Search Results - "PELLICCIARI, Roberto"

TGR5 Activation Inhibits Atherosclerosis by Reducing Macrophage Inflammation and Lipid Loading by Pols, Thijs W.H., Nomura, Mitsunori, Harach, Taoufiq, Lo Sasso, Giuseppe, Oosterveer, Maaike H., Thomas, Charles, Rizzo, Giovanni, Gioiello, Antimo, Adorini, Luciano, Pellicciari, Roberto, Auwerx, Johan, Schoonjans, Kristina

“…The G protein-coupled receptor TGR5 has been identified as an important component of the bile acid signaling network, and its activation has been linked to…”
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Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors by Wahlberg, Elisabet, Karlberg, Tobias, Kouznetsova, Ekaterina, Markova, Natalia, Macchiarulo, Antonio, Thorsell, Ann-Gerd, Pol, Ewa, Frostell, Åsa, Ekblad, Torun, Öncü, Delal, Kull, Björn, Robertson, Graeme Michael, Pellicciari, Roberto, Schüler, Herwig, Weigelt, Johan

“…PARP inhibitors have recently entered phase 3 clinical trials as cancer therapeutics, but the specificity of many of these compounds is unknown. Wahlberg et al…”
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Manipulation of brain kynurenines: glial targets, neuronal effects, and clinical opportunities by Schwarcz, Robert, Pellicciari, Roberto

“…Degradation of the essential amino acid tryptophan along the kynurenine pathway (KP) yields several neuroactive intermediates, including the free radical…”
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Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure–Activity Relationship, X‑ray Crystal Structure, and Anticancer Activity by Moniot, Sébastien, Forgione, Mariantonietta, Lucidi, Alessia, Hailu, Gebremedhin S, Nebbioso, Angela, Carafa, Vincenzo, Baratta, Francesca, Altucci, Lucia, Giacché, Nicola, Passeri, Daniela, Pellicciari, Roberto, Mai, Antonello, Steegborn, Clemens, Rotili, Dante

“…Sirt2 is a target for the treatment of neurological, metabolic, and age-related diseases including cancer. Here we report a series of Sirt2 inhibitors based on…”
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On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo by Amori, Laura, Guidetti, Paolo, Pellicciari, Roberto, Kajii, Yasushi, Schwarcz, Robert

“…In the mammalian brain, kynurenine aminotransferase II (KAT II) and kynurenine 3-monooxygenase (KMO), key enzymes of the kynurenine pathway (KP) of tryptophan…”
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Fluctuations in Endogenous Kynurenic Acid Control Hippocampal Glutamate and Memory by POCIVAVSEK, Ana, WU, Hui-Qiu, POTTER, Michelle C, ELMER, Greg I, PELLICCIARI, Roberto, SCHWARCZ, Robert

“…Kynurenic acid (KYNA), an astrocyte-derived metabolite, antagonizes the α7 nicotinic acetylcholine receptor (α7nAChR) and, possibly, the glycine co-agonist…”
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Highlights at the gate of tryptophan catabolism: a review on the mechanisms of activation and regulation of indoleamine 2,3-dioxygenase (IDO), a novel target in cancer disease by Macchiarulo, Antonio, Camaioni, Emidio, Nuti, Roberto, Pellicciari, Roberto

“…Indoleamine 2,3-dioxygenase (IDO) catalyzes the first and rate-limiting step of Kynurenine pathway along the major route of Tryptophan catabolism. The…”
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Continuous Flow Synthesis of Thieno[2,3‑c]isoquinolin-5(4H)‑one Scaffold: A Valuable Source of PARP‑1 Inhibitors by Filipponi, Paolo, Ostacolo, Carmine, Novellino, Ettore, Pellicciari, Roberto, Gioiello, Antimo

“…An efficient multistep method for the continuous flow synthesis of thieno[2,3-c]isoquinolin-5(4H)-one-A (TIQ-A), an important pharmacological tool and building…”
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From polypharmacology to target specificity: the case of PARP inhibitors by Liscio, Paride, Camaioni, Emidio, Carotti, Andrea, Pellicciari, Roberto, Macchiarulo, Antonio

“…Poly(ADP-ribose)polymerases (PARPs) catalyze a post-transcriptional modification of proteins, consisting in the attachment of mono, oligo or poly ADP-ribose…”
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Beyond bile acids: targeting Farnesoid X Receptor (FXR) with natural and synthetic ligands by Carotti, Andrea, Marinozzi, Maura, Custodi, Chiara, Cerra, Bruno, Pellicciari, Roberto, Gioiello, Antimo, Macchiarulo, Antonio

“…The modulation of FXR receptor remains an attractive area in drug discovery to develop novel therapeutic opportunities for liver and metabolic disorders…”
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The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis by Fiorucci, Stefano, Antonelli, Elisabetta, Rizzo, Giovanni, Renga, Barbara, Mencarelli, Andrea, Riccardi, Luisa, Orlandi, Stefano, Pellicciari, Roberto, Morelli, Antonio

