Search Results - "MOR, Marco"
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N‑Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition
Published in Journal of medicinal chemistry (23-07-2020)“…N-Acylethanolamine acid amidase (NAAA) is an N-terminal cysteine hydrolase primarily found in the endosomal–lysosomal compartment of innate and adaptive immune…”
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The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment
Published in Journal of medicinal chemistry (25-06-2015)“…The Hippo pathway is an important organ size control signaling network and the major regulatory mechanism of cell-contact inhibition. Yes associated protein…”
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L718Q Mutation as New Mechanism of Acquired Resistance to AZD9291 in EGFR-Mutated NSCLC
Published in Journal of thoracic oncology (01-10-2016)Get more information
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Dysphagia and mechanical ventilation in SARS-COV-2 pneumonia: It's real
Published in Clinical nutrition (Edinburgh, Scotland) (01-12-2022)“…Dysphagia can be a consequence of prolonged hospitalization in intensive care units (ICUs) due to severe SARS-CoV-2 pneumonia. This study aims at Identifying…”
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5
Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy
Published in Cancer cell (10-08-2015)“…The fibroblast growth factor (FGF)/FGF receptor (FGFR) system plays a crucial role in cancer by affecting tumor growth, angiogenesis, drug resistance, and…”
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Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase
Published in Glycobiology (Oxford) (01-06-2016)“…Heparanase is a β-d-glucuronidase which cleaves heparan sulfate chains in the extracellular matrix and on cellular membranes. A dysregulated heparanase…”
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Low molecular weight heparins in COVID-19 patients: beware of augmented renal clearance
Published in Critical care (London, England) (10-06-2020)“…Histologic analysis of pulmonary vessels in patients with COVID-19 has shown widespread thrombosis with alveolar capillary microthrombi [1]. A 52-year-old man…”
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Selective N-acylethanolamine-hydrolyzing acid amidase inhibition reveals a key role for endogenous palmitoylethanolamide in inflammation
Published in Proceedings of the National Academy of Sciences - PNAS (08-12-2009)“…Identifying points of control in inflammation is essential to discovering safe and effective antiinflammatory medicines. Palmitoylethanolamide (PEA) is a…”
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9
NAAA-regulated lipid signaling in monocytes controls the induction of hyperalgesic priming in mice
Published in Nature communications (24-02-2024)“…Circulating monocytes participate in pain chronification but the molecular events that cause their deployment are unclear. Using a mouse model of hyperalgesic…”
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Discovery of novel FGF trap small molecules endowed with anti-myeloma activity
Published in Pharmacological research (01-08-2024)“…Fibroblast growth factors (FGFs) act as proangiogenic and mitogenic cytokines in several cancers, including multiple myeloma (MM). Indeed, corrupted FGF…”
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Antinociceptive effects of the N-acylethanolamine acid amidase inhibitor ARN077 in rodent pain models
Published in Pain (Amsterdam) (01-03-2013)“…The N-acylethanolamine acid amidase inhibitor ARN077 exerts profound antinociceptive effects in animal pain models by enhancing endogenous lipid signaling at…”
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Systematic Modification of the Substitution Pattern of the 7-Hydroxy-5-oxopyrazolo[4,3- b ]pyridine-6-carboxamide Scaffold Enabled the Discovery of New Ligands with High Affinity and Selectivity for the Cannabinoid Type 2 Receptor
Published in Molecules (Basel, Switzerland) (24-06-2023)“…Selective ligands of the CB2 receptor are receiving considerable attention due to their potential as therapeutic agents for a variety of diseases. Recently,…”
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Targeting glucosylceramide synthase induces antiproliferative and proapoptotic effects in osimertinib-resistant NSCLC cell models
Published in Scientific reports (18-03-2024)“…The EGFR tyrosine kinase inhibitor osimertinib has been approved for the first-line treatment of EGFR -mutated Non-Small Cell Lung Cancer (NSCLC) patients…”
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Different roles for the acyl chain and the amine leaving group in the substrate selectivity of N-Acylethanolamine acid amidase
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2021)“…N-acylethanolamine acid amidase (NAAA) is an N-terminal nucleophile (Ntn) hydrolase that catalyses the intracellular deactivation of the endogenous analgesic…”
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15
Synthesis, Structural Elucidation, and Biological Evaluation of NSC12, an Orally Available Fibroblast Growth Factor (FGF) Ligand Trap for the Treatment of FGF-Dependent Lung Tumors
Published in Journal of medicinal chemistry (26-05-2016)“…NSC12 is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. It was identified by virtual…”
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Characterization of the fatty acid amide hydrolase inhibitor cyclohexyl carbamic acid 3'-carbamoyl-biphenyl-3-yl ester (URB597): effects on anandamide and oleoylethanolamide deactivation
Published in The Journal of pharmacology and experimental therapeutics (01-04-2005)“…Fatty acid amide hydrolase (FAAH) is an intracellular serine enzyme that catalyzes the hydrolysis of bioactive fatty acid ethanolamides such as anandamide and…”
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Chiral Recognition of Flexible Melatonin Receptor Ligands Induced by Conformational Equilibria
Published in Molecules (Basel, Switzerland) (04-09-2020)“…-anilinoethylamides are a class of melatoninergic agents with the aniline portion mimicking the indole ring of the natural ligand and the ethylamide chain…”
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A catalytic mechanism for cysteine N-terminal nucleophile hydrolases, as revealed by free energy simulations
Published in PloS one (28-02-2012)“…The N-terminal nucleophile (Ntn) hydrolases are a superfamily of enzymes specialized in the hydrolytic cleavage of amide bonds. Even though several members of…”
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Modulation of anxiety through blockade of anandamide hydrolysis
Published in Nature medicine (01-01-2003)“…The psychoactive constituent of cannabis, Delta(9)-tetrahydrocannabinol, produces in humans subjective responses mediated by CB1 cannabinoid receptors,…”
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Amino Acid Conjugates of Lithocholic Acid As Antagonists of the EphA2 Receptor
Published in Journal of medicinal chemistry (11-04-2013)“…The Eph receptor–ephrin system is an emerging target for the development of novel antiangiogenetic agents. We recently identified lithocholic acid (LCA) as a…”
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