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Relevant publications

 

All publications shall include the following statement to indicate that said foreground was generated with the assistance of financial support from the Community:

 

The research leading to these results has received funding from the European Community's Seventh Framework Programme [FP7-2007-2013] under grant agreement n° HEALTH-F2-2011-256986–project acronym PANACREAS.

 

  1. Alvarez R, Puebla MP, Díaz JF, Bento AC, García-Navas R, de la Iglesia-Vicente J, Mollinedo F, Andreu JM, Medarde M, and Pelaez R (2013). Endowing indole-based tubulin inhibitors with an anchor for derivatization: highly potent 3-substituted indolephenstatins and indoleisocombretastatins. Journal of Medicinal Chemistry 56, 2813-2827.
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  2. Bai J, Zambron BK, Vogel P. (2014) Amides in One-pot from Carboxylic Acids and Amines via Sulfinylamides.
    Organic Letters 16, 604-607.
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  3. K. Bum-Erdene, I. A. Gagarinov, P. M. Collins, M. Winger, A. G. Pearson, J. C. Wilson, H. Leffler, U. J. Nilsson, I. D. Grice, and H. Blanchard. Investigation into the feasibility of thioditaloside as a novel scaffold for galectin-3 specific inhibitors. ChemBioChem, 2013, 14, 1331-1342.
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  4. Inga Bauer,  Alessia Grozio, Denise Lasiglie',  Giovanna Basile,  Laura Sturla,  Mirko Magnone, Giovanna Sociali,  Debora Soncini,  Irene Caffa,  Alessandro Poggi,  Gabriele Zoppoli,  Michele Cea,  Georg Feldmann,  Raul Mostoslavsky,  Alberto Ballestrero,  Franco Patrone,  Santina Bruzzone, and  Alessio Nencioni (2012). The NAD+-dependent histone deacetylase SIRT6 promotes cytokine production and migration in pancreatic cancer cells by regulating Ca2+ responses. J. Biol. Chem. 287 (49), 40924-40937.
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  5. Bisht S, Feldmann G, Brossart P (2013). Pharmacokinetics and pharmacodynamics of sunitinib for the treatment of advanced pancreatic neuroendocrine tumors. Expert Opin Drug Metab Toxicol. Jun;9(6):777-88.
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  6. Bello C, Dal Bello G, Cea M, Nahimana A, Aubry D, Garuti A, Motta G, Moran E, Fruscione F, Pronzato P, Grossi F, Patrone F, Ballestrero A, Dupuis M, Sordat B, Zimmermann K, Loretan J, Wartmann M, Duchosal M, Nencioni A, Vogel P (2011). Anti-cancer activity of 5-O-alkyl 1,4-imino-1,4-dideoxyribitols. Bioorg. Med. Chem. 19, 7720-7727.
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  7. Bonilla X, EL-Habib Dakir EL-H, Mollinedo F, Gajate C (2015). Endoplasmic reticulum targeting in Ewing’s sarcoma by the alkylphospholipid analog edelfosine. Oncotarget 6, 14596-14613.
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  8. Breton CS, Aubry D, Ginet V, Puyal J, Heulot M, Widmann C, Duchosal MA, Nahimana A (2015). Combinative effects of β-Lapachone and APO866 on pancreatic cancer cell death through reactive oxygen species production and PARP-1 activation. Biochimie, 116:141-53.
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  9. Bruzzone S, Parenti MD, Grozio A, Ballestrero A, Bauer I, Del Rio A, Nencioni A (2013). Rejuvenating sirtuins: the rise of a new family of cancer drug targets.
    Curr Pharm Dec 19, 614-23, 2013.
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  10. Caffa I, D'Agostino V, Damonte P, Soncini D, Cea M, Monacelli F, Odetti P, Ballestrero A, Provenzani A, Longo VD, Nencioni A (2015). Fasting potentiates the anticancer activity of tyrosine kinase inhibitors by strengthening MAPK signaling inhibition. Oncotarget 20;6(14):11820-32.
