Full Text Journal Articles by
Author Elisa Uliassi

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Therapeutic strategies for identifying small molecules against prion diseases.

Elisa Uliassi, Lea Nikolic, Maria Laura Bolognesi, Giuseppe Legname,

Prion diseases are fatal neurodegenerative disorders, for which there are no effective therapeutic and diagnostic agents. The main pathological hallmark has been identified as conformational changes of the cellular isoform prion protein (PrP<sup>C</sup>) to a misfolded isoform of the prion protein (PrP<sup>Sc</sup>). Targeting PrP<sup>C</sup> and its conversion to PrP<sup>Sc</sup> is ... Read more >>

Cell Tissue Res (Cell and tissue research)
[2022, :]

Cited: 0 times

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Sustainable production of pharmaceutical, nutraceutical and bioactive compounds from biomass and waste.

Claudia Espro, Emilia Paone, Francesco Mauriello, Roberto Gotti, Elisa Uliassi, Maria Laura Bolognesi, Daily Rodríguez-Padrón, Rafael Luque,

The aim of this tutorial review is to provide a general overview of processes, technologies and challenges in the production of pharmaceutical and bioactive compounds from food waste and lignocellulosic residues. Particular attention is given to benign-by-design processes instinctively devoted to environmental sustainability for the recovery of bioactive compounds from ... Read more >>

Chem Soc Rev (Chemical Society reviews)
[2021, 50(20):11191-11207]

Cited: 1 time

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Cashew Nut Shell Liquid (CNSL) as a Source of Drugs for Alzheimer's Disease.

Elisa Uliassi, Andressa Souza de Oliveira, Luciana de Camargo Nascente, Luiz Antonio Soares Romeiro, Maria Laura Bolognesi,

Alzheimer's disease (AD) is a complex neurodegenerative disorder with a multifaceted pathogenesis. This fact has long halted the development of effective anti-AD drugs. Recently, a therapeutic strategy based on the exploitation of Brazilian biodiversity was set with the aim of discovering new disease-modifying and safe drugs for AD. In this ... Read more >>

Molecules (Molecules (Basel, Switzerland))
[2021, 26(18):]

Cited: 0 times

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Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer's Disease.

Lukas Gorecki, Elisa Uliassi, Manuela Bartolini, Jana Janockova, Martina Hrabinova, Vendula Hepnarova, Lukas Prchal, Lubica Muckova, Jaroslav Pejchal, Jana Z Karasova, Eva Mezeiova, Marketa Benkova, Tereza Kobrlova, Ondrej Soukup, Sabrina Petralla, Barbara Monti, Jan Korabecny, Maria Laura Bolognesi,

Since 2002, no clinical candidate against Alzheimer's disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called "multitarget directed ligand" approach and designed 36 novel tacrine-phenothiazine heterodimers which were <i>in vitro</i> evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2021, 12(9):1698-1715]

Cited: 0 times

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Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.

Giselle de Andrade Ramos, Andressa Souza de Oliveira, Manuela Bartolini, Marina Naldi, Irene Liparulo, Christian Bergamini, Elisa Uliassi, Ling Wu, Paul E Fraser, Monica Abreu, Alessandra Sofia Kiametis, Ricardo Gargano, Edilberto Rocha Silveira, Guilherme D Brand, Lukas Prchal, Ondřej Soukup, Jan Korábečný, Maria Laura Bolognesi, Luiz Antonio Soares Romeiro,

As part of our efforts to develop sustainable drugs for Alzheimer's disease (AD), we have been focusing on the inexpensive and largely available cashew nut shell liquid (CNSL) as a starting material for the identification of new acetylcholinesterase (AChE) inhibitors. Herein, we decided to investigate whether cardanol, a phenolic CNSL ... Read more >>

RSC Med Chem (RSC medicinal chemistry)
[2021, 12(7):1154-1163]

Cited: 1 time

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Turning Donepezil into a Multi-Target-Directed Ligand through a Merging Strategy.

