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Author Details

Francesco Berardi
Universita degli Studi di Bari
1965
173
35
Trey Ideker (CM4AI)
PMIDPaper TitleJournal TitlePublished Year
34902734Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (Ï¿<sub>1</sub>) receptor ligands with potent anti-amnesic effect.Eur J Med Chem2022
34586588Multifunctional thiosemicarbazones targeting sigma receptors: in vitro and in vivo antitumor activities in pancreatic cancer models.Cell Oncol (Dordr)2021
33052254Why PB28 Could Be a Covid 2019 Game Changer?ACS Med Chem Lett2020
31973006NO1, a New Sigma 2 Receptor/TMEM97 Fluorescent Ligand, Downregulates SOCE and Promotes Apoptosis in the Triple Negative Breast Cancer Cell Lines.Cancers (Basel)2020
33060197Comparative host-coronavirus protein interaction networks reveal pan-viral disease mechanisms.Science2020
33364961PB28, the Sigma-1 and Sigma-2 Receptors Modulator With Potent Anti-SARS-CoV-2 Activity: A Review About Its Pharmacological Properties and Structure Affinity Relationships.Front Pharmacol2020
31633399High-affinity sigma-1 (Ï¿<sub>1</sub>) receptor ligands based on the Ï¿<sub>1</sub> antagonist PB212.Future Med Chem2019
31265310Validation of Thiosemicarbazone Compounds as P-Glycoprotein Inhibitors in Human Primary Brain-Blood Barrier and Glioblastoma Stem Cells.Mol Pharm2019
29287249Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (Ͽ<sub>2</sub>) receptor and P-gp protein in the cytotoxic action: In vitro and in vivo activity in pancreatic tumors.Eur J Med Chem2018
35542423An innovative small molecule for promoting neuroreparative strategies.RSC Adv2018
29966437Sigma-2 receptor: past, present and perspectives on multiple therapeutic exploitations.Future Med Chem2018
29531859Synthesis, radiolabelling, and evaluation of [<sup>11</sup>C]PB212 as a radioligand for imaging sigma-1 receptors using PET.Am J Nucl Med Mol Imaging2018
28007569Sigma-2 receptor and progesterone receptor membrane component 1 (PGRMC1) are two different proteins: Proofs by fluorescent labeling and binding of sigma-2 receptor ligands to PGRMC1.Pharmacol Res2017
28364693The Ï¿<sub>1</sub> receptor agonist (+)-pentazocine increases store-operated Ca<sup>2+</sup> entry in MCF7Ï¿<sub>1</sub> and SK-N-SH cell lines.Pharmacol Rep2017
28086830Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer.BMC Cancer2017
28120522Sigma 2 receptor expression levels in blood and bladder from healthy and bladder cancer cattle.Vet Comp Oncol2017
26717207Development of sigma-1 (Ͽ1) receptor fluorescent ligands as versatile tools to study Ͽ1 receptors.Eur J Med Chem2016
27514711Design and Synthesis of New Selective P-gp Substrates and Inhibitors.Curr Pharm Des2016
26750618Functionalized Coumarine Fragment to Obtain Fluorescent and Selective P-Glycoprotein Ligands.Arch Pharm (Weinheim)2016
25462269From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.Eur J Med Chem2015
25843410Elements in support of the 'non-identity' of the PGRMC1 protein with the Ͽ2 receptor.Eur J Pharmacol2015
25666889Live imaging reveals a new role for the sigma-1 (Ͽ1) receptor in allowing microglia to leave brain injuries.Neurosci Lett2015
25637276Synthesis and pharmacological evaluation of ¹¹C-labeled piperazine derivative as a PET probe for sigma-2 receptor imaging.Nucl Med Biol2015
25757101Novel and Selective Fluorescent Ͽ2 -Receptor Ligand with a 3,4-Dihydroisoquinolin-1-one Scaffold: A Tool to Study Ͽ2 Receptors in Living Cells.Chembiochem2015
25462276Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity from Ͽ2 receptor affinity in mixed P-gp/Ͽ2 receptor agents.Eur J Med Chem2015
24174335PET radiotracers for imaging P-glycoprotein: the challenge for early diagnosis in AD.ChemMedChem2014
25379609SAR studies on tetrahydroisoquinoline derivatives: the role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein.J Med Chem2014
25093931Trimethoxybenzanilide-based P-glycoprotein modulators: an interesting case of lipophilicity tuning by intramolecular hydrogen bonding.J Med Chem2014
24732791Synthesis, radiolabeling and in vivo evaluation of [(11)C](R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT(7) receptor.Eur J Med Chem2014
24911087The effects of new sigma (Ï¿) receptor ligands, PB190 and PB212, in the models predictive of antidepressant activity.Pharmacol Rep2014
24508140Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HTâ¿¿ receptor.Bioorg Med Chem2014
24622785Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview.Rev Neurosci2014
24591318Design, synthesis, lipophilic properties, and binding affinities of potential ligands in positron emission tomography (PET) for visualization of brain dopamine D4 receptors.Chem Biodivers2014
24697311Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent and Ï¿ receptors binding properties.J Med Chem2014
23347803Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters.Bioorg Med Chem2013
24106081Sigma-2 receptor agonists as possible antitumor agents in resistant tumors: hints for collateral sensitivity.ChemMedChem2013
24100077Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.Bioorg Med Chem Lett2013
24161678Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of Ͽ⿿ receptors.Eur J Med Chem2013
23726026Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments.Bioorg Med Chem Lett2013
23415062Investigation of Ï¿ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.Bioorg Med Chem2013
23571499Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters.Exp Brain Res2013
23234641Comparative evaluation of two dye probes in the rat everted gut sac model for unambiguous classification of P-gp substrate and inhibitor.J Pharmacol Toxicol Methods2013
23374872Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.Bioorg Med Chem Lett2013
22112208Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.J Med Chem2012
22788968The therapeutic potential of 5-HT1A receptors: a patent review.Expert Opin Ther Pat2012
22738316Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.J Med Chem2012
228908832-Aminopyridine derivatives as potential Ï¿(2) receptor antagonists.ChemMedChem2012
22873661Activatable fluorescent probes: a new concept in optical molecular imaging.Curr Med Chem2012
22465185The sigma-1 receptor antagonist PB212 reduces the Ca²⁺-release through the inositol (1, 4, 5)-trisphosphate receptor in SK-N-SH cells.Eur J Pharmacol2012
22551149Lysosomal membrane permeabilization is an early event in Sigma-2 receptor ligand mediated cell death in pancreatic cancer.J Exp Clin Cancer Res2012
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Collaborators

Polish Academy of Sciences
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University of Turin
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University of California San Francisco
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Co-authored papers 1
University of California san francisco
Co-authored papers 1
University of Dundee
Co-authored papers 1
European Bioinformatics Institute
Co-authored papers 1
Wellcome Trust Sanger Institute
Co-authored papers 1
School of Clinical Medicine, University of Hong Kong
Co-authored papers 1
College of Life Sciences, University of Dundee
Co-authored papers 1
University of California san francisco
Co-authored papers 1
Quantitative Biosciences Institute (QBI), University of California San Francisco
Co-authored papers 1
Quantitative Biosciences Institute (QBI), University of California san francisco
Co-authored papers 1
University of California san francisco
Co-authored papers 1
Columbia University
Co-authored papers 1
University of California san francisco
Co-authored papers 1
University of California san francisco
Co-authored papers 1
University of Sheffield
Co-authored papers 1
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Department of Pharmaceutical Chemistry, University of California san francisco
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Washington University School of Medicine
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Icahn School of Medicine at Mount Sinai
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