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  11. Cagnetta A, Caffa I, Acharya C, Soncini D, Acharya P, Adamia S, Pierri I, Bergamaschi M, Garuti A, Fraternali G, Mastracci L, Provenzani A, Zucal C, Damonte G, Salis A, Montecucco F, Patrone F, Ballestrero A, Bruzzone S, Gobbi M, Nencioni A, Cea M. (2015). APO866 increases anti-tumor activity of cyclosporin-A by inducing mitochondrial and endoplasmic reticulum stress in leukemia cells. Clin Cancer Res. 21(17):3934-45.
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  12. Cuesta-Marbán A, Botet J, Czyz O, Cacharro LM, Gajate C, Hornillos V, Delgado J, Zhang H, Amat-Guerri F, Acuña AU, McMaster CR, Revuelta JL, Zaremberg V, and Mollinedo F (2013). Drug uptake, lipid rafts and vesicle trafficking modulate resistance to an anticancer lysophosphatidylcholine analogue in yeast.
    Journal of Biological Chemistry 288, 8405-8418.
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  13. Czyz O, Bitew T, Cuesta-Marbán A, McMaster CR, Mollinedo F, and Zaremberg V (2013). Alteration of plasma membrane organization by an anticancer lysophosphatidylcholine analogue induces intracellular acidification and internalization of plasma membrane transporters in yeast.
    Journal of Biological Chemistry 288, 8419-8432.
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  14. D’Adamio G, Parmeggian C, Goti A, Moreno-Vargas A, Moreno-Clavijo E, Robina I, Cardona F (2014). 6-Azido hyacinthacine A2 gives a straightforward access to the first multivalent pyrrolizidine architectures.
    Org. Biomol. Chem. 12, 6250-6266.
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  15. Fendrich V, Oh E, Bang S, Karikari C, Ottenhof N, Bisht S, Lauth M, Brossart P, Katsanis N, Maitra A, Feldmann G (2011). Ectopic overexpression of Sonic Hedgehog (Shh) induces stromal expansion and metaplasia in the adult murine pancreas. Neoplasia Oct;13(10): 923-30.
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  16. Feldmann G, Mishra A, Bisht S, Karikari C, Garrido-Laguna I, Rasheed Z, Ottenhof NA, Dadon T, Alvarez H, Fendrich V, Rajeshkumar NV, Matsui W, Brossart P, Hidalgo M, Bannerji R, Maitra A, Nelkin BD (2011). Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft  models.
    Cancer Biol Ther Oct 1;12(7):598-609.
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  17. Feldmann G, Bisht S, Schütte U, Haarmann J, Brossart P (2012). Everolimus for the treatment of pancreatic neuroendocrine tumors. Expert Opin Pharmacother. Oct;13(14):2073-84.
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  18. Feldmann G, Brossart P, Zipfel M, von Lilienfeld-Toal M (2013).Mixed response to ipilimumab in a melanoma patient with brain metastases: case report and review of the literature. Case Rep Oncol. Apr 20;6(1):229-35.
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  19. Feldmann G, Brossart P, von Lilienfeld-Toal M (2013). Transient and fully reversible leukocytosis in a myelodysplastic syndrome patient upon initiation of azacitidine treatment. Ann Hematol. Nov; 92 (11):1577-9.

  20. Garcia-Navas R, Munder M, and Mollinedo F (2012). Depletion of L-arginine induces autophagy as a cytoprotective response to endoplasmic reticulum stress in human T lymphocytes. Autophagy 8, 1557-1576.
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  21. Gajate C and Mollinedo F (2011).  Lipid rafts and Fas/CD95 signaling in cancer chemotherapy.
    Recent Patents on Anticancer Drug Discovery 6, 274-283.