Rosaria Perone, Claudia Albertini, Elisa Uliassi, Flaminia Di Pietri, Pedro de Sena Murteira Pinheiro, Sabrina Petralla, Nicola Rizzardi, Romana Fato, Lenka Pulkrabkova, Ondrej Soukup, Anna Tramarin, Manuela Bartolini, Maria Laura Bolognesi,

Thanks to the widespread use and safety profile of donepezil (1) in the treatment of Alzheimer's disease (AD), one of the most widely adopted multi-target-directed ligand (MTDL) design strategies is to modify its molecular structure by linking a second fragment carrying an additional AD-relevant biological property. Herein, supported by a ... Read more >>

ChemMedChem (ChemMedChem)
[2021, 16(1):187-198]

Cited: 2 times

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Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease.

Katarina Chalupova, Jan Korabecny, Manuela Bartolini, Barbara Monti, Doriano Lamba, Rosanna Caliandro, Alessandro Pesaresi, Xavier Brazzolotto, Anne-Julie Gastellier, Florian Nachon, Jaroslav Pejchal, Michaela Jarosova, Vendula Hepnarova, Daniel Jun, Martina Hrabinova, Rafael Dolezal, Jana Zdarova Karasova, Martin Mzik, Zdena Kristofikova, Jan Misik, Lubica Muckova, Petr Jost, Ondrej Soukup, Marketa Benkova, Vladimir Setnicka, Lucie Habartova, Marketa Chvojkova, Lenka Kleteckova, Karel Vales, Eva Mezeiova, Elisa Uliassi, Martin Valis, Eugenie Nepovimova, Maria Laura Bolognesi, Kamil Kuca,

A combination of tacrine and tryptophan led to the development of a new family of heterodimers as multi-target agents with potential to treat Alzheimer's disease. Based on the in vitro biological profile, compound S-K1035 was found to be the most potent inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), demonstrating ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 168:491-514]

Cited: 8 times

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Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform.

Carolina B Moraes, Gesa Witt, Maria Kuzikov, Bernhard Ellinger, Theodora Calogeropoulou, Kyriakos C Prousis, Stefano Mangani, Flavio Di Pisa, Giacomo Landi, Lucia Dello Iacono, Cecilia Pozzi, Lucio H Freitas-Junior, Bruno Dos Santos Pascoalino, Claudia P Bertolacini, Birte Behrens, Oliver Keminer, Jennifer Leu, Markus Wolf, Jeanette Reinshagen, Anabela Cordeiro-da-Silva, Nuno Santarem, Alberto Venturelli, Stephen Wrigley, Deepa Karunakaran, Bethlehem Kebede, Ina Pöhner, Wolfgang Müller, Joanna Panecka-Hofman, Rebecca C Wade, Martina Fenske, Joachim Clos, José María Alunda, María Jesús Corral, Elisa Uliassi, Maria Laura Bolognesi, Pasquale Linciano, Antonio Quotadamo, Stefania Ferrari, Matteo Santucci, Chiara Borsari, Maria Paola Costi, Sheraz Gul,

According to the World Health Organization, more than 1 billion people are at risk of or are affected by neglected tropical diseases. Examples of such diseases include trypanosomiasis, which causes sleeping sickness; leishmaniasis; and Chagas disease, all of which are prevalent in Africa, South America, and India. Our aim within ... Read more >>

SLAS Discov (SLAS discovery : advancing life sciences R & D)
[2019, 24(3):346-361]

Cited: 3 times

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A Focused Library of Psychotropic Analogues with Neuroprotective and Neuroregenerative Potential.

Elisa Uliassi, Luis Emiliano Peña-Altamira, Aixa V Morales, Francesca Massenzio, Sabrina Petralla, Michele Rossi, Marinella Roberti, Loreto Martinez Gonzalez, Ana Martinez, Barbara Monti, Maria Laura Bolognesi,

Overcoming the lack of effective treatments and the continuous clinical trial failures in neurodegenerative drug discovery might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting simultaneously neuroprotection and neuroregeneration. In the studies reported herein, we sought to identify small molecules that might exert neuroprotective and ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2019, 10(1):279-294]

Cited: 4 times

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A perspective on multi-target drug discovery and design for complex diseases.

