Publications

Nanotechnology-Based Targeted Drug Delivery: An Emerging Tool to Overcome Tuberculosis.
Baranyai Z, Soria-Carrera H, Alleva M, Millán-Placer AC, Lucía A, Martín-Rapún R, Aínsa JA, de la Fuente JM.
Adv. Therap. 2021; 4:2000113
DOI: 10.1002/adtp.202000113

In silico discovery and biological validation of ligands of FAD synthase, a promising new antimicrobial target.
Lans I, Anoz-Carbonell E, Palacio-Rodríguez K, Aínsa JA, Medina M, Cossio P.
PLoS Comput Biol. 2020 Aug 14;16(8):e1007898. doi: 10.1371/journal.pcbi.1007898.
PMID: 32797038

Co-delivery of free vancomycin and transcription factor decoy-nanostructured lipid carriers can enhance inhibition of methicillin resistant Staphylococcus aureus (MRSA).
Hibbitts A, Lucía A, Serrano-Sevilla I, De Matteis L, McArthur M, de la Fuente JM, Aínsa JA, Navarro F.
PLoS One. 2019 Sep 3;14(9):e0220684. doi: 10.1371/journal.pone.0220684.
PMID: 31479462

Design, Synthesis, and Efficacy Testing of Nitroethylene- and 7-Nitrobenzoxadiazol-Based Flavodoxin Inhibitors against Helicobacter pylori Drug-Resistant Clinical Strains and in Helicobacter pylori-Infected Mice.
Salillas S, Alías M, Michel V, Mahía A, Lucía A, Rodrigues L, Bueno J, Galano-Frutos JJ, De Reuse H, Velázquez-Campoy A, Carrodeguas JA, Sostres C, Castillo J, Aínsa JA, Díaz-de-Villegas MD, Lanas Á, Touati E, Sancho J.
J Med Chem. 2019 Jul 11;62(13):6102-6115. doi: 10.1021/acs.jmedchem.9b00355.
PMID: 31244111

Mycobacterial Aminoglycoside Acetyltransferases: A Little of Drug Resistance, and a Lot of Other Roles.
Sanz-García F, Anoz-Carbonell E, Pérez-Herrán E, Martín C, Lucía A, Rodrigues L, Aínsa JA.
Front Microbiol. 2019 Jan 30;10:46. doi: 10.3389/fmicb.2019.00046.
PMID: 30761098

Matryoshka-type gastro-resistant microparticles for the oral treatment of Mycobacterium tuberculosis.
Andreu V, Larrea A, Rodriguez-Fernandez P, Alfaro S, Gracia B, Lucía A, Usón L, Gomez AC, Mendoza G, Lacoma A, Dominguez J, Prat C, Sebastian V, Aínsa JA, Arruebo M.
Nanomedicine (Lond). 2019 Mar;14(6):707-726. doi: 10.2217/nnm-2018-0258.
PMID: 30734643

Polypeptidic Micelles Stabilized with Sodium Alginate Enhance the Activity of Encapsulated Bedaquiline.
Soria-Carrera H, Lucía A, De Matteis L, Aínsa JA, de la Fuente JM, Martín-Rapún R.
Macromol Biosci. 2019 Apr;19(4):e1800397. doi: 10.1002/mabi.201800397.
PMID: 30645022

Synthesis and biological activity of dehydrophos derivatives.
Jiménez-Andreu MM, Lucía Quintana A, Aínsa JA, Sayago FJ, Cativiela C.
Org Biomol Chem. 2019 Jan 31;17(5):1097-1112. doi: 10.1039/c8ob03079k.
PMID: 30633297

New active formulations against M. tuberculosis: Bedaquiline encapsulation in lipid nanoparticles and chitosan nanocapsules.
De Matteis L, Jary D, Lucía A, García-Embid S, Serrano-Sevilla I, Pérez D, Aínsa JA, Navarro FP, de la Fuente JM.
Chemical Engineering Journal. 2018 May;340: 181-191. https://doi.org/10.1016/j.cej.2017.12.110