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  22. Gajate C, Matos-da-Silva M, Dakir EL-H, Fonteriz RI, Alvarez J, and Mollinedo F  (2012). Antitumor alkyl-lysophospholipid analogue edelfosine induces apoptosis in pancreatic cancer by targeting endoplasmic reticulum. Oncogene 31: 2627-39. Featured Article.
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  23. Gajate C and Mollinedo F (2014). Lipid rafts, endoplasmic reticulum and mitochondria in the antitumor action of the alkylphospholipid analog edelfosine. Anti-Cancer Agents in Medicinal Chemistry 14, 509-527.
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  24. Gajate C and Mollinedo F (2015). Lipid rafts and raft-mediated supramolecular entities in the regulation of CD95 death receptor apoptotic signaling. Apoptosis 20, 584-606.
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  25. Gajate C and Mollinedo F (2015). Lipid raft-mediated Fas/CD95 apoptotic signaling in leukemic cells and normal leukocytes and therapeutic implications. Journal of Leukocyte Biology 98, 739-759.
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  26. Gillig A, Majjigapu SR, Sordat, B. Vogel P (2012). Synthesis of a C-Iminoribofuranoside Analog of the Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitor FK866. Helv. Chem. Acta 95, 34-42 (most read article of this journal in 2012).
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  27. Ginet V, Puyal J, Rummel C, Aubry D, Breton C, Cloux AJ, Majjigapu SR, Sordat B, Vogel P, Bruzzone S, Nencioni A, Duchosal MA, Nahimana A (2014). A critical role of autophagy in antileukemia/lymphoma effects of APO866, an inhibitor of NAD biosynthesis. Autophagy. Apr;10(4):603-17.
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  28. Grozio A, Sociali G, Sturla L, Caffa I, Soncini D, Salis A, Raffaelli N, De Flora A, Nencioni A, Bruzzone S (2013). CD73 protein as a source of extracellular precursors for sustained NAD+ biosynthesis in FK866-treated tumor cells.
    J Biol Chem. 288, 25938-49, 2013.
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  29. Hottin A, Carrión-Jiménez S, Moreno-Clavijo E, Moreno-Vargas AJ, Carmona AT, Robina I and Behr JB (2016). Expanding the library of divalent fucosidase inhibitors with polyamino and triazole-benzyl bridged bispyrrolidines.
    Org. Biomol. Chem. 14, 3212-3220.
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  30. Legembre P and Mollinedo F (2011). The plasma membrane: a catalyst in the decision to die or not to die?
    Recent Patents on Anticancer Drug Discovery 6, 271-273.
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  31. Lepur A, Carlsson MC, Novak R, Dumić J, Nilsson UJ, Leffler H. (2012). Galectin-3 endocytosis by carbohydrate independent and dependent pathways in different macrophage like cell types.
    Biochim Biophys Acta. Jul;1820(7):804-18.
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  32. Lepur A, Salomonsson E, Nilsson UJ, Leffler H (2012). Ligand induced galectin-3 protein self-association.
    J Biol Chem. Jun 22;287(26):21751-6.
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  33. Magnone M, Nencioni A, Bruzzone S (2015). NAD+ Levels Control T Cell Calcium Signaling and Activation (2015). Messenger 4, 1-6.
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  34. Mandal S and Nilsson UJ (2014). Tri-isopropylsilyl thioglycosides as masked glycosyl thiol nucleophiles for the synthesis of S-linked glycosides and glyco-conjugates. Org. Biomol. Chem. 12, 4816-4819.
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  35. Mandal S, Rajput VK, Leffler H, Mukhopadhyay B, Nilsson UJ (2016). Galactose-amidine derivatives as selective antagonists of galectin-9. Can. J. Chem., in press: DOI:10.1139/cjc-2015-0598.
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  36. Matassini C, Mirabella S, Ferhati X, Faggi C, Robina I, Goti A, Moreno-Clavijo E, Moreno-Vargas AJ and Cardona F (2014). Polyhydroxyamino piperidine iminosugars and pipecolic acid analogs from a D-mannose derived aldehyde.
