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1. D7.2: Dissemination Plan

Author

Asanova, Sabina and Torquati, Ilaria

Subjects
dissemination, exploitation plan
Abstract

The document presents the first version of the Dissemination Plan for the SELFIE project. It sets out main tools and channels through which the consortium will aim at maximally disseminate the results that have been generated throughout the project. The dissemination plan describes the strategy developed for the activities and results. The document first presents the revision timeline, giving an overview when the dissemination plan will be adapted (if necessary) and sets out the main rules that will be applied during the dissemination activities, including GDPR compliance. It further sheds the light on the main target audience. In the second part of the document we present the main channels, including social media as well as the tools that will be used, such as flyers and newsletters. We also present non-exhaustive lists for the scientific journals and external events at which we plan to present the SELFIE project. Dissemination Plan is concluded with an outline on how we will evaluate and track the dissemination activities.

Published
2020
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2. D7.1: Project Website and Project identity defined

Author

Torquati, Ilaria and Ofenheimer, Ursula

Subjects
project identity, project website
Abstract

This deliverable describes the development and the focus of project visual identity and gives some examples of its application in communication tools. Moreover, the structure and the design of the SELFIE website, which will be online and operational by M3, is presented here.

Published
2020
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4. Exploring the Role of N6-Substituents in Potent Dual Acting 5′-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice

Author

Petrelli, Riccardo, primary, Scortichini, Mirko, additional, Kachler, Sonja, additional, Boccella, Serena, additional, Cerchia, Carmen, additional, Torquati, Ilaria, additional, Del Bello, Fabio, additional, Salvemini, Daniela, additional, Novellino, Ettore, additional, Luongo, Livio, additional, Maione, Sabatino, additional, Jacobson, Kenneth A., additional, Lavecchia, Antonio, additional, Klotz, Karl-Norbert, additional, and Cappellacci, Loredana, additional

Published
2017
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5. From the covalent linkage of drugs to novel inhibitors of ribonucleotide reductase: Synthesis and biological evaluation of valproic esters of 3′-C-methyladenosine

Author

Petrelli, Riccardo, Meli, Maria, Vita, Patrizia, Torquati, Ilaria, Ferro, Arianna, Vodnala, Munender, D’Alessandro, Natale, Tolomeo, Manlio, Del Bello, Fabio, Kusumanchi, Praveen, Franchetti, Palmarisa, Grifantini, Mario, Jayaram, Hiremagalur N., Hofer, Anders, and Cappellacci, Loredana

Published
2014
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29. Synthesis of Triazole-Linked Analogues of c-di-GMP and Their Interactions with Diguanylate Cyclase

Author

Fernicola, Silvia, primary, Torquati, Ilaria, additional, Paiardini, Alessandro, additional, Giardina, Giorgio, additional, Rampioni, Giordano, additional, Messina, Marco, additional, Leoni, Livia, additional, Del Bello, Fabio, additional, Petrelli, Riccardo, additional, Rinaldo, Serena, additional, Cappellacci, Loredana, additional, and Cutruzzolà, Francesca, additional

Published
2015
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30. Exploring the Role of N 6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice∇.

Author

Petrelli, Riccardo, Scortichini, Mirko, Kachler, Sonja, Boccella, Serena, Cerchia, Carmen, Torquati, Ilaria, Del Bello, Fabio, Salvemini, Daniela, Novellino, Ettore, Luongo, Livio, Maione, Sabatino, Jacobson, Kenneth A., Lavecchia, Antonio, Karl-Norbert Klotz, and Cappellacci, Loredana

Published
2017
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31. 5′-C-Ethyl-tetrazolyl-N6-Substituted Adenosine and 2-Chloro-adenosine Derivatives as Highly Potent Dual Acting A1 Adenosine Receptor Agonists and A3 Adenosine Receptor Antagonists

Author

Petrelli, Riccardo, primary, Torquati, Ilaria, additional, Kachler, Sonja, additional, Luongo, Livio, additional, Maione, Sabatino, additional, Franchetti, Palmarisa, additional, Grifantini, Mario, additional, Novellino, Ettore, additional, Lavecchia, Antonio, additional, Klotz, Karl-Norbert, additional, and Cappellacci, Loredana, additional

Published
2015
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33. 5'-C-Ethyl-tetrazolyl-N 6-Substituted Adenosine and 2-Chloro-adenosine Derivatives as Highly Potent Dual Acting A1 Adenosine Receptor Agonists and A3 Adenosine Receptor Antagonists.

