebaria A, Goudet C.
Pharmacol Res. 2023 Jan;187:106602
- Control of Theta Oscillatory Activity Underlying Fear Expression by mGlu5 Receptors
Matulewicz P, Ramos-Prats A, Gómez-Santacana X, Llebaria A, Ferraguti F.
Cells. 2022 Nov 10;11(22):3555
- Caged-carvedilol as a new tool for visible-light photopharmacology of β-adrenoceptors in native tissues
Duran-Corbera A, Font J, Faria M, Prats E, Consegal M, Catena J, Muñoz L, Raldua D, Rodriguez-Sinovas A, Llebaria A, Rovira X.
iScience. 2022 Sep 13;25(10):105128
- Design and Validation of the First Family of Photo-Activatable Ligands for Melatonin Receptors
Somalo-Barranco G, Serra C, Lyons D, Piggins HD, Jockers R, Llebaria A.
J Med Chem. 2022 Aug 25;65(16):11229-11240.
- Light-Induced Activation of a Specific Type-5 Metabotropic Glutamate Receptor Antagonist in the Ventrobasal Thalamus Causes Analgesia in a Mouse Model of Breakthrough Cancer Pain
Notartomaso S, Antenucci N, Liberatore F, Mascio G, Boccadamo Pompili SV, Font J, Scioli M, Luongo L, Arcella A, Gradini R, Llebaria A, Nicoletti F.
Int J Mol Sci. 2022 Jul 20;23(14):8018
- Photoswitchable allosteric modulators for metabotropic glutamate receptors
Gómez-Santacana X, Panarello S, Rovira X, Llebaria A.
Curr Opin Pharmacol. 2022 Oct;66:102266
- Ligand Targeting the β1-Adrenoceptor Enables Light-Control of the Cardiac Rhythm
Duran-Corbera A, Faria M, Ma Y, Prats E, Dias A, Catena J, Martinez KL, Raldua D, Llebaria A, Rovira X.
Angew Chem Int Ed Engl. 2022 Jul 25;61(30):e202203449
- Fast Photoswitchable Molecular Prosthetics Control Neuronal Activity in the Cochlea
Garrido-Charles A, Huet A, Matera C, Thirumalai A, Hernando J, Llebaria A, Moser T, Gorostiza P.
J Am Chem Soc. 2022 Jun 1;144(21):9229-9239
- Environmental levels of carbaryl impair zebrafish larvae behaviour: The potential role of ADRA2B and HTR2B
Faria M, Bellot M, Bedrossiantz J, Ramírez JRR, Prats E, Garcia-Reyero N, Gomez-Canela C, Mestres J, Rovira X, Barata C, Oliván LMG, Llebaria A, Raldua D.
J Hazard Mater. 2022 Jun 5;431:128563
- S-Methyl-L-Ergothioneine to L-Ergothioneine Ratio in Urine Is a Marker of Cystine Lithiasis in a Cystinuria Mouse Model
López de Heredia M, Muñoz L, Carru C, Sotgia S, Zinellu A, Serra C, Llebaria A, Kato Y, Nunes V.
Antioxidants (Basel). 2021 Sep 7;10(9):1424
- Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations
Nasrallah C, Cannone G, Briot J, Rottier K, Berizzi AE, Huang CY, Quast RB, Hoh F, Banères JL, Malhaire F, Berto L, Dumazer A, Font-Ingles J, Gómez- Santacana X, Catena J, Kniazeff J, Goudet C, Llebaria A, Pin JP, Vinothkumar KR, Lebon G
Cell Rep. 2021 Aug 31;36(9):109648
- Remote local photoactivation of morphine produces analgesia without opioid-related adverse effects
López-Cano M, Font J, Aso E, Sahlholm K, Cabré G, Giraldo J, De Koninck Y, Hernando J, Llebaria A, Fernández-Dueñas V, Ciruela F.
Br J Pharmacol. 2023 Apr;180(7):958-974
- New Paradigm in NKT Cell Antigens: MCS-0208 (2-(Hydroxymethyl)phenylthio-phytoceramide) - an Aryl-Phytoceramide Compound with a Single Hydroxyl Group Stimulates NKT Cells
Borràs-Tudurí R, Alcaide A, Aspeslag S, Usero L, Serra C, Roura-Mir C, Elewaut D, Llebaria A.
ChemMedChem. 2021 Aug 19;16(16):2491-2496
- Mimetics of extra virgin olive oil phenols with anti-cancer stem cell activity
Cuyàs E, Gumuzio J, Lozano-Sánchez J, Segura-Carretero A, Verdura S, Bosch-Barrera J, Martin-Castillo B, Nonell-Canals A, Llebaria A, Cabello S, Serra C, Sanchez-Martinez M, Martin ÁG, Menendez JA
Aging (Albany NY). 2020 Nov 9;12(21):21057-21075
- Mechanistic Insights into Light-Driven Allosteric Control of GPCR Biological Activity
Ricart-Ortega M, Berizzi AE, Pereira V, Malhaire F, Catena J, Font J, Gómez-
Santacana X, Muñoz L, Zussy C, Serra C, Rovira X, Goudet C, Llebaria AACS Pharmacol Transl Sci. 2020 Aug 18;3(5):883-895
- Photoswitchable Antagonists for a Precise Spatiotemporal Control of β2-Adrenoceptors
Duran-Corbera A, Catena J, Otero-Viñas M, Llebaria A, Rovira X.
