PRINCIPAL INVESTIGATOR

POSTDOCTORAL RESEARCHERS:

• Miguel X. Fernandes (“Agustín de Betancourt” Researcher, ULL)

PHD STUDENTS AND TRAINEES:

• Adrián Puerta Arocha (Doctorate Program in Health Sciences, PGC2018-094503-B-C22, MCIU/AEI/FEDER, UE)
• Alexis Galán Rodríguez (Doctorate Program in Chemistry, PGC2018-094503-B-C22, MCIU/AEI/FEDER, UE)
• Amina Moutayakine (Doctorate Program in Chemistry, PGC2018-094503-B-C22, MCIU/AEI/FEDER, UE)
• Alicia Hernández Pérez (Doctorate Program in Health Sciences, Doctorado Industrial, Orfan Biotech SL)

RESEARCH LINES:

• Drug discovery: Early identification of the therapeutic targets of biologically active molecules. The identification of the biological targets with which the small molecules interact is determined based on phenotypic and in silico experimental data. Once the biological target has been predicted, the process to validate it goes through the confirmation of the activity of the compound on the proposed target. The next step involves studying the effect in live models, when the compound gains added value and the viability of its technology transfer is evaluated.
• Bioprospecting of marine and terrestrial resources. The search for new bioactive compounds from natural sources has been motivated by the increase in the worldwide incidence of various types of cancer and the emergence of pathogens resistant to the available antibiotics. Our institute participates in the bioprospecting of marine and terrestrial resources in our region, Latin America, Africa and Asia in order to access substances of interest to the pharmaceutical, cosmetic, food or veterinary industries.
• Design and synthesis of molecular probes. The fluorescent probes used in immunofluorescence techniques are usually antibodies. However, anchoring a fluorescent group to a small molecule by derivatisation facilitates cell localization studies. Based on the results of structure-function studies, we can define the site in the reference molecule where a fluorescent fragment can be introduced.

FUNDED PROJECTS:

• Preparation of the MSC-ITN action “Multitargeted therapies against pancreatic ductal adenocarcinoma (PANCNET, EIN2019-102928) PI: José M. Padrón (01/06/2019 to 31/05/2021, 16,200 €).
• Inhibition of glutamine metabolism as therapy against pancreatic ductal adenocarcinoma («Inhibición del metabolismo de la glutamina como terapia contra el adenocarcinoma ductal pancreático. «Agustín de Betancourt») project. PI: Miguel X. Fernandes; IP-ULL: José M. Padrón. Regional Government of Tenerife (2018-2022, 160,000 €).

PUBLICACTIONS 2019:

