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Your search keyword '"Carullo, Gabriele"' showing total 12 results
Start Over Author "Carullo, Gabriele" Publisher american chemical society
12 results on '"Carullo, Gabriele"'

1. Targeting Relevant HDACs to Support the Survival of Cone Photoreceptors in Inherited Retinal Diseases: Identification of a Potent Pharmacological Tool with In Vitro and In Vivo Efficacy.

Author

Carullo, Gabriele, Orsini, Noemi, Piano, Ilaria, Pozzetti, Luca, Papa, Alessandro, Fontana, Anna, Napoli, Debora, Corsi, Francesca, Marco, Beatrice Di, Galante, Alessia, Marotta, Ludovica, Panzeca, Giovanna, O'Brien, Justine, Sanchez, Alicia Gomez, Doherty, Harry, Mahon, Niamh, Clarke, Leni, Contri, Chiara, Pasquini, Silvia, and Gorelli, Beatrice

Published
2024
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2. Development of Epigenetic Modifiers with Therapeutic Potential in FMS-Related Tyrosine Kinase 3/Internal Tandem Duplication (FLT3/ITD) Acute Myeloid Leukemia and Other Blood Malignancies.

Author

Carullo, Gabriele, Rossi, Sara, Giudice, Valentina, Pezzotta, Alex, Chianese, Ugo, Scala, Pasqualina, Carbone, Sabrina, Fontana, Anna, Panzeca, Giovanna, Pasquini, Silvia, Contri, Chiara, Gemma, Sandra, Ramunno, Anna, Saponara, Simona, Galvani, Francesca, Lodola, Alessio, Mor, Marco, Benedetti, Rosaria, Selleri, Carmine, and Varani, Katia

Published
2024
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3. Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization.

Author

Butini, Stefania, Grether, Uwe, Jung, Kwang-Mook, Ligresti, Alessia, Allarà, Marco, Postmus, Annemarieke G. J., Maramai, Samuele, Brogi, Simone, Papa, Alessandro, Carullo, Gabriele, Sykes, David, Veprintsev, Dmitry, Federico, Stefano, Grillo, Alessandro, Di Guglielmo, Bruno, Ramunno, Anna, Stevens, Anna Floor, Heer, Dominik, Lamponi, Stefania, and Gemma, Sandra

Published
2024
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4. In Silico-Guided Rational Drug Design and Synthesis of Novel 4‑(Thiophen-2-yl)butanamides as Potent and Selective TRPV1 Agonists.

Author

Romeo, Isabella, Brizzi, Antonella, Pessina, Federica, Ambrosio, Francesca Alessandra, Aiello, Francesca, Belardo, Carmela, Carullo, Gabriele, Costa, Giosuè, De Petrocellis, Luciano, Frosini, Maria, Luongo, Livio, Maramai, Samuele, Paolino, Marco, Moriello, Aniello Schiano, Mugnaini, Claudia, Scorzelli, Francesco, Maione, Sabatino, Corelli, Federico, Di Marzo, Vincenzo, and Alcaro, Stefano

Published
2023
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5. GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery

Author

Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica, Carullo, Gabriele, Mazzotta, Sarah, Vega Holm, Margarita, Iglesias Guerra, Fernando, Vega Pérez, José Manuel, Aiello, Francesca, Brizzi, Antonella, Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica, Carullo, Gabriele, Mazzotta, Sarah, Vega Holm, Margarita, Iglesias Guerra, Fernando, Vega Pérez, José Manuel, Aiello, Francesca, and Brizzi, Antonella

Abstract

The G-protein coupled receptors (GPCRs) activated by free fatty acids (FFAs) have emerged as new and exciting drug targets, due to their plausible translation from pharmacology to medicines. This perspective aims to report recent research about GPR120/FFAR4 and its involvement in several diseases, including cancer, inflammatory conditions, and central nervous system disorders. The focus is to highlight the importance of GPR120 in Type 2 diabetes mellitus (T2DM). GPR120 agonists, useful in T2DM drug discovery, have been widely explored from a structure–activity relationship point of view. Since the identification of the first reported synthetic agonist TUG-891, the research has paved the way for the development of TUG-based molecules as well as new and different chemical entities. These molecules might represent the starting point for the future discovery of GPR120 agonists as antidiabetic drugs.