    Eur. J. Org. Chem. 5419–5432.
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  37. Melo-Lima S, Lopes MC and Mollinedo F (2014). Necroptosis is associated with low procaspase-8 and active RIPK1 and -3 in human glioma cells. Oncoscience 1, 649-664. The cover of the journal was given to this manuscript.
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  38. Melo-Lima, S, Lopes MC and Mollinedo F (2015). ERK1/2 acts as a switch between necrotic and apoptotic cell death in ether phospholipid edelfosine-treated glioblastoma cells. Pharmacological Research 95-96, 2-11.
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  39. Mollinedo F, Fernández M, Hornillos V, Delgado J, Amat-Guerri F, Acuña AU, Nieto-Miguel T, Villa-Pulgarín JA, González-García C, Ceña V, and Gajate C (2011). Involvement of lipid rafts in the localization and dysfunction effect of the antitumor ether phospholipid edelfosine in mitochondria. Cell Death & Disease 2:e158.
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  40. Mollinedo F, and Gajate C (2012). Lipid rafts, cholesterol and apoptosis in cancer and neurodegenerative diseases. In "A Toxicological/Pharmacological Approach to Chemico-Biological Interactions at a Membrane Level" (Jurado, A.S., Pedroso, M.C., and de Almeida, L., eds), pp. 27-40, Research Signpost, Transworld Research Network, Kerala, India. ISBN: 978-81-308-0494-1.

  41. Mollinedo F (2012). Lipid raft involvement in yeast cell growth and death. Frontiers in Oncology 22, e140.
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  42. Mollinedo F (2014). Antitumor alkylphospholipid analogs: a promising and growing family of synthetic cell membrane-targeting molecules for cancer treatment. Anti-Cancer Agents in Medicinal Chemistry 14, 495-498.
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  43. Mollinedo F and Gajate C (2015). Lipid rafts as major platforms for signaling regulation in cancer.
    Advances in Biological Regulation 57, 130-146.
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  44. Montecucco F, Cea M, Bauer I, Soncini D, Caffa I, Lasigliè D, Nahimana A, Uccelli A, Bruzzone S, Nencioni A. (2013). Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors As Therapeutics: Rationales, Controversies, Clinical Experience. Curr Drug Targets. Jun 1;14(6):637-43.
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  45. Moreno-Clavijo E, Carmona AT, Moreno-Vargas AJ, Molina L, Wright DW, Davies GJ, Robina I. Exploring a Multivalent Approach on α-L-Fucosidase Inhibition. Eur. J. Org. Chem. 7328-7336.
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  46. Moreno-Clavijo E, Moreno-Vargas AG, Carmona AT, Robina I (2013). Strain promoted retro-Dieckmann-Type Condensation on [2.2.2]- and [2.2.1]bicyclic Systems: a Fragmentation Reaction for the Preparation of Functionalized Heterocycles and Carbocycles. Org. Biomol. Chem. 11, 7016-7025.
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  47. Nischalke HD, Schmitz V, Luda C, Aldenhoff K, Berger C, Feldmann G, Sauerbruch T, Spengler U, Nattermann J (2012). Detection of IGF2BP3, HoxB7, and NEK2 mRNA expression in brush cytology specimens as a new diagnostic tool in patients with biliary strictures. PLOS one 2012;7(8):e42141. Epub 2012 Aug 7.
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  48. Palomero Rodríguez MÁ, García Navas R, Laporta Báez Y, de Vicente Sánchez J, Moyano Maza JC, Rodríguez López JM, Sánchez Conde MP and Mollinedo F (2015). Arginase activity and CD3ζ expression after major surgery. Intensive Care Med. 41, 939-940.