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase.
Mori G, Orena BS, Franch C, Mitchenall LA, Godbole AA, Rodrigues L, Aguilar-Pérez C, Zemanová J, Huszár S, Forbak M, Lane TR, Sabbah M, Deboosere N, Frita R, Vandeputte A, Hoffmann E, Russo R, Connell N, Veilleux C, Jha RK, Kumar P, Freundlich JS, Brodin P, Aínsa JA, Nagaraja V, Maxwell A, Mikušová K, Pasca MR, Ekins S.
Tuberculosis (Edinb). 2018 Sep;112:98-109. doi: 10.1016/j.tube.2018.08.004.
PMID: 30205975

Boldine-Derived Alkaloids Inhibit the Activity of DNA Topoisomerase I and Growth of Mycobacterium tuberculosis.
García MT, Carreño D, Tirado-Vélez JM, Ferrándiz MJ, Rodrigues L, Gracia B, Amblar M, Aínsa JA, de la Campa AG.
Front Microbiol. 2018 Jul 24;9:1659. doi: 10.3389/fmicb.2018.01659.
PMID: 30087665

Synergy between Circular Bacteriocin AS-48 and Ethambutol against Mycobacterium tuberculosis.
Aguilar-Pérez C, Gracia B, Rodrigues L, Vitoria A, Cebrián R, Deboosère N, Song OR, Brodin P, Maqueda M, Aínsa JA.
Antimicrob Agents Chemother. 2018 Aug 27;62(9):e00359-18. doi: 10.1128/AAC.00359-18.
PMID: 29987141

Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs.
Glaus F, Dedić D, Tare P, Nagaraja V, Rodrigues L, Aínsa JA, Kunze J, Schneider G, Hartkoorn RC, Cole ST, Altmann KH.
J Org Chem. 2018 Jul 6;83(13):7150-7172. doi: 10.1021/acs.joc.8b00193.
PMID: 29542926

Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors.
Song L, Merceron R, Gracia B, Quintana AL, Risseeuw MDP, Hulpia F, Cos P, Aínsa JA, Munier-Lehmann H, Savvides SN, Van Calenbergh S.
J Med Chem. 2018 Apr 12;61(7):2753-2775. doi: 10.1021/acs.jmedchem.7b01570.
PMID: 29510037

Discovery of antimicrobial compounds targeting bacterial type FAD synthetases.
Sebastián M, Anoz-Carbonell E, Gracia B, Cossio P, Aínsa JA, Lans I, Medina M.
J Enzyme Inhib Med Chem. 2018 Dec;33(1):241-254. doi: 10.1080/14756366.2017.1411910.
PMID: 29258359

Ionophore A23187 shows anti-tuberculosis activity and synergy with tebipenem.
Huang W, Briffotaux J, Wang X, Liu L, Hao P, Cimino M, Buchieri MV, Namouchi A, Aínsa JA, Gicquel B.
Tuberculosis (Edinb). 2017 Dec;107:111-118. doi: 10.1016/j.tube.2017.09.001.
PMID: 29050757

How can nanoparticles contribute to antituberculosis therapy?
Costa-Gouveia J, Aínsa JA, Brodin P, Lucía A.
Drug Discov Today. 2017 Mar;22(3):600-607. doi: 10.1016/j.drudis.2017.01.011.
PMID: 28137645

Antituberculosis drugs: reducing efflux=increasing activity.
Rodrigues L, Parish T, Balganesh M, Aínsa JA.
Drug Discov Today. 2017 Mar;22(3):592-599. doi: 10.1016/j.drudis.2017.01.002.
PMID: 28089787

Structure-Activity Relationships of Spectinamide Antituberculosis Agents: A Dissection of Ribosomal Inhibition and Native Efflux Avoidance Contributions.
Liu J, Bruhn DF, Lee RB, Zheng Z, Janusic T, Scherbakov D, Scherman MS, Boshoff HI, Das S, Rakesh, Waidyarachchi SL, Brewer TA, Gracia B, Yang L, Bollinger J, Robertson GT, Meibohm B, Lenaerts AJ, Aínsa J, Böttger EC, Lee RE.
ACS Infect Dis. 2017 Jan 13;3(1):72-88. doi: 10.1021/acsinfecdis.6b00158.
PMID: 28081607

