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Thomas van Leeuwen, Luca Buzzetti, Luca Alessandro Perego, Paolo Melchiorre
We report a simple protocol for the photochemical Giese addition of C(sp3)-centered radicals to a variety of electron-poor olefins. The chemistry does not require external photoredox catalysts. Instead, it harnesses the excited-state reactivity of 4-alkyl-1,4-dihydropyridines (4-alkyl-DHPs) to generate alkyl radicals. Crucial for reactivity is the use of a catalytic amount of Ni(bpy)32+ (bpy = 2,2'-bipyridyl), which acts as an electron mediator to facilitate the redox processes involving fleeting and highly reactive intermediates...
February 12, 2019: Angewandte Chemie
Bertrand Schweitzer-Chaput, Matthew A Horwitz, Eduardo de Pedro Beato, Paolo Melchiorre
Chemists extensively use free radical reactivity for applications in organic synthesis, materials science, and life science. Traditionally, generating radicals requires strategies that exploit the bond dissociation energy or the redox properties of the precursors. Here, we disclose a photochemical catalytic approach that harnesses different physical properties of the substrate to form carbon radicals. We use a nucleophilic dithiocarbamate anion catalyst, adorned with a well-tailored chromophoric unit, to activate alkyl electrophiles via an SN 2 pathway...
February 2019: Nature Chemistry
Giuseppa Augello, Maria Rita Emma, Antonella Cusimano, Antonina Azzolina, Sarah Mongiovì, Roberto Puleio, Giovanni Cassata, Alessandro Gulino, Beatrice Belmonte, Roberto Gramignoli, Stephen C Strom, James A McCubrey, Giuseppe Montalto, Melchiorre Cervello
Hepatocellular carcinoma (HCC) is a highly malignant tumor that responds very poorly to existing therapies, most probably due to its extraordinary inter- and intra-tumor molecular heterogeneity. The modest therapeutic response to molecular targeted agents underlines the need for new therapeutic approaches for HCC. In this study, we took advantage of well-characterized human HCC cell lines, differing in transcriptomic subtypes, DNA mutation and amplification alterations, reflecting the heterogeneity of primary HCCs, to provide a preclinical evaluation of the specific heat shock protein 90 (HSP90) inhibitor AUY922 (luminespib)...
November 29, 2018: International Journal of Cancer. Journal International du Cancer
Leonardo Dini, Martina Del Lungo, Francesco Resta, Michele Melchiorre, Valentina Spinelli, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Annunziatina Laurino, Laura Sartiani, Raffaele Coppini, Guido Mannaioni, Elisabetta Cerbai, Maria Novella Romanelli
A prominent role of hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels has been suggested based on their expression and (dys)function in dorsal root ganglion (DRG) neurons, being likely involved in peripheral nociception. Using HCN blockers as antinociceptive drugs is prevented by the widespread distribution of these channels. However, tissue-specific expression of HCN isoforms varies significantly, HCN1 and HCN2 being considered as major players in DRG excitability. We characterized the pharmacological effect of a novel compound, MEL55A, able to block selectively HCN1/HCN2 isoforms, on DRG neuron excitability in-vitro and for its antiallodynic properties in-vivo ...
2018: Frontiers in Pharmacology
Maria Gabriella Melchiorre, Giovanni Lamura, Francesco Barbabella
BACKGROUND: People with multimorbidity, especially older people, have complex health and social needs, and require an integrated care approach. In this respect, eHealth could be of support. This paper aims to describe the implementation of eHealth technologies in integrated care programs for people with multimorbidity in Europe, and to analyse related benefits and barriers according to outcomes from ICARE4EU study and within the more general conceptual framework of the "10 e's" in eHealth by Gunther Eysenbach...
2018: PloS One
Giulio Goti, Bartosz Bieszczad, Alberto Vega-Peñaloza, Paolo Melchiorre
We report a visible-light-mediated organocatalytic strategy for the enantioselective acyl radical conjugate addition to enals, leading to valuable 1,4-dicarbonyl compounds. The process capitalizes upon the excited-state reactivity of 4-acyl-1,4-dihydropyridines that, upon visible-light absorption, can trigger the generation of acyl radicals. By means of a chiral amine catalyst, iminium ion activation of enals ensures a stereoselective radical trap. We also demonstrate how the combination of this acylation process with a second catalyst-controlled bond-forming event allows to selectively access the full matrix of all possible stereoisomers of the resulting 2,3-substituted 1,4-dicarbonyl products...
