Mauro Niso

发表

Cyclohexylpiperazine derivative PB28, a σ2 agonist and σ1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer

A. Paradiso, F. Berardi, R. Perrone, 2006, Molecular Cancer Therapeutics.

Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ1) receptor ligands with potent anti-amnesic effect.

B. Delprat, F. Berardi, Mauro Niso, 2021, European journal of medicinal chemistry.

Multi-Target Directed Ligands (MTDLs) Binding the σ1 Receptor as Promising Therapeutics: State of the Art and Perspectives

M. Leopoldo, Mauro Niso, C. Abate, 2021, International journal of molecular sciences.

High-affinity sigma-1 (σ1) receptor ligands based on the σ1 antagonist PB212.

M. Leopoldo, F. Berardi, Mauro Niso, 2019, Future medicinal chemistry.

Design, Synthesis, Lipophilic Properties, and Binding Affinities of Potential Ligands in Positron Emission Tomography (PET) for Visualization of Brain Dopamine D4 Receptors

E. Lacivita, M. Leopoldo, F. Berardi, 2014, Chemistry & biodiversity.

ABC pumps and their role in active drug transport.

F. Berardi, R. Perrone, N. Colabufo, 2009, Current topics in medicinal chemistry.

1‐Cyclohexyl‐4‐(4‐arylcyclohexyl)piperazines: Mixed σ and Human Δ8–Δ7 Sterol Isomerase Ligands with Antiproliferative and P‐Glycoprotein Inhibitory Activity

F. Berardi, R. Perrone, N. Colabufo, 2011, ChemMedChem.

Sigma-2 receptor: past, present and perspectives on multiple therapeutic exploitations.

F. Berardi, Mauro Niso, C. Abate, 2018, Future medicinal chemistry.

Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity from σ2 receptor affinity in mixed P-gp/σ2 receptor agents.

F. Berardi, Mauro Niso, R. Luisi, 2015, European journal of medicinal chemistry.

From 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.

F. Berardi, R. Perrone, N. Colabufo, 2015, European journal of medicinal chemistry.

Novel and Selective Fluorescent σ2‐Receptor Ligand with a 3,4‐Dihydroisoquinolin‐1‐one Scaffold: A Tool to Study σ2 Receptors in Living Cells

F. Berardi, Mauro Niso, C. Riganti, 2015, Chembiochem : a European journal of chemical biology.

Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent and σ receptors binding properties.

E. Lacivita, F. Berardi, R. Perrone, 2014, Journal of medicinal chemistry.

Is the sigma2 receptor a histone binding protein?

F. Berardi, R. Perrone, N. Colabufo, 2006, Journal of medicinal chemistry.

4-Biphenyl and 2-naphthyl substituted 6,7-dimethoxytetrahydroisoquinoline derivatives as potent P-gp modulators.

A. Paradiso, F. Berardi, R. Perrone, 2008, Bioorganic & medicinal chemistry.

Correlation between sigma2 receptor protein expression and histopathologic grade in human bladder cancer.

F. Berardi, R. Perrone, N. Colabufo, 2006, Cancer letters.

The sigma-2 receptor agonist PB28 inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells.

F. Berardi, R. Perrone, N. Colabufo, 2006, Cell calcium.

σ2 Receptor and Its Role in Cancer with Focus on a MultiTarget Directed Ligand (MTDL) Approach

E. Lacivita, Mauro Niso, C. Abate, 2021, Molecules.

Antiproliferative and cytotoxic effects of some sigma2 agonists and sigma1 antagonists in tumour cell lines.

F. Berardi, R. Perrone, N. Colabufo, 2004, Naunyn-Schmiedeberg's archives of pharmacology.

Mitochondrial Membranes of Human SH-SY5Y Neuroblastoma Cells Express Serotonin 5-HT7 Receptor

E. Lacivita, M. Leopoldo, Mauro Niso, 2020, International journal of molecular sciences.

Human epididymal and prostatic tracts of vas deferens: different contraction response to noradrenaline stimulation in isolated organ bath assay.

F. Berardi, R. Perrone, N. Colabufo, 2007, European journal of pharmacology.

The Tertiary Amine Nitrogen Atom of Piperazine Sulfonamides as a Novel Determinant of Potent and Selective β3‐Adrenoceptor Agonists

Mauro Niso, M. Perrone, A. Scilimati, 2009, ChemMedChem.

Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.