“…Background & Aims: The farnesoid X receptor (FXR) is an endogenous sensor for bile acids and inhibits bile acid synthesis by inducing small heterodimer partner…”
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Novel 1,4-Dihydropyridine Derivatives as Mineralocorticoid Receptor Antagonists by Pérez-Gordillo, Felipe Luis, Serrano-Morillas, Natalia, Acosta-García, Luz Marina, Aranda, María Teresa, Passeri, Daniela, Pellicciari, Roberto, Pérez de Vega, María Jesús, González-Muñiz, Rosario, Alvarez de la Rosa, Diego, Martín-Martínez, Mercedes

“…The mineralocorticoid receptor (MR) belongs to the steroid receptor subfamily of nuclear receptors. MR is a transcription factor key in regulating blood…”
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The farnesoid X receptor promotes adipocyte differentiation and regulates adipose cell function in vivo by Rizzo, Giovanni, Disante, Moises, Mencarelli, Andrea, Renga, Barbara, Gioiello, Antimo, Pellicciari, Roberto, Fiorucci, Stefano

“…The differentiation of a preadipocyte into a mature adipocyte is a highly regulated process that requires a scripted program of transcriptional events leading…”
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The Astrocyte-Derived α7 Nicotinic Receptor Antagonist Kynurenic Acid Controls Extracellular Glutamate Levels in the Prefrontal Cortex by Wu, Hui-Qiu, Pereira, Edna F. R., Bruno, John P., Pellicciari, Roberto, Albuquerque, Edson X., Schwarcz, Robert

“…The cognitive deficits seen in schizophrenia patients are likely related to abnormal glutamatergic and cholinergic neurotransmission in the prefrontal cortex…”
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Farnesoid X Receptor:  From Structure to Potential Clinical Applications by Pellicciari, Roberto, Costantino, Gabriele, Fiorucci, Stefano

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Bile acid derivatives as ligands of the farnesoid x receptor: molecular determinants for bile acid binding and receptor modulation by Gioiello, Antimo, Cerra, Bruno, Mostarda, Serena, Guercini, Chiara, Pellicciari, Roberto, Macchiarulo, Antonio

“…Bile acids are a peculiar class of steroidal compounds that never cease to amaze. From being simple detergents with a primary role in aiding the absorption of…”
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Poly(ADP-ribose) Catabolism Triggers AMP-dependent Mitochondrial Energy Failure by Formentini, Laura, Macchiarulo, Antonio, Cipriani, Giulia, Camaioni, Emidio, Rapizzi, Elena, Pellicciari, Roberto, Moroni, Flavio, Chiarugi, Alberto

“…Upon massive DNA damage, hyperactivation of the nuclear enzyme poly(ADP-ribose) polymerase (PARP)-1 causes severe depletion of intracellular NAD and ATP pools…”
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Targeting the MDM2/MDM4 interaction interface as a promising approach for p53 reactivation therapy by Pellegrino, Marsha, Mancini, Francesca, Lucà, Rossella, Coletti, Alice, Giacchè, Nicola, Manni, Isabella, Arisi, Ivan, Florenzano, Fulvio, Teveroni, Emanuela, Buttarelli, Marianna, Fici, Laura, Brandi, Rossella, Bruno, Tiziana, Fanciulli, Maurizio, D'Onofrio, Mara, Piaggio, Giulia, Pellicciari, Roberto, Pontecorvi, Alfredo, Marine, Jean Christophe, Macchiarulo, Antonio, Moretti, Fabiola

“…Restoration of wild-type p53 tumor suppressor function has emerged as an attractive anticancer strategy. Therapeutics targeting the two p53-negative…”
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Design, Synthesis, Crystallographic Studies, and Preliminary Biological Appraisal of New Substituted Triazolo[4,3‑b]pyridazin-8-amine Derivatives as Tankyrase Inhibitors by Liscio, Paride, Carotti, Andrea, Asciutti, Stefania, Karlberg, Tobias, Bellocchi, Daniele, Llacuna, Laura, Macchiarulo, Antonio, Aaronson, Stuart A, Schüler, Herwig, Pellicciari, Roberto, Camaioni, Emidio

“…Searching for selective tankyrases (TNKSs) inhibitors, a new small series of 6,8-disubstituted triazolo[4,3-b]piridazines has been synthesized and…”
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Nongenomic Actions of Bile Acids. Synthesis and Preliminary Characterization of 23- and 6,23-Alkyl-Substituted Bile Acid Derivatives as Selective Modulators for the G-Protein Coupled Receptor TGR5 by Pellicciari, Roberto, Sato, Hiroyuki, Gioiello, Antimo, Costantino, Gabriele, Macchiarulo, Antonio, Sadeghpour, Bahman M, Giorgi, Gianluca, Schoonjans, Kristina, Auwerx, Johan

“…23-Alkyl-substituted and 6,23-alkyl-disubstituted derivatives of chenodeoxycholic acid are identified as potent and selective agonists of TGR5, a G-protein…”
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