  49. Reis-Sobreiro M, Roué G, Moros A, Gajate C, De la Iglesia-Vicente J, Colomer D, Mollinedo F (2013). Lipid raft-mediated Akt signaling as a therapeutic target in mantle cell lymphoma. Blood Cancer Journal 3, e118.
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  50. Parenti MD, Grozio A, Bauer I, Galeno L, Damonte P, Millo E, Sociali G, Franceschi C, Ballestrero A, Bruzzone S, Rio AD, Nencioni A (2014). Discovery of Novel and Selective SIRT6 Inhibitors. J Med Chem 57, 4796-804.
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  51. Parenti MD, Bruzzone S, Nencioni A, Del Rio A (2015). Selectivity hot spots of sirtuin catalytic cores.
    Mol. Biosyst. 11:2263-72.
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  52. Peterson K, Weymouth-Wilson A and Nilsson UJ (2015). Aryl sulfonates in inversions at secondary carbohydrate hydroxyls: a new and improved route towards 3-azido-3-deoxy-β-D-galactopyranosides. J. Carbohydr. Chem., 34, 490-499.
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  53. Rajput VK, Leffler H, Nilsson UJ, Mukhopadhyay B (2014). Synthesis and evaluation of iminocoumaryl and coumaryl derivatized glycosides as galectin antagonists. Bioorg. med. Chem. Lett., 24, 3516-3520.
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  54. Pilar ER, Moreno-Clavijo E, Jiménez SC, Carmona AT, Moreno-Vargas AJ, Caffa I, Montecucco F, Cea M, Nencioni A, Robina I (2014). Synthesis and Cancer growth inhibitory activities of 2-Fatty-Alkylated Pyrrolidine-3,4-diol Derivatives. Arkivoc, Part (III) 197-214.
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  55. Rodríguez PE, Moreno-Clavijo E, Carmona AT, Moreno-Vargas AJ, Robina I (2014). Rapid discovery of potent α-fucosidase inhibitors by in situ screening of a library of (pyrrolidin-2-yl)triazoles. Org. Biomol. Chem. 12, 5898-5904.
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  56. Sánchez-Blanco A, Rodríguez-Matellán AG, Reis-Sobreiro M, Sáenz-Narciso B, Cabello J, Mohler WA, Mollinedo F (2014). Caenorhabditis elegans as a platform to study the mechanism of action of synthetic antitumor lipids.
    Cell Cycle 13, 3375-3389.
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  57. Schütte U, Bisht S, Heukamp LC, Kebschull M, Haarmann AFJ, Hoffmann P, Bendas G, Buettner R, Brossart P, Feldmann G (2014). Hippo signaling mediates proliferation, invasiveness and metastatic potential of clear cell renal cell carcinoma. Translational Oncology. Apr;7(2):309-21.
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  58. Sociali G, Galeno L, Parenti MD, Grozio A, Bauer I, Passalacqua M, Boero S, Donadini A, Millo E, Bellotti M, Sturla L, Damonte P, Puddu A, Ferroni C, Varchi G, Franceschi C, Ballestrero A, Poggi A, Bruzzone S, Nencioni A, Del Rio A (2015). Quinazolinedione SIRT6 inhibitors sensitize cancer cells to chemotherapeutics.
    Eur J Med Chem. Sep 18;102:530-9.
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  59. Sociali G, Raffaghello L, Magnone M, Zamporlini F, Emionite L, Sturla L, Bianchi G, Vigliarolo T, Nahimana A, Nencioni A, Raffaelli N, Bruzzone S (2016). Antitumor effect of combined NAMPT and CD73 inhibition in an ovarian cancer model. Oncotarget; 7(3):2968-84
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  60. Soncini D, Caffa I, Zoppoli G, Cea M, Cagnetta A, Passalacqua M, Mastracci L, Boero S, Montecucco F, Sociali G, Lasigliè D, Damonte P, Grozio A, Mannino E, Poggi A, D'Agostino VG, Monacelli F, Provenzani A, Odetti P, Ballestrero A, Bruzzone S, Nencioni A (2014). Nicotinamide phosphoribosyltransferase promotes epithelial-to-mesenchymal transition as a soluble factor independent of its enzymatic activity. J Biol Chem 289, 34189-204.