F. Berardi, R. Perrone, N. Colabufo, 2012, Journal of medicinal chemistry.

3-benzazecine-based cyclic allene derivatives as highly potent P-glycoprotein inhibitors overcoming doxorubicin multidrug resistance.

A. V. Varlamov, N. Colabufo, Mauro Niso, 2019, Future medicinal chemistry.

A New Class of 1‐Aryl‐5,6‐dihydropyrrolo[2,1‐a]isoquinoline Derivatives as Reversers of P‐Glycoprotein‐Mediated Multidrug Resistance in Tumor Cells

N. Colabufo, Mauro Niso, M. de Candia, 2018, ChemMedChem.

Distribution of sigma receptors in EMT‐6 cells: preliminary biological evaluation of PB167 and potential for in‐vivo PET

F. Fazio, F. Berardi, R. Perrone, 2005, The Journal of pharmacy and pharmacology.

Towards metabolically stable 5-HT7 receptor ligands: a study on 1-arylpiperazine derivatives and related isosters

E. Lacivita, M. Leopoldo, F. Berardi, 2013, Experimental Brain Research.

Structure-activity relationship study towards non-peptidic positron emission tomography (PET) radiotracer for gastrin releasing peptide receptors: Development of [18F] (S)-3-(1H-indol-3-yl)-N-[1-[5-(2-fluoroethoxy)pyridin-2-yl]cyclohexylmethyl]-2-methyl-2-[3-(4-nitrophenyl)ureido]propionamide.

E. Lacivita, M. Leopoldo, R. Perrone, 2017, Bioorganic & medicinal chemistry.

Design and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties

H. Stark, E. Lacivita, M. Leopoldo, 2022, Molecules.

4-Nitro-2,1,3-benzoxadiazole derivatives as potential fluorescent sigma receptor probes

N. Colabufo, Mauro Niso, A. Rescifina, 2015 .

Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P‐glycoprotein inhibitors: the role of molecular flatness

C. Adamo, N. Colabufo, Mauro Niso, 2016, Chemical biology & drug design.

Trimethoxybenzanilide-based P-glycoprotein modulators: an interesting case of lipophilicity tuning by intramolecular hydrogen bonding.

F. Berardi, R. Perrone, N. Colabufo, 2014, Journal of medicinal chemistry.

1,2,3,4-Tetrahydroisoquinoline/2 H -chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1

N. Colabufo, Mauro Niso, L. Pisani, 2022 .

Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.

F. Berardi, R. Perrone, N. Colabufo, 2007, Journal of medicinal chemistry.

Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands for visualization of brain dopamine D3 receptors.

Francesco Berardi, Roberto Perrone, E. Lacivita, 2006, Journal of medicinal chemistry.

A Benzopyrane Derivative as a P‐Glycoprotein Stimulator: A Potential Agent to Decrease β‐Amyloid Accumulation in Alzheimer’s Disease

M. Leopoldo, F. Berardi, R. Perrone, 2012, ChemMedChem.

Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ₂ receptors.

S. Ametamey, F. Berardi, R. Perrone, 2013, European journal of medicinal chemistry.

1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.

N. Colabufo, Mauro Niso, L. Pisani, 2019, European journal of medicinal chemistry.

Electrochemical performance and transport properties of a Nafion membrane in a hydrogen-bromine cell environment

Mauro Niso, 1987 .

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Ureidopropanamides as Formyl Peptide Receptor 2 (FPR2) Agonists to Target the Resolution of Inflammation in Central Nervous System Disorders.

E. Lacivita, M. Leopoldo, Mauro Niso, 2022, Journal of medicinal chemistry.

Functional N‐Formyl Peptide Receptor 2 (FPR2) Antagonists Based on the Ureidopropanamide Scaffold Have Potential To Protect Against Inflammation‐Associated Oxidative Stress

E. Lacivita, M. Leopoldo, R. Perrone, 2017, ChemMedChem.

Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome.

E. Lacivita, M. Leopoldo, M. Ragozzino, 2020, European journal of medicinal chemistry.

Why PB28 Could Be a Covid 2019 Game Changer?

M. Leopoldo, F. Berardi, R. Perrone, 2020, ACS medicinal chemistry letters.

Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.

A. Paradiso, F. Berardi, R. Perrone, 2008, Bioorganic & medicinal chemistry.

Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.

P. Svenningsson, E. Lacivita, M. Leopoldo, 2015, Bioorganic & medicinal chemistry.

Analogues of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.