• Filipović NR, Ristić P, Janjić G, Klisuric O, Padron JM, Donnard M, Gulea M, Todorović TR. Silver-based monomer and coordination polymer with organic thiocyanate ligand: Structural, computational and antiproliferative activity study. 2019 Polyhedron 173,114132 doi: 10.1016/j.poly.2019.114132
• Sánchez-Fernández EM, García-Moreno MI, Arroba AI, Aguilar-Diosdado M, Padrón JM, García-Hernández R, Gamarro F, Fustero S, Sánchez-Aparicio J-E, Masgrau L, García Fernández JM, Ortiz Mellet C. Synthesis of polyfluoroalkyl SP2-iminosugar glycolipids and evaluation of their immunomodulatory properties towards anti-tumor, anti-leishmanial and anti-inflammatory therapies. 2019 European Journal of Medicinal Chemistry 182,111604. doi: 10.1016/j.ejmech.2019.111604
• Roldán-Peña JM,Romero-Real V,Hicke J,Maya I,Franconetti A,Lagunes I,PadrónJM, Petralla S,Poeta E,Naldi M,Bartolini M,Monti B,Bolognesi ML,López Ó,Fernández-Bolaños JG.Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer’s disease: Selective subnanomolar BuChE inhibitors. 2019 Eur J Med Chem. 2019 Nov 1;181:111550. doi: 10.1016/j.ejmech.2019.07.053
• Cortés-Percino A,Vega-Báez JL,Romero-López A,Puerta A,Merino-Montiel P,Meza-Reyes S,Padrón JM, Montiel-Smith S. Synthesis and evaluation of pyrimidine steroids as antiproliferative agents. 2019 Oct 12;24(20). pii: E3676. doi: 10.3390/molecules24203676
• Ingold M,Colella L,Hernández P,Batthyány C,Tejedor D,Puerta A,García-Tellado F, Padrón JM,Porcal W,López GV.A Focused Library of NO-Donor Compounds with Potent Antiproliferative Activity Based on Green Multicomponent Reactions. 2019 Sep 18;14(18):1669-1683. doi: 10.1002/cmdc.201900385
• Sánchez-Fernández EM,García-Moreno MI,García-Hernández R,PadrónJM,García Fernández JM,Gamarro F,Ortiz Mellet C. Thiol-ene “click” synthesis and pharmacological evaluation of C-glycoside SP2-iminosugar glycolipids. 2019 Aug 8;24(16). pii: E2882. doi: 10.3390/molecules24162882
• Sánchez-Tafolla L, Padrón JM, Mendoza G, Luna-Rodríguez M, Fernández JJ, Norte M, Trigos Á. Antiproliferative activity of biomass extract from Pseudomonas cedrina. 2019 Electronic Journal of Biotechnology 40, pp. 40-44. doi: 10.1016/j.ejbt.2019.03.010
• Castillo QA, Padrón JM, Wojtas L, Keramane M, Germosén EA. Koanolide A, antiproliferative germacrane-type sesquiterpene lactone from Koanophyllon gibbosum. 2019 Tetrahedron Letters 60(25), pp. 1640-1642. doi: 10.1016/j.tetlet.2019.05.036
• Luque-Agudo V,Albarrán-Velo J,Light ME,Padrón JM,Román E,Serrano JA, Gil Synthesis and antiproliferative activity of new 2-glyco-3-nitro-2H-chromenes. Bioorg Chem. 2019 Jun;87:112-116. doi: 10.1016/j.bioorg.2019.03.016
• Castro SJ,Casero CN,Padrón JM,Nicotra VE.Selective Antiproliferative Withanolides from Species in the Genera Eriolarynx and Deprea. J Nat 2019 May 24;82(5):1338-1344. doi: 10.1021/acs.jnatprod.9b00117
• Patel DM,Sharma MG,Vala RM,Lagunes I,Puerta A,Padrón JM,Rajani DP,PatelHydroxyl alkyl ammonium ionic liquid assisted green and one-pot regioselective access to functionalized pyrazolodihydropyridine core and their pharmacological evaluation. Bioorg Chem. 2019 May;86:137-150. doi: 10.1016/j.bioorg.2019.01.029
• Hamulić D,Stadler M,Hering S,Padrón JM,Bassett R,Rivas F,Loza-Mejía MA, Dea-Ayuela MA,González-Cardenete MA.Synthesis and Biological Studies of (+)-Liquiditerpenoic Acid A (Abietopinoic Acid) and Representative Analogues: SAR Stud J Nat Prod. 2019 Apr 26;82(4):823-831. doi: 10.1021/acs.jnatprod.8b00884
• Beer MF,Bivona AE,Sánchez Alberti A,Cerny N,Reta GF,Martín VS,PadrónJM, Malchiodi EL,Sülsen VP,Donadel OJ.Preparation of sesquiterpene lactone derivatives: Cytotoxic activity and selectivity of action. 2019 Mar 20;24(6). pii: E1113. doi: 10.3390/molecules24061113
• Padrón JM, Emiliano A, Castillo QA. Secondary Metabolites from Pterocaulon alopecuroides and their Antiproliferative Activities. 2019 Pharmacognosy Journal 11(3), pp. 493-495. doi: 10.5530/pj.2019.11.78
• Franceschy C,Espinoza C, Padrón JM,Landa-Cadena G,Norte M,Fernández JJ, Shnyreva A,Trigos Á. Antiproliferative potential of 3β,5α,6β,7α- tetrahydroxyergosta-8(14),22-diene produced by Acremonium persicinum isolated from an alkaline crater lake in Puebla, Mexico. Nat Prod Res. 2019 Sep 26:1-4. doi: 10.1080/14786419.2019.1669032. [Epub ahead of print]
• Brahmbhatt GC,Sutariya TR,Atara HD,Parmar NJ,Gupta VK,Lagunes I,PadrónJM, Murumkar PR,Yadav MR. New pyrazolyl-dibenzo[b,e][1,4]diazepinones: room temperature one-pot synthesis and biological evaluation. Mol Divers. 2019 May 24. doi: 10.1007/s11030-019-09958-z. [Epub ahead of print]
• Lagunes I, Begines P, Silva A, Galán AR, Puerta A, Fernandes MX, Maya I, Fernández-Bolaños JG, López Ó, Padrón JM. Selenocoumarins as new multitarget antiproliferative agents: Synthesis, biological evaluation and in silico calculations. Eur J Med Chem. 2019 Oct 1;179:493-501. doi: 10.1016/j.ejmech.2019.06.073
• Dinić J, Ríos-Luci C, Karpaviciene I, Cikotiene I, Fernandes MX, Pešić M, Padrón JM. CKT0353, a novel microtubule targeting agent, overcomes paclitaxel induced resistance in cancer cells. Invest New Drugs. 2019 Jun 8. doi: 10.1007/s10637-019- 00803-6. [Epub ahead of print]
• Rodriguez-Rodriguez AE, Donate-Correa J, Rovira J, Cuesto G, Luis-Ravelo D, Fernandes MX, Acevedo-Arozena A, Diekmann F, Acebes A, Torres A, Porrini E. Inhibition of the mTOR pathway: A new mechanism of β cell toxicity induced by Tacrolimu Am J Transplant. 2019 Dec;19(12):3240-3249. doi: 10.1111/ajt.15483
• Serina J, Fernandes MX, Castilho PC. Effects of hydroxycinnamic acids on the glycolysis pathway. 2019 South African Journal of Botany 120, pp. 219-229. doi: 10.1016/j.sajb.2018.06.016
• Other selected publications from the last 10 years:
• Podolski-Renić A,Banković J,Dinić J,Ríos-Luci C,Fernandes MX,OrtegaN,Kovačević-Grujičić N, Martín VS,Padrón JM, Pešić M. DTA0100, dual topoisomerase II and microtubule inhibitor, evades paclitaxel resistance in P- glycoprotein overexpressing cancer cells. Eur J Pharm Sci. 2017 Jul 15;105:159-168. doi: 10.1016/j.ejps.2017.05.011
• Silveira-Dorta G, Sousa IJ, Fernandes MX, Martín VS, Padrón JM. Synthesis and identification of unprecedented selective inhibitors of CK1ε. Eur J Med 2015;96:308-17. doi: 10.1016/j.ejmech.2015.03.046
• Silveira-Dorta G, Martín VS, Padrón JM. Synthesis and antiproliferative activity of glutamic acid-based dipeptides. Amino Acids. 2015 Aug;47(8):1527-32. doi: 10.1007/s00726-015-1987-0