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Discovery and Preclinical Characterization of I-0436650, a Selective SHP2 Allosteric Inhibitor for RAS-Driven CancersTargeted therapies for RAS-driven cancers can deliver strong initial responses, but tumors often develop adaptive…Discovery and Optimization of IRBM-Z-2, an Allosteric Zika Virus NS2B–NS3 Protease Inhibitor Exhibiting In Vivo EfficacyFrom Hit to Lead: The Chemistry Story Behind IRBM-Z-2 Every successful drug candidate begins with…
Plasma metabolomic profiling identifies a metabolic signature for non–muscle-invasive bladder cancer independent of hematuriaNon-Muscle Invasive Bladder Cancer (NMIBC) and the Challenge of Long-Term Surveillance Non-muscle-invasive bladder cancer (NMIBC)…
An allosteric inhibitor of the Zika virus NS2B-NS3 protease with oral efficacy in mouse modelsZika Virus as a Therapeutic Target Zika virus (ZIKV) represents a persistent global health threat,…
Novel azabicyclic series of potent SHP2 allosteric inhibitorsSHP2 as a Therapeutic Target Src homology phosphotyrosine phosphatase 2 (SHP2), encoded by PTPN11, is…
Modulation of huntingtin S421 phosphorylation in a Huntington’s disease mouse model and its detection in nonhuman primate cerebrospinal fluidHuntington’s disease (HD) is a progressive neurodegenerative disease caused by the expansion of a CAG…
De novo discovery of cyclic peptide inhibitors of IL-11 signalingUnlocking New Avenues for IL-11 Therapeutics Interleukin-11 (IL-11), a member of the cytokine family, has…
Tandem mass spectrometry-based assay for heparan-N-sulphatase in paediatric CSF: A potential pharmacodynamic biomarker for mucopolysaccharidosis type IIIA therapyUltra-sensitive tandem mass spectrometry-based assay development and validation The article, “ LC-MS/MS Assay for Heparan-N-Sulphatase…
A patent review of SHP2 allosteric inhibitors (2018-present)Petrocchi, A., & Ciammaichella, A. (2024). A patent review of SHP2 allosteric inhibitors (2018-present). Expert…
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitorsSimona Ponzi, Federica Ferrigno, Monica Bisbocci, Cristina Alli, Jesus M. Ontoria, Alessia Petrocchi, Carlo Toniatti,…
The Urine Metabolome of R6/2 and zQ175DN Huntington’s Disease Mouse ModelsSpeziale R, Montesano C, Di Pietro G, Cicero DO, Summa V, Monteagudo E, Orsatti L.…
Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein ReceptorOur peptide chemistry team is excited to announce a new publication in the journal “Circulation”,…
Discovery of a Novel Series of Potent SHP2 Allosteric InhibitorsPetrocchi A, Grillo A, Ferrante L, Randazzo P, Prandi A, De Matteo M, Iaccarino C,…
Discovery of a Novel Series of Imidazopyrazine Derivatives as Potent SHP2 Allosteric InhibitorsBy Esther Torrente, Valentina Fodale, Alina Ciammaichella, Federica Ferrigno, Jesus M. Ontoria, Simona Ponzi, Ilaria…
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and DiabetesThe IRBM peptide chemistry team is proud to announce a new publication in ACS Medicinal…
Novel gametocyte-specific and all-blood-stage transmission-blocking chemotypes from high throughput screening on Plasmodium falciparum gametocytesBy Paonessa, G., Siciliano, G., Graziani, R., Lalli, C., Cecchetti, O., Alli, C., La Valle,…
Efficacy of PEGylated ciliary neurotrophic factor superagonist variant in diet-induced obesity miceAt IRBM, we are passionate about understanding the underlying biology of disease, to drive drugdiscovery.…
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 proteaseStefania Colarusso, Federica Ferrigno, Simona Ponzi, Francesca Pavone, Immacolata Conte, Luigi Abate, Elisa Beghetto, Antonino…