J Med Chem. 2020 Aug 13;63(15):8458-8470
- Development and validation of a mass spectrometry binding assay for mGlu5 receptor
Ricart-Ortega M, Berizzi AE, Catena J, Malhaire F, Muñoz L, Serra C, Lebon G, Goudet C, Llebaria A.
Anal Bioanal Chem. 2020 Sep;412(22):5525-5535
- Optical Modulation of Metabotropic Glutamate Receptor Type 5 In Vivo Using a Photoactive Drug
López-Cano M, Font J, Llebaria A, Fernández-Dueñas V, Ciruela F.
Drug. Methods Mol Biol. 2019;1947:351-359
- Reversible silencing of endogenous receptors in intact brain tissue using 2-photon pharmacology
Pittolo S, Lee H, Lladó A, Tosi S, Bosch M, Bardia L, Gómez-Santacana X, Llebaria A, Soriano E, Colombelli J, Poskanzer KE, Perea G, Gorostiza P
Proc. Natl. Acad. Sci. U. S. A., 2019, 116 (27), 13680-13689 - GPCR photopharmacology
Ricart-Ortega M, Font J, Llebaria A
Mol. Cell. Endocrinol., 2019, 488, 36-51 - A light-controlled allosteric modulator unveils a role for mGlu4 receptors during early stages of ischemia in the rodent cerebellar cortex
Bossi S, Helleringer R, Galante M, Monlleó E, Trapero A, Rovira X, Daniel H, Llebaria A, McLean H
Front. Cell. Neurosci., 2018, 12, 449 - Dietary and microbial oxazoles induce intestinal inflammation by modulating aryl hydrocarbon receptor responses
Iyer SS, Gensollen T, Gandhi A, Oh SF, Neves JF, Collin F, Lavin R, Serra C, Glickman J, de Silva PSA, Sartor RB, Besra G, Hauser R, Maxwell A, Llebaria A, Blumberg RS
Cell, 2018, 173(5), 1123-1134.e11 - Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs
Nasrallah C, Rottier K, Marcellin R, Compan V, Font J, Llebaria A, Pin JP, Banères JL, Lebon G
Sci. Rep., 2018, 8(1), 4407 - Dynamic modulation of inflammatory pain-related affective and sensory symptoms by optical control of amygdala metabotropic glutamate receptor 4
Zussy C, Gómez-Santacana X, Rovira X, de Bundel D, Ferrazzo S, Bosch D, Asede D, Malhaire F, Acher F, Giraldo J, Valjent E, Ehrlich I, Ferraguti F, Pin JP, Llebaria A, Goudet C
Mol. Psychiatr., 2018, 23(3), 509-520 - Optical activation of endogenous metabotropic glutamate receptor 4 (mGlu4) in the amygdala dynamically regulates symptoms associated with persistent inflammatory pain
Zussy C, Gómez-Santacana X, Rovira X, de Bundel D, Ferrazzo S, Bosch D, Asede D, Malhaire F, Acher F, Giraldo J, Valjent E, Ehrlich I, Ferraguti F, Pin JP, Llebaria A, Goudet C
Mol. Psychiatr., 2018, 23(3), 489 - Shedding light on metabotropic glutamate receptors using optogenetics and photopharmacology
Goudet C, Rovira X, Llebaria A
Curr. Opin. Pharmacol., 2018, 38, 8-15 - Mechanical allodynia assessment in a murine neuropathic pain model
Notartomaso S, Scarselli P, Di Pietro P, Battaglia G, Llebaria A, Ciruela F, Nicoletti F
Bio-protocol, 2018, 8(2), e2671 - Formalin murine model of pain
López-Cano M, Fernández-Dueñas V, Llebaria A, Ciruela F
Bio-protocol, 2017, 7(23), e2628 - Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer
Liu J, Zhang Z, Moreno-Delgado D, Dalton JA, Rovira X, Trapero A, Goudet C, Llebaria A, Giraldo J, Yuan Q, Rondard P, Huang S, Liu J, Pin JP
eLife, 2017, 6, e26985 - Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
Font J, López-Cano M, Notartomaso S, Scarselli P, Di Pietro P, Bresolí-Obach R, Battaglia G, Malhaire F, Rovira X, Catena J, Giraldo J, Pin JP, Fernández-Dueñas V, Goudet C, Nonell S, Nicoletti F, Llebaria A, Ciruela F
eLife, 2017, 6, e23545 - Positional isomers of bispyridine benzene derivatives induce efficacy changes on mGlu5 negative allosteric modulation
Gómez-Santacana X, Dalton JAR, Rovira X, Pin JP, Goudet C, Gorostiza P, Giraldo J, Llebaria A
Eur. J. Med. Chem., 2017, 127, 567-576 - Illuminating phenylazopyridines to photoswitch metabotropic glutamate receptors: from the flask to the animals