November 12, 2018: Angewandte Chemie
Stephen L Abrams, Matilde Y Follo, Linda S Steelman, Kvin Lertpiriyapong, Lucio Cocco, Stefano Ratti, Alberto M Martelli, Saverio Candido, Massimo Libra, Ramiro M Murata, Pedro L Rosalen, Giuseppe Montalto, Melchiorre Cervello, Agnieszka Gizak, Dariusz Rakus, Weifeng Mao, Paolo Lombardi, James A McCubrey
Berberine (BBR) is a common nutraceutical consumed by millions worldwide. BBR has many different effects on human health, e.g., diabetes, diarrhea, inflammation and now more recently it has been proposed to have potent anti-cancer effects. BBR has been shown to suppress the growth of cancer cells more than normal cells. BBR has been proposed to exert its growth-inhibitory effects by many different biochemical mechanisms including: suppression of cell cycle progression, induction of reactive oxygen species, induction of apoptosis and autophagy and interactions with DNA potentially leading to DNA damage, and altered gene expression...
October 17, 2018: Advances in Biological Regulation
Luca Buzzetti, Giacomo Ercole Martino Crisenza, Paolo Melchiorre
The fast-moving fields of photoredox and photocatalysis have recently provided fresh opportunities to expand the potential of synthetic organic chemistry. Advances in light-mediated processes have mainly been guided so far by empirical findings and the quest for reaction invention. The general perception, however, is that photocatalysis is entering a more mature phase where the combination of experimental and mechanistic studies will play a dominant role in sustaining further innovation. This Minireview outlines the key mechanistic studies to consider when developing a photochemical process, and the best techniques available for acquiring relevant information...
October 19, 2018: Angewandte Chemie
Lucia Barbera, Laura M De Plano, Domenico Franco, Giuseppe Gattuso, Salvatore P P Guglielmino, Gabriele Lando, Anna Notti, Melchiorre F Parisi, Ilenia Pisagatti
A new type of coating, based on carboxylato-pillar[5]arene/poly(allylamine hydrochloride) multilayer films, for the sustained release of antibiotics with in vitro antiadhesive and antimicrobial activity against Gram-positive and Gram-negative bacteria is described.
September 6, 2018: Chemical Communications: Chem Comm
Zhong-Yan Cao, Tamal Ghosh, Paolo Melchiorre
The photochemical activity of electron donor-acceptor (EDA) complexes provides a way to generate radicals under mild conditions. This strategy has found application in chemical synthesis and recently in enantioselective catalysis. Reported methods classically relied on the formation of intermolecular EDA complexes, generated upon aggregation of two suitable reagents. Herein, we further expand the synthetic utility of this strategy demonstrating that an intramolecular EDA complex can trigger a photochemical catalytic enantioselective radical process...
August 16, 2018: Nature Communications
Pablo Bonilla, Yannick P Rey, Catherine M Holden, Paolo Melchiorre
Radical cascade processes are invaluable for their ability to rapidly construct complex chiral molecules from simple substrates. However, implementing catalytic asymmetric variants is difficult. Reported herein is a visible-light-mediated organocatalytic strategy that exploits the excited-state reactivity of chiral iminium ions to trigger radical cascade reactions with high enantioselectivity. By combining two sequential radical-based bond-forming events, the method converts unactivated olefins and α,β-unsaturated aldehydes into chiral adducts in a single step...
September 24, 2018: Angewandte Chemie
Serena Leone, Jole Fonderico, Chiara Melchiorre, Andrea Carpentieri, Delia Picone
The reaction of free amino groups in proteins with reactive carbonyl species, known as glycation, leads to the formation of mixtures of products, collectively referred to as advanced glycation endproducts (AGEs). These compounds have been implicated in several important diseases, but their role in pathogenesis and clinical symptoms' development is still debated. Particularly, AGEs are often associated to the formation of amyloid deposits in conformational diseases, such as Alzheimer's and Parkinson's disease, and it has been suggested that they might influence the mechanisms and kinetics of protein aggregation...
July 16, 2018: Molecular and Cellular Biochemistry
Fabio Melchiorre, Francesca Patella, Lorenzo Pescatori, Filippo Pesapane, Enrico Fumarola, Pierpaolo Biondetti, Pietro Brambillasca, Cristian Monaco, Anna Maria Ierardi, Giuseppe Franceschelli, Gianpaolo Carrafiello
Drug-eluting bead transarterial chemoembolization (DEB-TACE) is a relative new endovascular treatment based on the use of microspheres to release chemotherapeutic agents within a target lesion with controlled pharmacokinetics. This aspect justifies the immediate success of DEB-TACE, that nowadays represents one of the most used treatments for unresectable hepatocellular carcinoma. However, there is no consensus about the choice of the best embolotherapy technique. In this review, we describe the available microspheres and report the results of the main comparative studies, to clarify the role of DEB-TACE in the hepatocellular carcinoma management...