Guiding chemically synthesized peptide drug lead optimization by de-risking mast cell degranulation related toxicities of a NaV1.7 peptide inhibitorPeptides can induce non IgE-mediated anaphylactoid reactions. These effects are triggered by the direct interaction…
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of PainTargeting ion channels involved in nociception is currently being investigated for the treatment of pain.…
Oligomerization, albumin binding and catabolism of therapeutic peptides in the subcutaneous compartment: an investigation on lipidated GLP-1 analogsWe are delighted to publish our first paper of 2022 in the Journal of Pharmaceutical…
IRBM & Heidelberg University Hospital publishes in Cell Reports Medicine on kynurenine pathway activation and deviation to anthranilic and kynurenic acid in fibrosing chronic Graft-Versus-Host DiseaseOur Biomarkers team, in collaboration with Dr. Thomas Luft group at the Heidelberg University Hospital…
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 InhibitorsFollowing the first report in the Journal of Medicinal Chemistry in 2020, the IRBM peptide…
Discovery and characterization of novel peptide inhibitors of the NRF2/MAFG/DNA ternary complex for the treatment of cancerOur Peptide Chemistry team, in collaboration with scientists at Merck & Co., Inc., Rahway, NJ, USA, reported on the…
Targeting of eIF6-driven translation induces a metabolic rewiring that reduces NAFLD and the consequent evolution to hepatocellular carcinomaAt IRBM we are passionate about helping companies develop medicines in a wide range of…
IRBM cited in UniQure publication on using HTT-lowering therapies to slow down neurodegeneration in Huntington’s DiseaseUniQure has just published a study in Science Translational Medicine using a Huntingtin (HTT)-lowering therapy.…
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular DiseasesOur integrated drug discovery efforts on the Relaxin-2 peptide hormone, in collaboration with our collaborators…Cyclic Phosphopantothenic Acid Prodrugs for Treatment of Pantothenate Kinase-Associated NeurodegenerationMutations in the human PANK2 gene are implicated in neurodegenerative diseases such as pantothenate kinase-associated…Analysis of mutant and total huntingtin expression in Huntington’s disease murine modelsHuntington’s disease (HD) is a monogenetic neurodegenerative disorder that is caused by the expansion of…NRF2 activation by reversible KEAP1 binding induces the antioxidant response in primary neurons and astrocytes of a Huntington’s disease mouse modelOxidative stress has been associated with pathogenesis in several diseases including Huntington’s disease (HD), a…Optimization of Linear and Cyclic Peptide Inhibitors of KEAP1-NRF2 Protein-Protein InteractionStefania Colarusso, Daniele De Simone, Tommaso Frattarelli, Matteo Andreini, Mauro Cerretani, Antonino Missineo, Daniele Moretti,…Discovery of the First Human Arylsulfatase A Reversible Inhibitor Impairing Mouse Oocyte FertilizationBy Caroselli Silvia; Canipari Rita; Zwergel Clemens; Pirolli Adele; Sabatino Manuela; Mai Antonello; Valente Sergio;…Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-Coil Domain TruncationsBy Brown Zachary Z; Mapelli Claudio; McCracken Amy Bittner; Chen Kuanchang; Zhu Xiaohong; Garbaccio Robert…Discovery and Preliminary Characterization of Translational Modulators that Impair the Binding of eIF6 to 60S Ribosomal SubunitsBy Pesce Elisa; Miluzio Annarita; Cirino Delia; Calamita Piera; Manfrini