Published
2021

11. Harnessing the Role of HDAC6 in Idiopathic Pulmonary Fibrosis: Design, Synthesis, Structural Analysis, and Biological Evaluation of Potent Inhibitors.

Author

Campiani G, Cavella C, Osko JD, Brindisi M, Relitti N, Brogi S, Saraswati AP, Federico S, Chemi G, Maramai S, Carullo G, Jaeger B, Carleo A, Benedetti R, Sarno F, Lamponi S, Rottoli P, Bargagli E, Bertucci C, Tedesco D, Herp D, Senger J, Ruberti G, Saccoccia F, Saponara S, Gorelli B, Valoti M, Kennedy B, Sundaramurthi H, Butini S, Jung M, Roach KM, Altucci L, Bradding P, Christianson DW, Gemma S, and Prasse A

Subjects
Dose-Response Relationship, Drug, Histone Deacetylase 6 metabolism, Histone Deacetylase Inhibitors chemical synthesis, Histone Deacetylase Inhibitors chemistry, Humans, Idiopathic Pulmonary Fibrosis metabolism, Idiopathic Pulmonary Fibrosis pathology, Models, Molecular, Molecular Structure, Structure-Activity Relationship, Drug Design, Histone Deacetylase 6 antagonists & inhibitors, Histone Deacetylase Inhibitors pharmacology, Idiopathic Pulmonary Fibrosis drug therapy
Abstract

Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed by our immunohistochemistry studies on HDAC6 overexpression in IPF lung tissues. We herein developed a series of novel h HDAC6 inhibitors, having low inhibitory potency over h HDAC1 and h HDAC8, as potential pharmacological tools for IPF treatment. Their inhibitory potency was combined with low in vitro and in vivo toxicity. Structural analysis of 6h and structure-activity relationship studies contributed to the optimization of the binding mode of the new molecules. The best-performing analogues were tested for their efficacy in inhibiting fibrotic sphere formation and cell viability, proving their capability in reverting the IPF phenotype. The efficacy of analogue 6h was also determined in a validated human lung model of TGF-β1-dependent fibrogenesis. The results highlighted in this manuscript may pave the way for the identification of first-in-class molecules for the treatment of IPF.

Published
2021
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12. GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.

Author

Carullo G, Mazzotta S, Vega-Holm M, Iglesias-Guerra F, Vega-Pérez JM, Aiello F, and Brizzi A

Subjects
Adipogenesis, Animals, Carboxylic Acids chemistry, Carboxylic Acids metabolism, Carboxylic Acids therapeutic use, Diabetes Mellitus, Type 2 drug therapy, Humans, Hypoglycemic Agents metabolism, Hypoglycemic Agents therapeutic use, Ligands, Mice, Phenylpropionates metabolism, Phenylpropionates therapeutic use, Receptors, G-Protein-Coupled metabolism, Structure-Activity Relationship, Sulfonamides chemistry, Sulfonamides metabolism, Sulfonamides therapeutic use, Drug Discovery, Hypoglycemic Agents chemistry, Phenylpropionates chemistry, Receptors, G-Protein-Coupled agonists
Abstract

The G-protein coupled receptors (GPCRs) activated by free fatty acids (FFAs) have emerged as new and exciting drug targets, due to their plausible translation from pharmacology to medicines. This perspective aims to report recent research about GPR120/FFAR4 and its involvement in several diseases, including cancer, inflammatory conditions, and central nervous system disorders. The focus is to highlight the importance of GPR120 in Type 2 diabetes mellitus (T2DM). GPR120 agonists, useful in T2DM drug discovery, have been widely explored from a structure-activity relationship point of view. Since the identification of the first reported synthetic agonist TUG-891, the research has paved the way for the development of TUG-based molecules as well as new and different chemical entities. These molecules might represent the starting point for the future discovery of GPR120 agonists as antidiabetic drugs.

Published
2021
Full Text
View/download PDF

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