E. Lacivita, R. Perrone, Mauro Niso, 2011, Journal of medicinal chemistry.

Synthesis, 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.

G. Knudsen, E. Lacivita, M. Leopoldo, 2014, European journal of medicinal chemistry.

Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.

Sabina Podlewska, Andrzej J Bojarski, Luisa Speranza, 2016, European journal of medicinal chemistry.

Phenylsulfonylfuroxans as modulators of multidrug-resistance-associated protein-1 and P-glycoprotein.

F. Berardi, R. Perrone, N. Colabufo, 2010, Journal of medicinal chemistry.

Selective agonists for serotonin 7 (5-HT7) receptor and their applications in preclinical models: an overview

Giovanni Laviola, Walter Adriani, Francesco Berardi, 2014, Reviews in the neurosciences.

Rigid versus flexible anilines or anilides confirm the bicyclic ring as the hydrophobic portion for optimal σ2 receptor binding and provide novel tools for the development of future σ2 receptor PET radiotracers

F. Berardi, Mauro Niso, C. Abate, 2016 .

EGFR tyrosine kinase inhibitors and multidrug resistance: perspectives.

M. Leopoldo, F. Berardi, R. Perrone, 2011, Frontiers in bioscience.

Bicalutamide failure in prostate cancer treatment: involvement of Multi Drug Resistance proteins.

Giancarlo Albo, Francesco Berardi, Roberto Perrone, 2008, European journal of pharmacology.

Sigma‐2 Receptor Agonists as Possible Antitumor Agents in Resistant Tumors: Hints for Collateral Sensitivity

F. Berardi, R. Perrone, N. Colabufo, 2013, ChemMedChem.

Perspectives of P-glycoprotein modulating agents in oncology and neurodegenerative diseases: pharmaceutical, biological, and diagnostic potentials.

Francesco Berardi, Roberto Perrone, F. Berardi, 2010, Journal of medicinal chemistry.

Multi‐Drug‐Resistance‐Reverting Agents: 2‐Aryloxazole and 2‐Arylthiazole Derivatives as Potent BCRP or MRP1 Inhibitors

F. Berardi, R. Perrone, N. Colabufo, 2009, ChemMedChem.

Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents.

E. Lacivita, M. Leopoldo, F. Berardi, 2004, Journal of medicinal chemistry.

Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.

Anders Ettrup, Szabolcs Lehel, Matthias M Herth, 2014, Bioorganic & medicinal chemistry.

Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.

E. Lacivita, M. Leopoldo, F. Berardi, 2013, Bioorganic & medicinal chemistry letters.

Investigations 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.

P. Svenningsson, E. Lacivita, M. Leopoldo, 2012, Journal of medicinal chemistry.

Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.

F. Berardi, R. Perrone, N. Colabufo, 2008, Bioorganic & medicinal chemistry letters.

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.

E. Lacivita, M. Leopoldo, F. Berardi, 2007, Bioorganic & medicinal chemistry.

Elements in support of the 'non-identity' of the PGRMC1 protein with the σ2 receptor.

F. Berardi, Mauro Niso, A. Menga, 2015, European journal of pharmacology.

The interaction of celecoxib with MDR transporters enhances the activity of mitomycin C in a bladder cancer cell line

N. Colabufo, A. Azzariti, Mauro Niso, 2013, Molecular Cancer.

Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28).

F. Berardi, R. Perrone, N. Colabufo, 2009, Journal of medicinal chemistry.

Development of N-(1-Adamantyl)benzamides as Novel Anti-Inflammatory Multitarget Agents Acting as Dual Modulators of the Cannabinoid CB2 Receptor and Fatty Acid Amide Hydrolase.

M. Loza, J. Brea, E. Sotelo, 2022, Journal of medicinal chemistry.

Cannabinoid Receptor Subtype 2 (CB2R) in a Multitarget Approach: Perspective of an Innovative Strategy in Cancer and Neurodegeneration.

Mauro Niso, F. Intranuovo, G. Mangiatordi, 2020, Journal of medicinal chemistry.