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria.
Singh V, Dhar N, Pató J, Kolly GS, Korduláková J, Forbak M, Evans JC, Székely R, Rybniker J, Palčeková Z, Zemanová J, Santi I, Signorino-Gelo F, Rodrigues L, Vocat A, Covarrubias AS, Rengifo MG, Johnsson K, Mowbray S, Buechler J, Delorme V, Brodin P, Knott GW, Aínsa JA, Warner DF, Kéri G, Mikušová K, McKinney JD, Cole ST, Mizrahi V, Hartkoorn RC.
Mol Microbiol. 2017 Jan;103(1):13-25. doi: 10.1111/mmi.13535.
PMID: 27677649

Lipid transport in Mycobacterium tuberculosis and its implications in virulence and drug development.
Bailo R, Bhatt A, Aínsa JA.
Biochem Pharmacol. 2015 Aug 1;96(3):159-67. doi: 10.1016/j.bcp.2015.05.001.
PMID: 25986884

Measuring efflux and permeability in mycobacteria.
Rodrigues L, Viveiros M, Aínsa JA.
Methods Mol Biol. 2015;1285:227-39. doi: 10.1007/978-1-4939-2450-9_13.
PMID: 25779319

Spectinamides: a new class of semisynthetic antituberculosis agents that overcome native drug efflux.
Lee RE, Hurdle JG, Liu J, Bruhn DF, Matt T, Scherman MS, Vaddady PK, Zheng Z, Qi J, Akbergenov R, Das S, Madhura DB, Rathi C, Trivedi A, Villellas C, Lee RB, Rakesh, Waidyarachchi SL, Sun D, McNeil MR, Aínsa JA, Boshoff HI, Gonzalez-Juarrero M, Meibohm B, Böttger EC, Lenaerts AJ.
Nat Med. 2014 Feb;20(2):152-158. doi: 10.1038/nm.3458.
PMID: 24464186

Analysis of mutations in streptomycin-resistant strains reveals a simple and reliable genetic marker for identification of the Mycobacterium tuberculosis Beijing genotype.
Villellas C, Aristimuño L, Vitoria MA, Prat C, Blanco S, García de Viedma D, Domínguez J, Samper S, Aínsa JA.
J Clin Microbiol. 2013 Jul;51(7):2124-30. doi: 10.1128/JCM.01944-12.
PMID: 23616454

Zanthoxylum capense constituents with antimycobacterial activity against Mycobacterium tuberculosis in vitro and ex vivo within human macrophages.
Luo X, Pires D, Aínsa JA, Gracia B, Duarte N, Mulhovo S, Anes E, Ferreira MJ.
J Ethnopharmacol. 2013 Mar 7;146(1):417-22. doi: 10.1016/j.jep.2013.01.013.
PMID: 23337743

Role of the Mmr efflux pump in drug resistance in Mycobacterium tuberculosis.
Rodrigues L, Villellas C, Bailo R, Viveiros M, Aínsa JA.
Antimicrob Agents Chemother. 2013 Feb;57(2):751-7. doi: 10.1128/AAC.01482-12.
PMID: 23165464

Inhibitors of mycobacterial efflux pumps as potential boosters for anti-tubercular drugs.
Viveiros M, Martins M, Rodrigues L, Machado D, Couto I, Aínsa J, Amaral L.
Expert Rev Anti Infect Ther. 2012 Sep;10(9):983-98. doi: 10.1586/eri.12.89.
PMID: 23106274

Mycobacterial shuttle vectors designed for high-level protein expression in infected macrophages.
Eitson JL, Medeiros JJ, Hoover AR, Srivastava S, Roybal KT, Aínsa JA, Hansen EJ, Gumbo T, van Oers NS.
Appl Environ Microbiol. 2012 Oct;78(19):6829-37. doi: 10.1128/AEM.01674-12.
PMID: 22820329

Functional and genetic characterization of the tap efflux pump in Mycobacterium bovis BCG.
Ramón-García S, Mick V, Dainese E, Martín C, Thompson CJ, De Rossi E, Manganelli R, Aínsa JA.
Antimicrob Agents Chemother. 2012 Apr;56(4):2074-83. doi: 10.1128/AAC.05946-11.
PMID: 22232275

A prodrug approach for improving antituberculosis activity of potent Mycobacterium tuberculosis type II dehydroquinase inhibitors.
Tizón L, Otero JM, Prazeres VF, Llamas-Saiz AL, Fox GC, van Raaij MJ, Lamb H, Hawkins AR, Aínsa JA, Castedo L, González-Bello C.
J Med Chem. 2011 Sep 8;54(17):6063-84. doi: 10.1021/jm2006063.
PMID: 21780742