Nicola; Oliveto Stefania; Ricciardi Sara;…Luminescence-Based, Low- and Medium-Throughput Assays for Drug Screening in Schistosoma mansoni Larval StageBy Guidi Alessandra; Gimmelli Roberto; Ruberti Giovina; Bresciani Alberto From Methods in molecular biology (Clifton,…A novel member of Prame family, Gm12794c, counteracts retinoic acid differentiation through the methyltransferase activity of PRC2By Napolitano Giuliana; Fusco Salvatore; Cirillo Carmine; De Martino Ilaria; Addeo Martina; Falco Geppino; Tagliaferri…Synthesis and Antiproliferative Activity of Nitric Oxide-Donor Largazole ProdrugsBy Borgini Matteo; Zamperini Claudio; Poggialini Federica; Botta Maurizio; Zamperini Claudio; Botta Maurizio; Ferrante Luca;…The miRNAs Role in Melanoma and in Its Resistance to TherapyBy Varrone Francesca; Caputo Emilia From International journal of molecular sciences (2020), 21(3), , Language:…
Ultrasensitive quantitative measurement of huntingtin phosphorylation at residue S13By Cariulo, Cristina; Verani, Margherita; Martufi, Paola; Ingenito, Raffaele; Finotto, Marco; Deguire, Sean M.; Lavery,…
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based DesignIn the last few years macrocyclic peptides have emerged as a better class of lead…
IRBM & collaborators publish on techniques for characterizing peptides in Type 2 diabetes and a peptide drug discovery program for Huntington’s diseaseNowadays, there is a strong drive to explore new areas of chemical space in search…
IRBM publishes in J. Peptide Science on methods to study catabolism, key to designing more stable peptidesIRBM used liquid chromatography-high resolution mass spectrometry to explore different methods for the study of…
A spectroscopic and molecular dynamics study on the aggregation process of a long-acting lipidated therapeutic peptide: the case of semaglutideM. Venanzi, M. Savioli, R. Cimino, E. Gatto, A. Palleschi, G. Ripani, D. Cicero, E.…IRBM & CHDI Foundation publishes in J. MedChem on potential imaging biomarker for Huntington’s diseaseScience advances by collaborations and publications. Over the last decade, IRBM has done significant research…
IRBM & University of Rome publishes in PLOS on new chemotype with antiparasitic activity for treating sleeping sicknessTrypanosoma brucei is a parasite responsible for human African trypanosomiasis, also known as sleeping sickness,…
IRBM publishes on optimizing a new series of Trypanosoma brucei growth inhibitors, the parasite responsible of the sleeping sicknessHuman African trypanosomiasis (HAT) , also known as sleeping sickness, is a parasitic disease that…
IRBM & University of Rome publishes in Nature on crucial signaling pathway in muscle homeostasis and regenerationIRBM, working with the University of Rome’s Department of Biology, examined signaling pathways involved with…
IRBM’s publishes in Cells on establishing a human blood-brain barrier model for use in drug discovery for neurodegenerative diseases such as Huntington’sUnderstanding the Blood-Brain Barrier (BBB) and Its Role in CNS Drug Development The blood-brain barrier…
Combined Peptide and Small-Molecule Approach Toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 InteractionThe NRF2/ARE signalling pathway is a key mediator in oxidative stress and therefore a potential…
Dihydroxypyrimidine Scaffold to Target HIV‑1 Nucleocapsid ProteinIRBM and their collaborators’ at the universities of Strasbourg and Siena have recently published a…