Author

Petrelli, Riccardo, Torquati, Ilaria, Kachler, Sonja, Luongo, Livio, Maione, Sabatino, Franchetti, Palmarisa, Grifantini, Mario, Novellino, Ettore, Lavecchia, Antonio, Klotz, Karl-Norbert, and Cappellacci, Loredana

Subjects
*ADENOSINE derivatives, *ADENOSINE synthesis, *GLAUCOMA treatment, *SUBSTITUTION reactions, *CHEMICAL affinity, *METHYL groups
Abstract

A series of N 6-substituted-5'-C-(2-ethyl-2H-tetrazol-5-yl)-adenosine and 2-chloro-adenosine derivatives was synthesized as novel, highly potent dual acting hA1AR agonists and hA3AR antagonists, potentially useful in the treatment of glaucoma and other diseases. The best affinity and selectivity profiles were achieved by N 6-substitution with a 2-fluoro-4-chloro-phenyl- or a methyl- group. Through an in silico receptor-driven approach, the molecular bases of the hA1- and hA3AR recognition and activation of this series of 5'-C-ethyl-tetrazolyl derivatives were explained. [ABSTRACT FROM AUTHOR]

Published
2015
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34. Synthesis of Triazole-Linked Analogues of c-di-GMP and Their Interactions with Diguanylate Cyclase

Author

Alessandro Paiardini, Loredana Cappellacci, Livia Leoni, Fabio Del Bello, Marco Messina, Francesca Cutruzzolà, Riccardo Petrelli, Ilaria Torquati, Silvia Fernicola, Giorgio Giardina, Serena Rinaldo, Giordano Rampioni, Fernicola, Silvia, Torquati, Ilaria, Paiardini, Alessandro, Giardina, Giorgio, Rampioni, Giordano, Messina, Marco, Leoni, Livia, Del Bello, Fabio, Petrelli, Riccardo, Rinaldo, Serena, Cappellacci, Loredana, and Cutruzzolà, Francesca

Subjects
Models, Molecular, Guanine, Phosphodiesterase Inhibitors, Stereochemistry, Allosteric regulation, pharmaceutical science, Substrate Specificity, Structure-Activity Relationship, Drug Discovery, c-di-GMP, biofilm, Pseudomonas aeruginosa, Caulobacter crescentus, WspR, PleD, RocR, inhibitors, copper(I)-catalyzed 1,3-dipolar cycloaddition, click chemistry, Huisgen cycloaddition, alkynes, azides, dinucleoside, heterodinucleoside, 1,2,3-triazole, purine, Structure–activity relationship, Moiety, Cyclic GMP, biology, Chemistry, Escherichia coli Proteins, Active site, Triazoles, Small molecule, Anti-Bacterial Agents, Biofilms, Drug Design, Pseudomonas aeruginosa, Phosphodiester bond, Second messenger system, biology.protein, Molecular Medicine, Indicators and Reagents, Diguanylate cyclase, Phosphorus-Oxygen Lyases, molecular medicine, drug discovery
Abstract

Cyclic di-GMP (c-di-GMP) is a widespread second messenger that plays a key role in bacterial biofilm formation. The compound's ability to assume multiple conformations allows it to interact with a diverse set of target macromolecules. Here, we analyzed the binding mode of c-di-GMP to the allosteric inhibitory site (I-site) of diguanylate cyclases (DGCs) and compared it to the conformation adopted in the catalytic site of the EAL phosphodiesterases (PDEs). An array of novel molecules has been designed and synthesized by simplifying the native c-di-GMP structure and replacing the charged phosphodiester backbone with an isosteric nonhydrolyzable 1,2,3-triazole moiety. We developed the first neutral small molecule able to selectively target DGCs discriminating between the I-site of DGCs and the active site of PDEs; this molecule represents a novel tool for mechanistic studies, particularly on those proteins bearing both DGC and PDE modules, and for future optimization studies to target DGCs in vivo.

Published
2015
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35. Exploring the Role of N(6)-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice

Author

Loredana Cappellacci, Carmen Cerchia, Fabio Del Bello, Sonja Kachler, Sabatino Maione, Serena Boccella, Livio Luongo, Daniela Salvemini, Karl-Norbert Klotz, Mirko Scortichini, Ettore Novellino, Kenneth A. Jacobson, Riccardo Petrelli, Antonio Lavecchia, Ilaria Torquati, Petrelli, Riccardo, Scortichini, Mirko, Kachler, Sonja, Boccella, Serena, Cerchia, Carmen, Torquati, Ilaria, Del Bello, Fabio, Salvemini, Daniela, Novellino, Ettore, Luongo, Livio, Maione, Sabatino, Jacobson, Kenneth A, Lavecchia, Antonio, Klotz, Karl-Norbert, Cappellacci, Loredana, and Klotz, Karl Norbert