Antimycobacterial evaluation and preliminary phytochemical investigation of selected medicinal plants traditionally used in Mozambique.
Luo X, Pires D, Aínsa JA, Gracia B, Mulhovo S, Duarte A, Anes E, Ferreira MJ.
J Ethnopharmacol. 2011 Sep 1;137(1):114-20. doi: 10.1016/j.jep.2011.04.062.
PMID: 21571059

Inhibition of drug efflux in mycobacteria with phenothiazines and other putative efflux inhibitors.
Rodrigues L, Aínsa JA, Amaral L, Viveiros M.
Recent Pat Antiinfect Drug Discov. 2011 May;6(2):118-27. doi: 10.2174/157489111796064579.
PMID: 21517739

Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone.
Familiar O, Munier-Lehmann H, Aínsa JA, Camarasa MJ, Pérez-Pérez MJ.
Eur J Med Chem. 2010 Dec;45(12):5910-8. doi: 10.1016/j.ejmech.2010.09.056.
PMID: 20951473

The complex whiJ locus mediates environmentally sensitive repression of development of Streptomyces coelicolor A3(2).
Aínsa JA, Bird N, Ryding NJ, Findlay KC, Chater KF.
Antonie Van Leeuwenhoek. 2010 Aug;98(2):225-36. doi: 10.1007/s10482-010-9443-3.
PMID: 20405209

Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
Ramón-García S, Martín C, Thompson CJ, Aínsa JA.
Antimicrob Agents Chemother. 2009 Sep;53(9):3675-82. doi: 10.1128/AAC.00550-09.
PMID: 19564371

Transcriptional analysis of and resistance level conferred by the aminoglycoside acetyltransferase gene aac(2′)-Id from Mycobacterium smegmatis.
Mick V, Rebollo MJ, Lucía A, García MJ, Martín C, Aínsa JA.
J Antimicrob Chemother. 2008 Jan;61(1):39-45. doi: 10.1093/jac/dkm440.
PMID: 18032424

Contribution of the Rv2333c efflux pump (the Stp protein) from Mycobacterium tuberculosis to intrinsic antibiotic resistance in Mycobacterium bovis BCG.
Ramón-García S, Martín C, De Rossi E, Aínsa JA.
J Antimicrob Chemother. 2007 Mar;59(3):544-7. doi: 10.1093/jac/dkl510.
PMID: 17242035

Novel streptomycin resistance gene from Mycobacterium fortuitum.
Ramón-García S, Otal I, Martín C, Gómez-Lus R, Aínsa JA.
Antimicrob Agents Chemother. 2006 Nov;50(11):3920-2. doi: 10.1128/AAC.00223-06.
PMID: 16954315

Role of mycobacterial efflux transporters in drug resistance: an unresolved question.
De Rossi E, Aínsa JA, Riccardi G.
FEMS Microbiol Rev. 2006 Jan;30(1):36-52. doi: 10.1111/j.1574-6976.2005.00002.x.
PMID: 16438679

Characterization of tetracycline resistance mediated by the efflux pump Tap from Mycobacterium fortuitum.
Ramón-García S, Martín C, Aínsa JA, De Rossi E.
J Antimicrob Chemother. 2006 Feb;57(2):252-9. doi: 10.1093/jac/dki436.
PMID: 16373429

The multidrug transporters belonging to major facilitator superfamily in Mycobacterium tuberculosis.
De Rossi E, Arrigo P, Bellinzoni M, Silva PA, Martín C, Aínsa JA, Guglierame P, Riccardi G.
Mol Med. 2002 Nov;8(11):714-24.
PMID: 12520088

Molecular approaches to tuberculosis.
Aínsa JA, Martín C, Gicquel B.
Mol Microbiol. 2001 Oct;42(2):561-70. doi: 10.1046/j.1365-2958.2001.02652.x.
PMID: 11703676

Characterization of P55, a multidrug efflux pump in Mycobacterium bovis and Mycobacterium tuberculosis.
Silva PE, Bigi F, Santangelo MP, Romano MI, Martín C, Cataldi A, Aínsa JA.
Antimicrob Agents Chemother. 2001 Mar;45(3):800-4. doi: 10.1128/AAC.45.3.800-804.2001.
PMID: 11181364