Rona R Ramsay, Marija R Popovic-Nikolic, Katarina Nikolic, Elisa Uliassi, Maria Laura Bolognesi,

Diseases of infection, of neurodegeneration (such as Alzheimer's and Parkinson's diseases), and of malignancy (cancers) have complex and varied causative factors. Modern drug discovery has the power to identify potential modulators for multiple targets from millions of compounds. Computational approaches allow the determination of the association of each compound with ... Read more >>

Clin Transl Med (Clinical and translational medicine)
[2018, 7(1):3]

Cited: 118 times

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Development of a Focused Library of Triazole-Linked Privileged-Structure-Based Conjugates Leading to the Discovery of Novel Phenotypic Hits against Protozoan Parasitic Infections.

Elisa Uliassi, Lorna Piazzi, Federica Belluti, Andrea Mazzanti, Marcel Kaiser, Reto Brun, Carolina B Moraes, Lucio H Freitas-Junior, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Chiara Borsari, Maria Paola Costi, Maria Laura Bolognesi,

Protozoan infections caused by Plasmodium, Leishmania, and Trypanosoma spp. contribute significantly to the burden of infectious diseases worldwide, causing severe morbidity and mortality. The inadequacy of available treatments calls for cost- and time-effective drug discovery endeavors. To this end, we envisaged the triazole linkage of privileged structures as an effective ... Read more >>

ChemMedChem (ChemMedChem)
[2018, 13(7):678-683]

Cited: 4 times

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Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity.

Elisa Uliassi, Giulia Fiorani, R Luise Krauth-Siegel, Christian Bergamini, Romana Fato, Giulia Bianchini, J Carlos Menéndez, Maria Teresa Molina, Eulogio López-Montero, Federico Falchi, Andrea Cavalli, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Gesa Witt, Carolina B Moraes, Lucio H Freitas-Junior, Chiara Borsari, Maria Paola Costi, Maria Laura Bolognesi,

Crassiflorone is a natural product with anti-mycobacterial and anti-gonorrhoeal properties, isolated from the stem bark of the African ebony tree Diospyros crassiflora. We noticed that its pentacyclic core possesses structural resemblance to the quinone-coumarin hybrid 3, which we reported to exhibit a dual-targeted inhibitory profile towards Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 141:138-148]

Cited: 5 times

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Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.

Jakub Jeřábek, Elisa Uliassi, Laura Guidotti, Jan Korábečný, Ondřej Soukup, Vendula Sepsova, Martina Hrabinova, Kamil Kuča, Manuela Bartolini, Luis Emiliano Peña-Altamira, Sabrina Petralla, Barbara Monti, Marinella Roberti, Maria Laura Bolognesi,

Multi-target drug discovery is one of the most followed approaches in the active central nervous system (CNS) therapeutic area, especially in the search for new drugs against Alzheimer's disease (AD). This is because innovative multi-target-directed ligands (MTDLs) could more adequately address the complexity of this pathological condition. In a continuation ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2017, 127:250-262]

Cited: 18 times

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Neuroregeneration versus neurodegeneration: toward a paradigm shift in Alzheimer's disease drug discovery.

Elisa Uliassi, Annachiara Gandini, Rosaria Carmela Perone, Maria Laura Bolognesi,

Alzheimer's disease represents an enormous global burden in terms of human suffering and economic cost. To tackle the current lack of effective drugs and the continuous clinical trial failures might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting neural stem cells (NSCs) regeneration. In this ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2017, 9(10):995-1013]

Cited: 6 times

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Molecular basis for covalent inhibition of glyceraldehyde-3-phosphate dehydrogenase by a 2-phenoxy-1,4-naphthoquinone small molecule.

Stefano Bruno, Elisa Uliassi, Mirko Zaffagnini, Federica Prati, Christian Bergamini, Riccardo Amorati, Gianluca Paredi, Marilena Margiotta, Paola Conti, Maria Paola Costi, Marcel Kaiser, Andrea Cavalli, Romana Fato, Maria Laura Bolognesi,

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) has recently gained attention as an antiprotozoan and anticancer drug target. We have previously identified 2-phenoxy-1,4-naphthoquinone as an inhibitor of both Trypanosoma brucei and human GAPDH. Herein, through multiple chemical, biochemical, and biological studies, and through the design of analogs, we confirmed the formation of a covalent ... Read more >>

Chem Biol Drug Des (Chemical biology & drug design)
[2017, 90(2):225-235]

Cited: 5 times

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Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