July 10, 2018: Future Oncology
Stephen L Abrams, Kvin Lertpiriyapong, Li V Yang, Alberto M Martelli, Lucio Cocco, Stefano Ratti, Marco Falasca, Ramiro M Murata, Pedro L Rosalen, Paolo Lombardi, Massimo Libra, Saverio Candido, Giuseppe Montalto, Melchiorre Cervello, Linda S Steelman, James A McCubrey
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive, highly metastatic malignancy and accounts for 85% of pancreatic cancers. PDAC patients have poor prognosis with a five-year survival of only 5-10%. Mutations at the TP53 gene are readily detected in pancreatic tumors isolated from PDAC patients. We have investigated the effects of restoration of wild-type (WT) TP53 activity on the sensitivity of pancreatic cancer cells to: chemotherapy, targeted therapy, as well as, nutraceuticals. Upon introduction of the WT-TP53 gene into the MIA-PaCa-2 pancreatic cancer cell line, the sensitivity to drugs used to treat pancreatic cancer cells such as: gemcitabine, fluorouracil (5FU), cisplatin, irinotecan, oxaliplatin, and paclitaxel increased significantly...
August 2018: Advances in Biological Regulation
Daniele Mazzarella, Giacomo E M Crisenza, Paolo Melchiorre
Reported herein is a visible-light-mediated organocatalytic direct C-H functionalization of toluene derivatives to afford enantioenriched β-benzylated aldehydes from the corresponding enals. The process combines the oxidative power of a chiral excited-state iminium ion and the basic nature of its counteranion to trigger the generation of benzylic radicals by means of a sequential multisite proton-coupled electron transfer mechanism. This study shows that feedstock chemicals generally used as solvents, such as toluene and xylene derivatives, can be used as substrates for making chiral molecules with high enantioselectivity...
July 11, 2018: Journal of the American Chemical Society
Chiara Botto, Giuseppa Augello, Erika Amore, Maria Rita Emma, Antonina Azzolina, Gennara Cavallaro, Melchiorre Cervello, Maria Luisa Bondì
Hepatocellular carcinoma (HCC) is one of the most important causes of cancer deaths worldwide. Gene therapy is a novel approach for treating HCC. A safe and efficient gene delivery method, using viral or non-viral vectors, is a crucial factor for developing a successful HCC gene therapy. Among non-viral vectors, cationic solid lipid nanoparticles (cSLN) have advantages such as biocompatibility and transfection efficiency. In this study, novel cSLN were prepared, characterized and complexed with a plasmid (shNUPR1) capable of inhibiting the expression of the NUPR1 gene, which is involved in HCC growth and chemoresistance...
May 1, 2018: Journal of Biomedical Nanotechnology
William H Chappell, Saverio Candido, Stephen L Abrams, Suzanne Russo, Roger Ove, Alberto M Martelli, Lucio Cocco, Giulia Ramazzotti, Melchiorre Cervello, Giuseppe Montalto, Linda S Steelman, Xiaohong Leng, Ralph B Arlinghaus, Massimo Libra, James A McCubrey
Neutrophil gelatinase-associated lipocalin (NGAL a.k.a lipocalin 2, lnc2) is a secreted protein which can form a complex with matrix metalloproteinase-9 (MMP9). This MMP9/NGAL complex has been associated with metastasis. MMP9 and NGAL are detected in the urine of patients afflicted with many different types of cancer, including prostate cancer. The effects of p53, NF-κB and the androgen receptor (AR) on the expression of NGAL was examined in four prostate cancer cell lines. Prostate cancer cell lines that are AR negative and expressed either mutant or no p53 (DU145 and PC3) displayed higher levels of NGAL expression compared to the prostate cancer cell lines (LNCaP and 22Rv-1) which are AR positive and express wild type (WT) p53...
August 2018: Advances in Biological Regulation
M Venturini, P De Nardi, P Marra, M Panzeri, G Brembilla, F Morelli, F Melchiorre, F De Cobelli, A Del Maschio
No abstract text is available yet for this article.
June 2018: Techniques in Coloproctology
Daniela Castiglia, Serena Leone, Rachele Tamburino, Lorenza Sannino, Jole Fonderico, Chiara Melchiorre, Andrea Carpentieri, Stefania Grillo, Delia Picone, Nunzia Scotti
Plastid-based MNEI protein mutants retain the structure, stability and sweetness of their bacterial counterparts, confirming the attractiveness of the plastid transformation technology for high-yield production of recombinant proteins. The prevalence of obesity and diabetes has dramatically increased the industrial demand for the development and use of alternatives to sugar and traditional sweeteners. Sweet proteins, such as MNEI, a single chain derivative of monellin, are the most promising candidates for industrial applications...
August 2018: Planta
Nadia Lampiasi, Kazuo Umezawa, Giuseppe Montalto, Melchiorre Cervello
No abstract text is available yet for this article.
July 2018: Biochimica et biophysica acta. Molecular cell research
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