IRBM publishes in Nature Scientific Reports on the Janus effect of glucocorticoids on the differentiation of muscle fibro/adipogenic progenitorsFibro-adipogenic progenitors (FAPs) are known to cause muscle impairment in non-physiological settings, such as aging…
Discovery of 4-((1-(1H-imidazol-2-yl)alkoxy)methyl)pyridines as a new class of Trypanosoma cruzi growth inhibitorsStopping the night time kissing bug: IRBM’s scientists recently published a Bioorganic & medicinal chemistry…
Ring Finger Protein 11 acts on ligand-activated EGFR via the direct interaction with the UIM region of ANKRD13 protein familyMattioni A, Boldt K, Auciello G, Komada M, Rappoport JZ, Ueffing M, Castagnoli L, Cesareni…
Whole-Genome Phage Display Libraries: A Powerful Tool for Antigen DiscoveryBeghetto E, Gargano N. Whole-Genome Phage Display Libraries: A Powerful Tool for Antigen Discovery. Methods…Developmental abnormalities in cortical GABAergic system in mice lacking mGlu3 metabotropic glutamate receptors.By Imbriglio Tiziana; Verhaeghe Remy; Pascarelli Maria Teresa; Chece Giuseppina; Del Percio Claudio; Fucile Sergio;…Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNSBy Bencheva Leda Ivanova; De Matteo Marilenia; Ferrante Luca; Ferrara Marco; Prandi Adolfo; Randazzo Pietro;…
Application of an in Vitro Blood−Brain Barrier Model in the Selection of Experimental Drug Candidates for the Treatment of Huntington’s DiseaseBy Di Marco, Annalise; Gonzalez Paz, Odalys; Fini, Ivan; Vignone, Domenico; Cellucci, Antonella; Battista, Maria…Salivary Metabolome and Soccer Match: Challenges for Understanding Exercise induced Changes.By Pitti Erica; Petrella Greta; Cicero Daniel Oscar; Di Marino Sara; Summa Vincenzo; Perrone Marco;…Fish-derived antimicrobial peptides: Activity of a chionodracine mutant against bacterial models and human bacterial pathogens.By Buonocore Francesco; Picchietti Simona; Porcelli Fernando; Della Pelle Giulia; Poerio Elia; Fausto Anna Maria;…Omomyc Reveals New Mechanisms To Inhibit the MYC Oncogene.By Demma Mark J; O’Neil Jennifer; Mapelli Claudio; Walji Abbas; Sun Angie; Zelina John; Hall…Development and characterization of cellular biosensors for HTS of erythroid differentiation inducers targeting the transcriptional activity of γ-globin and β-globin gene promoters.By Breveglieri Giulia; Finotti Alessia; Cosenza Lucia Carmela; Zuccato Cristina; Borgatti Monica; Gambari Roberto; Breveglieri…Aspergillus olivimuriae sp. nov., a halotolerant species isolated from olive brine.By Crognale Silvia; Pesciaroli Lorena; Felli Martina; Petruccioli Maurizio; D’Annibale Alessandro; Bresciani Alberto; Peterson Stephen…Multiple Synthetic Routes to the Mini-Protein Omomyc and Coiled-coil Domain Truncations.Brown ZZ, Mapelli C, Farasat I, Shoultz AV, Orvieto F, Santoprete A, Bianchi E, Johnson…
Phospho-S129 Alpha-Synuclein Is Present in Human Plasma but Not in Cerebrospinal Fluid as Determined by an Ultrasensitive Immunoassay.By Cariulo Cristina; Martufi Paola; Verani Margherita; Azzollini Lucia; Caricasole Andrea; Petricca Lara; Bruni Giordana;…The Outcomes of Decorated Prolines in the Discovery of Antimicrobial Peptides from Temporin-L.By Buommino Elisabetta; Carotenuto Alfonso; Antignano Ignazio; Bellavita Rosa; Merlino Francesco; Novellino Ettore; Brancaccio Diego;…A novel member of Prame family, Gm12794c, counteracts retinoic acid differentiation through the methyltransferase activity of PRC2.Napolitano G, Tagliaferri D, Fusco S, Cirillo C, De Martino I, Addeo M, Mazzone P,…Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agent.By Saccoliti Francesco; Madia Valentina Noemi; Tudino Valeria; De Leo Alessandro; Pescatori Luca; Messore