Anna Junker, Ramachandran Balasubramanian, Antonella Ciancetta, Elisa Uliassi, Evgeny Kiselev, Chiara Martiriggiano, Kevin Trujillo, Giorgi Mtchedlidze, Leah Birdwell, Kyle A Brown, T Kendall Harden, Kenneth A Jacobson,

UDP and UDP-glucose activate the P2Y14 receptor (P2Y14R) to modulate processes related to inflammation, diabetes, and asthma. A computational pipeline suggested alternatives to naphthalene of a previously reported P2Y14R antagonist (3, PPTN) using docking and molecular dynamics simulations on a hP2Y14R homology model based on P2Y12R structures. By reevaluating the ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2016, 59(13):6149-6168]

Cited: 13 times

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From Companion Diagnostics to Theranostics: A New Avenue for Alzheimer's Disease?

Maria Laura Bolognesi, Annachiara Gandini, Federica Prati, Elisa Uliassi,

The recent literature signals a growing paradigm shift toward integrating therapeutics and diagnostics rather than developing and deploying them separately. In this gradual move toward more effective and personalized medications, companion diagnostics are an intermediate stage. The next step may be "theranostics", in which single chemical entities are developed to ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2016, 59(17):7759-7770]

Cited: 10 times

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The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment.

Matteo Santucci, Tatiana Vignudelli, Stefania Ferrari, Marco Mor, Laura Scalvini, Maria Laura Bolognesi, Elisa Uliassi, Maria Paola Costi,

The Hippo pathway is an important organ size control signaling network and the major regulatory mechanism of cell-contact inhibition. Yes associated protein (YAP) and transcriptional co-activator with PDZ-binding motif (TAZ) are its targets and terminal effectors: inhibition of the pathway promotes YAP/TAZ translocation to the nucleus, where they interact with ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2015, 58(12):4857-4873]

Cited: 72 times

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Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor.

Evgeny Kiselev, Ramachandran Balasubramanian, Elisa Uliassi, Kyle A Brown, Kevin Trujillo, Vsevolod Katritch, Eva Hammes, Raymond C Stevens, T Kendall Harden, Kenneth A Jacobson,

The P2Y14R is a G(i/o)-coupled receptor of the P2Y family of purinergic receptors that is activated by extracellular UDP and UDP-glucose (UDPG). In an earlier report we described a P2Y14R fluorescent probe, MRS4174, based on the potent and selective antagonist PPTN, a naphthoic acid derivative. Here, we report the design, ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2015, 25(21):4733-4739]

Cited: 4 times

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Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.

Eugenie Nepovimova, Elisa Uliassi, Jan Korabecny, Luis Emiliano Peña-Altamira, Sarah Samez, Alessandro Pesaresi, Gregory E Garcia, Manuela Bartolini, Vincenza Andrisano, Christian Bergamini, Romana Fato, Doriano Lamba, Marinella Roberti, Kamil Kuca, Barbara Monti, Maria Laura Bolognesi,

We report the identification of multitarget anti-Alzheimer compounds designed by combining a naphthoquinone function and a tacrine fragment. In vitro, 15 compounds displayed excellent acetylcholinesterase (AChE) inhibitory potencies and interesting capabilities to block amyloid-β (Aβ) aggregation. The X-ray analysis of one of those compounds in complex with AChE allowed rationalizing ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2014, 57(20):8576-8589]

Cited: 43 times

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Toward the development of dual-targeted glyceraldehyde-3-phosphate dehydrogenase/trypanothione reductase inhibitors against Trypanosoma brucei and Trypanosoma cruzi.

Federica Belluti, Elisa Uliassi, Giacomo Veronesi, Christian Bergamini, Marcel Kaiser, Reto Brun, Angelo Viola, Romana Fato, Paul A M Michels, R Luise Krauth-Siegel, Andrea Cavalli, Maria Laura Bolognesi,

A significant improvement in the treatment of trypanosomiases has been achieved with the recent development of nifurtimox-eflornithine combination therapy (NECT). As an alternative to drug combinations and as a means to overcome most of the antitrypanosomatid drug discovery challenges, a multitarget drug design strategy has been envisaged. To begin testing ... Read more >>

ChemMedChem (ChemMedChem)
[2014, 9(2):371-382]

Cited: 9 times

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