Subjects
0301 basic medicine, Agonist, Models, Molecular, Formalin Test, Adenosine, Molecular model, medicine.drug_class, Stereochemistry, Adenosine A3 Receptor Antagonist, Pharmacology, 03 medical and health sciences, Mice, 0302 clinical medicine, Drug Discovery, medicine, Adenosine A1 Receptor Agonist, Chemistry, Animal, Receptor, Adenosine A1, Receptor, Adenosine A3, Antagonist, Receptors, Purinergic P1, Purinergic P1 Receptor Agonist, Adenosine receptor, Acute Pain, HYDIA, 030104 developmental biology, Nociception, Molecular Medicine, Analgesic, Purinergic P1 Receptor Antagonist, 030217 neurology & neurosurgery, medicine.drug, Human
Abstract

Structural determinants of affinity of N(6)-substituted-5'-C-(ethyltetrazol-2-yl)adenosine and 2-chloroadenosine derivatives at adenosine receptor (AR) subtypes were studied with binding and molecular modeling. Small N(6)-cycloalkyl and 3-halobenzyl groups furnished potent dual acting A1AR agonists and A3AR antagonists. 4 was the most potent dual acting human (h) A1AR agonist (Ki = 0.45 nM) and A3AR antagonist (Ki = 0.31 nM) and highly selective versus A2A; 11 and 26 were most potent at both h and rat (r) A3AR. All N(6)-substituted-5'-C-(ethyltetrazol-2-yl)adenosine derivatives proved to be antagonists at hA3AR but agonists at the rA3AR. Analgesia of 11, 22, and 26 was evaluated in the mouse formalin test (A3AR antagonist blocked and A3AR agonist strongly potentiated). N(6)-Methyl-5'-C-(ethyltetrazol-2-yl)adenosine (22) was most potent, inhibiting both phases, as observed combining A1AR and A3AR agonists. This study demonstrated for the first time the advantages of a single molecule activating two AR pathways both leading to benefit in this acute pain model.

Published
2017

36. 5′-C-Ethyl-tetrazolyl-N6-Substituted Adenosine and 2-Chloro-adenosine Derivatives as Highly Potent Dual Acting A1 Adenosine Receptor Agonists and A3 Adenosine Receptor Antagonists

Author

Sabatino Maione, Karl-Norbert Klotz, Mario Grifantini, Loredana Cappellacci, Sonja Kachler, Palmarisa Franchetti, Ettore Novellino, Riccardo Petrelli, Antonio Lavecchia, Ilaria Torquati, Livio Luongo, Petrelli, R, Torquati, I, Kachler, S, Luongo, Livio, Maione, Sabatino, Franchetti, P, Grifantini, M, Novellino, E, Lavecchia, Antonio, Klotz, Kn, Cappellacci, L., Petrelli, Riccardo, Torquati, Ilaria, Kachler, Sonja, Franchetti, Palmarisa, Grifantini, Mario, Novellino, Ettore, Klotz, Karl-Norbert, and Cappellacci, Loredana

Subjects
Models, Molecular, Adenosine, Stereochemistry, Adenosine A3 Receptor Antagonist, Adenosine A3 Receptor Antagonists, CHO Cells, Radioligand Assay, Structure-Activity Relationship, Cricetulus, Cricetinae, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Computer Simulation, Receptor, Adenosine A1 Receptor Agonist, Molecular Structure, biology, Animal, Receptor, Adenosine A1, Chemistry, Drug Discovery3003 Pharmaceutical Science, Medicine (all), Chinese hamster ovary cell, Receptor, Adenosine A3, biology.organism_classification, Adenosine receptor, Adenosine A1 Receptor Agonists, CHO Cell, Molecular Medicine, Cricetulu, Selectivity, Adenosine A2B receptor, Human, medicine.drug
Abstract

A series of N(6)-substituted-5'-C-(2-ethyl-2H-tetrazol-5-yl)-adenosine and 2-chloro-adenosine derivatives was synthesized as novel, highly potent dual acting hA1AR agonists and hA3AR antagonists, potentially useful in the treatment of glaucoma and other diseases. The best affinity and selectivity profiles were achieved by N(6)-substitution with a 2-fluoro-4-chloro-phenyl- or a methyl- group. Through an in silico receptor-driven approach, the molecular bases of the hA1- and hA3AR recognition and activation of this series of 5'-C-ethyl-tetrazolyl derivatives were explained.

Published
2015

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