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  61. Stegmayr J, Lepur A, Kahl-Knutsson B, Aguilar-Moncayo A, Klyosov AA, Fields RA, Oredsson S, Nilsson UJ and Leffler H (2016). Low or No Inhibitory Potency of the Canonical Galectin Carbohydrate Binding Site by Pectins and Galactomannans. J. Biol. Chem., Published on April 26, 2016 as Manuscript M116.721464.

  62. Steimer F, Carmona AT, Moreno-Vargas AJ, Caffa I, Cea M, Montecucco F, Nencioni A, Vogel P, Robina I (2014). Synthesis of Pyrrolidine 3,4-Diol Derivatives with Anticancer Activity on Pancreatic Tumor Cells.
    Heterocycles, 88, 1445-1464.
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  63. Tenzer S, Moro A, Kuharev J, Francis AC, Vidalino L, Provenzani A, Macchi P. Proteome-wide characterization of the RNA-binding protein RALY-interactome using the in vivo-biotinylation-pulldown-quant (iBioPQ) approach. J Proteome Res. 2013 Jun 7;12(6):2869-84.
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  64. Thongon N, Castiglioni I, Zucal C, Latorre E, D’Agostino VG, Bauer I, Pancher M, Ballestrero A, Feldmann G, Nencioni A, Provenzani A. The GSK3β inhibitor BIS I reverts YAP-dependent EMT signature in PDAC cell lines by decreasing SMADs expression level. Oncotarget Mar 28. [Epub ahead of print]
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  65. Varela RE, Villa-Pulgarin JA, Yepes E, Müller I, Modolell M, Muñoz DL, Robledo SM, Muskus CE, López-Abán J, Muro A, Vélez ID, Mollinedo F (2012). In vitro and in vivo efficacy of ether lipid edelfosine against Leishmania spp. and SbV-resistant parasites. PLoS Neglected Tropical Diseases 6(4): 31612.
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  66. Varela-M RE, Mollinedo-Gajate C, Muro A, Mollinedo F (2014). The HSP90 inhibitor 17-AAG potentiates the antileishmanial activity of the ether lipid edelfosine. Acta Tropica 131, 32-36.
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  67. Von Mach T, Carlsson MC, Straube T, Nilsson U, Leffler H, Jacob R. (2014) Ligand binding and complex formation of galectin-3 is modulated by pH variations. Biochem J. 457(1):107-115.
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  68. Yepes E, Varela-M R.E, López-Abán J, Dakir EL-H, Mollinedo F, Muro A (2014). In vitro and in vivo anti-schistosomal activity of the alkylphospholipid analog edelfosine. PLoS ONE 9(10):e109431.
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  69. Yepes E, Varela-M R.E, López-Abán J, Rojas-Caraballo J, Muro A, Mollinedo F (2015). Inhibition of granulomatous inflammation and prophylactic treatment of schistosomiasis with a combination of edelfosine and praziquantel.
    PloS Neglected Tropical Diseases 9(7):e0003893.
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  70. Zambron BK, Dubbaka SR, Markovic D, Moreno-Clavijo E, Vogel P (2013). Amide Formation in One Pot from Carboxylic Acids and Amines via Carboxyl and Sulfinyl Mixed Anhydrides. Org. Lett. 15 (10), pp 25502553.
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  71. Zucal C, D'Agostino VG, Casini A, Mantelli B, Thongon N, Soncini D, Caffa I, Cea M, Ballestrero A, Quattrone A, Indraccolo S, Nencioni A, Provenzani A. (2015). EIF2A-dependent translational arrest protects leukemia cells from the energetic stress induced by NAMPT inhibition. BMC Cancer. 15:855.
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