WhiA, a protein of unknown function conserved among gram-positive bacteria, is essential for sporulation in Streptomyces coelicolor A3(2).
Aínsa JA, Ryding NJ, Hartley N, Findlay KC, Bruton CJ, Chater KF.
J Bacteriol. 2000 Oct;182(19):5470-8. doi: 10.1128/jb.182.19.5470-5478.2000.
PMID: 10986251

A response regulator-like protein that functions at an intermediate stage of sporulation in Streptomyces coelicolor A3(2).
Aínsa JA, Parry HD, Chater KF.
Mol Microbiol. 1999 Nov;34(3):607-19. doi: 10.1046/j.1365-2958.1999.01630.x.
PMID: 10564501

Molecular cloning and characterization of Tap, a putative multidrug efflux pump present in Mycobacterium fortuitum and Mycobacterium tuberculosis.
Aínsa JA, Blokpoel MC, Otal I, Young DB, De Smet KA, Martín C.
J Bacteriol. 1998 Nov;180(22):5836-43. doi: 10.1128/JB.180.22.5836-5843.1998.
PMID: 9811639

katGI and katGII encode two different catalases-peroxidases in Mycobacterium fortuitum.
Menéndez MC, Aínsa JA, Martín C, García MJ.
J Bacteriol. 1997 Nov;179(22):6880-6. doi: 10.1128/jb.179.22.6880-6886.1997.
PMID: 9371430

Isolation by genetic labeling of a new mycobacterial plasmid, pJAZ38, from Mycobacterium fortuitum.
Gavigan JA, Aínsa JA, Pérez E, Otal I, Martín C.
J Bacteriol. 1997 Jul;179(13):4115-22. doi: 10.1128/jb.179.13.4115-4122.1997.
PMID: 9209023

Aminoglycoside 2′-N-acetyltransferase genes are universally present in mycobacteria: characterization of the aac(2′)-Ic gene from Mycobacterium tuberculosis and the aac(2′)-Id gene from Mycobacterium smegmatis.
Aínsa JA, Pérez E, Pelicic V, Berthet FX, Gicquel B, Martín C.
Mol Microbiol. 1997 Apr;24(2):431-41. doi: 10.1046/j.1365-2958.1997.3471717.x.
PMID: 9159528

Construction of a family of Mycobacterium/Escherichia coli shuttle vectors derived from pAL5000 and pACYC184: their use for cloning an antibiotic-resistance gene from Mycobacterium fortuitum.
Aínsa JA, Martín C, Cabeza M, De la Cruz F, Mendiola MV.
Gene. 1996 Oct 17;176(1-2):23-6. doi: 10.1016/0378-1119(96)00202-8.
PMID: 8918226

Characterization of the chromosomal aminoglycoside 2′-N-acetyltransferase gene from Mycobacterium fortuitum.
Aínsa JA, Martin C, Gicquel B, Gomez-Lus R.
Antimicrob Agents Chemother. 1996 Oct;40(10):2350-5. doi: 10.1128/AAC.40.10.2350.
PMID: 8891143

J.A. Gonzalo Asensio; S. Samper Blasco; J.A. Aínsa; I. Otal Gil; C. Martín Montañés.
Los Retos de la Erradicación de la Tuberculosis en el Siglo XXI.
En: Aplicación de la Biotecnología en la Ciencia Veterinaria. pp. 117 – 134. 2012. ISBN 978-84-7867-202-8

P.E.A. Silva; J.A. Aínsa.
Drugs and drug interactions.
En: Tuberculosis 2007: From Basic Science to Patient Care. pp. 593 – 634. 2007.
Bernd Sebastian Kamps (ed), www.tuberculosistextbook.com

J. Content; M. Braibant; N.D. Connel; J.A. Aínsa.
Transport processes.
En: Tuberculosis and the Tubercle Bacillus. pp. 379 – 401. 2004. ISBN 1-55581-295-3
ST Cole, KD Eisenach, DN McMurray, WR Jacobs-Jr, (eds). American Society for Microbiology Press, Washington D.C., USA

J.A. Aínsa; C. Martín.
Molecular basis of aminoglycoside resistance in Mycobacterium
En: Recent Research Developments in Antimicrobial Agents & Chemotherapy 4, (I): 1-10. 2000.
Research Signpost, Trivandrum, India.