Sigma-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

F. Berardi, Mauro Niso, W. Hawkins, 2017, BMC Cancer.

Interaction of the σ2 Receptor Ligand PB28 with the Human Nucleosome: Computational and Experimental Probes of Interaction with the H2A/H2B Dimer

R. Glennon, F. Berardi, R. Perrone, 2010, ChemMedChem.

New Pharmacological Strategies against Pancreatic Adenocarcinoma: The Multifunctional Thiosemicarbazone FA4

E. Giovannetti, A. Avan, Mauro Niso, 2022, Molecules.

PB28, 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

F. Berardi, N. Colabufo, Mauro Niso, 2020, Frontiers in Pharmacology.

F281, synthetic agonist of the sigma-2 receptor, induces Ca2+ efflux from the endoplasmic reticulum and mitochondria in SK-N-SH cells.

N. Colabufo, Mauro Niso, M. Contino, 2009, Cell calcium.

Development of Fluorescent 4-[4-(3H-Spiro[isobenzofuran-1,4′-piperidin]-1′-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques

E. Sotelo, Mauro Niso, C. Riganti, 2023, Journal of medicinal chemistry.

Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (σ2) receptor and P-gp protein in the cytotoxic action: In vitro and in vivo activity in pancreatic tumors.

F. Berardi, Mauro Niso, C. Riganti, 2018, European journal of medicinal chemistry.

Novel metal chelators thiosemicarbazones with activity at the σ2 receptors and P-glycoprotein: an innovative strategy for resistant tumor treatment

F. Berardi, Mauro Niso, S. Ferorelli, 2015 .

Collateral Sensitivity of sigma-2 Receptor ligands: Potentials in the Treatment of Multidrug Resistant Tumors

Mauro Niso, C. Riganti, C. Abate, 2014 .

Sigma-2 Receptor: Biomarker for Solid Tumor Diagnosis and Target for Tumor Treatment

Mauro Niso, 2013 .

2‐Aminopyridine Derivatives as Potential σ2 Receptor Antagonists

F. Berardi, R. Perrone, Mauro Niso, 2012, ChemMedChem.

PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma.

F. Berardi, R. Perrone, N. Colabufo, 2008, Bioorganic & medicinal chemistry letters.

Sigma-2 Receptor Ligand Binding Modulates Association between TSPO and TMEM97

R. Mach, Mauro Niso, M. Cahill, 2023, International journal of molecular sciences.

Multifunctional thiosemicarbazones targeting sigma receptors: in vitro and in vivo antitumor activities in pancreatic cancer models

F. Berardi, Mauro Niso, J. Kopecka, 2021, Cellular Oncology.

Sigma‐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

F. Berardi, M. Suematsu, Mauro Niso, 2017, Pharmacological research.

Fluorescent derivatives of σ receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.

F. Berardi, R. Perrone, Mauro Niso, 2011, Journal of medicinal chemistry.

In vitro and ex vivo characterization of sigma-1 and sigma-2 receptors: agonists and antagonists in biological assays.

R. Perrone, N. Colabufo, Mauro Niso, 2009, Central nervous system agents in medicinal chemistry.

Antiproliferative and cytotoxic effects of some σ2 agonists and σ1 antagonists in tumour cell lines

F. Berardi, R. Perrone, N. Colabufo, 2004, Naunyn-Schmiedeberg's Archives of Pharmacology.

In Vitro and In Silico Analysis of the Residence Time of Serotonin 5-HT7 Receptor Ligands with Arylpiperazine Structure: A Structure-Kinetics Relationship Study.

C. Perrone-Capano, E. Lacivita, M. Leopoldo, 2022, ACS chemical neuroscience.

Knowledge-Based Design of Long-Chain Arylpiperazine Derivatives Targeting Multiple Serotonin Receptors as Potential Candidates for Treatment of Autism Spectrum Disorder.

M. Loza, E. Lacivita, M. Leopoldo, 2021, ACS chemical neuroscience.

Investigation of σ receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.

F. Berardi, R. Perrone, Mauro Niso, 2013, Bioorganic & medicinal chemistry.

Novel 4-(4-aryl)cyclohexyl-1-(2-pyridyl)piperazines as Delta(8)-Delta(7) sterol isomerase (emopamil binding protein) selective ligands with antiproliferative activity.

M. Leopoldo, F. Berardi, R. Perrone, 2008, Journal of medicinal chemistry.

Novel 4-( 4-Aryl ) cyclohexyl-1-( 2-pyridyl ) piperazines as ∆ 8-∆ 7 Sterol Isomerase ( Emopamil Binding Protein ) Selective Ligands with Antiproliferative Activity

M. Leopoldo, F. Berardi, R. Perrone, 2008 .