Gómez-Santacana X, Pittolo S, Rovira X, Lopez M, Zussy C, Dalton JAR, Faucherre A, Jopling C, Pin JP, Ciruela F, Goudet C, Giraldo J, Gorostiza P, Llebaria A
ACS Central Sci., 2017, 3(1), 81-91 - OptoGluNAM4.1, a photoswitchable allosteric antagonist for real-time control of mGlu4 receptor activity
Rovira X, Trapero A, Pittolo S, Zussy C, Faucherre A, Jopling C, Giraldo J, Pin JP, Gorostiza P, Goudet C, Llebaria A
Cell Chem. Biol., 2016, 23(8), 929-934 - Optical control of endogenous receptors and cellular excitability using targeted covalent photoswitches
Izquierdo-Serra M, Bautista-Barrufet A, Trapero A, Garrido-Charles A, Diaz-Tahoces A, Camarero N, Pittolo S, Valbuena S, Perez-Jimenez A, Gay M, Garcia-Moll A, Rodriguez-Escrich C, Lerma J, De La Villa P, Fernandez E, Pericas MA, Llebaria A, Gorostiza P
Nat. Commun., 2016, 7, 12221 - Shining light on an mGlu5 photoswitchable NAM: a theoretical perspective
Dalton JAR, Lans I, Rovira X, Malhaire F, Gómez-Santacana X, Pittolo S, Gorostiza P, Llebaria A, Goudet C, Pin JP, Giraldo J
Curr. Neuropharmacol., 2016, 14(5), 441-454 - Galacto configured N-aminoaziridines: a new type of irreversible inhibitor of β-galactosidases
Alcaide A, Trapero A, Pérez Y, Llebaria A
Org. Biomol. Chem., 2015, 13(20), 5690-5697 - Synthesis and evaluation of hydroxymethylaminocyclitols as glycosidase inhibitors
Trapero A, Egido-Gabás M, Bujons J, Llebaria A
J. Org. Chem., 2015, 80(7), 3512-3529 - Overlapping binding sites drive allosteric agonism and positive cooperativity in type 4 metabotropic glutamate receptors
Rovira X, Malhaire F, Scholler P, Rodrigo J, Gonzalez-Bulnes P, Llebaria A, Pin JP, Giraldo J, Goudet C
Faseb J., 2015, 29(1), 116-130 - Exploring the active conformation of cyclohexane carboxylate positive allosteric modulators of the type 4 metabotropic glutamate receptor
Rovira X, Harrak Y, Trapero A, González-Bulnes P, Malhaire F, Pin JP, Goudet C, Giraldo J, Llebaria A
ChemMedChem, 2014, 9(12), 2685-2698 - An allosteric modulator to control endogenous G protein-coupled receptors with light
Pittolo S, Gómez-Santacana X, Eckelt K, Rovira X, Dalton J, Goudet C, Pin JP, Llobet A, Giraldo J, Llebaria A, Gorostiza P
Nat. Chem. Biol., 2014, 10(10), 813-815 - A double effect molecular switch leads to a novel potent negative allosteric modulator of metabotropic glutamate receptor 5
Gómez-Santacana X, Rovira X, Dalton JA, Goudet C, Pin JP, Gorostiza P, Giraldo J, Llebaria A
MedChemComm, 2014, 5(10), 1548-1554 - Glucocerebrosidase inhibitors: future drugs for the treatment of Gaucher disease?
Trapero A, Llebaria A
Future Med. Chem., 2014, 6(9), 975-977 - Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation
Dalton JAR, Gómez-Santacana X, Llebaria A, Giraldo J
J. Chem Inf. Model., 2014, 54(5), 1476-1487 - Aziridine ring opening for the synthesis of sphingolipid analogues: inhibitors of sphingolipid-metabolizing enzymes
Alcaide A, Llebaria A
J. Org. Chem., 2014, 79(7), 2993-3029 - Structural and functional characterization of a novel nonglycosidic type I NKT agonist with immunomodulatory properties
Kerzerho J, Yu ED, Barra CM, Alari-Pahisa E, Girardi E, Harrak Y, Lauzurica P, Llebaria A, Zajonc DM, Akbari O, Castaño AR
J. Immunol., 2012, 188(5), 2254-2265 - NKT TCR recognition of CD1d-α-C-galactosylceramide
Patel O, Cameron G, Pellicci DG, Liu Z, Byun HS, Beddoe T, McCluskey J, Franck RW, Castaño AR, Harrak Y, Llebaria A, Bittman R, Porcelli SA, Godfrey DI, Rossjohn J
J. Immunol., 2011, 187(9), 4705-4713 - Galacto-configured aminocyclitol phytoceramides are potent in vivo invariant natural killer T cell stimulators
Harrak Y, Barra CM, Delgado A, Castaño AR, Llebaria A
J. Am. Chem. Soc., 2011, 133(31), 12079-12084