Antonella;…Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery.By Borbely Adina; Figueras Eduard; Martins Ana; Kemker Isabell; Frese Marcel; Sewald Norbert; Martins Ana;…Inhibiting pathologically active ADAM10 rescues synaptic and cognitive decline in Huntington’s disease.By Vezzoli Elena; Caron Ilaria; Besusso Dario; Conforti Paola; Battaglia Elisa; Rivetti di Val Cervo…Collagen Prolyl Hydroxylation-Dependent Metabolic Perturbation Governs Epigenetic Remodeling and Mesenchymal Transition in Pluripotent and Cancer Cells.By D’Aniello Cristina; Cermola Federica; Migliaccio Agnese; Casalino Laura; De Cesare Dario; Patriarca Eduardo J;…Octreotide Conjugates for Tumor Targeting and Imaging.By Figueras Eduard; Martins Ana; Borbely Adina; Frese Marcel; Sewald Norbert; Martins Ana; Gallinari Paola;…Bromoindirubin-3′-oxime intercepts GSK3 signaling to promote and enhance skeletal muscle differentiation affecting miR-206 expression in miceBy Ragozzino, Elvira; Brancaccio, Mariarita; Di Costanzo, Antonella; Scalabri, Francesco; Andolfi, Gennaro; Wanderlingh, Luca G.;…Frataxin Structure and FunctionBy Castro Ignacio Hugo; Pignataro Maria Florencia; Sewell Karl Ellioth; Herrera Maria Georgina; Noguera Martin…Sulphide as a leaving group: highly stereoselective bromination of alkyl phenyl sulphidesBy Canestrari Daniele; Cioffi Caterina; Biancofiore Ilaria; Lancianesi Stefano; Ghisu Lorenza; Adamo Mauro F A;…An Ig Transmembrane Domain Motif Improves the Function of TCRs Transduced in Human T Cells: Implications for ImmunotherapyBy D’Apice Luciana; Cipria Deborah; Sartorius Rossella; Coscia Maria R; Oreste Umberto; Marzullo Vincenzo M;…Improved selective class I HDAC and novel selective HDAC3 inhibitors: Beyond hydroxamic acids and benzamidesBy Bresciani, Alberto; Ontoria, Jesus M.; Biancofiore, Ilaria; Cellucci, Antonella; Ciammaichella, Alina; Di Marco, Annalise;…A novel method using nuclear magnetic resonance for plasma proteinbinding assessment in drug discovery programs.By Gallo, Mariana; Matteucci, Sara; Alaimo, Nadine; Pitti, Erica; Orsale, Maria V.; Summa, Vincenzo; Cicero,…Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid ProteinBy Mori Mattia; Dasso Lang Maria Chiara; Palombi Nastasja; Friggeri Laura; Botta Maurizio; Saladini Francesco;…Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.By Nizi, Emanuela; Sferrazza, Alessio; Fabbrini, Danilo; Nardi, Valentina; Andreini, Matteo; Graziani, Rita; Gennari, Nadia;…Quantifying autophagy using novel LC3B and p62 TR-FRET assays.By Bresciani, Alberto; Spiezia, Maria Carolina; Boggio, Roberto; Cariulo, Cristina; Nordheim, Anja; Altobelli, Roberta; Kuhlbrodt,…Determination of acetyl coenzyme A in human whole blood by ultra-performance liquid chromatography-mass spectrometryBy Speziale, Roberto; Montesano, Camilla; De Leonibus, Maria Lucia; Bonelli, Fabio; Fezzardi, Paola; Beconi, Maria…Early metabolic response to acute myocardial ischaemia in patients undergoing elective coronary angioplasty.By Di Marino Sara; Lembo Angelo; Summa Vincenzo; Cicero Daniel Oscar; Viceconte Nicola; Tanzilli Gaetano;…Fosmetpantotenate (RE-024), a phosphopantothenate replacement therapy for pantothenate kinase-associated neurodegeneration: Mechanism of action and efficacy in nonclinical models.By Elbaum Daniel; Beconi Maria G; Quinton Maria S; Vaino Andrew; Monteagudo Edith; Di Marco…A liquid chromatography high-resolution mass spectrometry in vitro assay to assess metabolism at the injection site of subcutaneously administered therapeutic peptides.Esposito S, de Leonibus ML, Ingenito R, Bianchi E, Orsatti L, Monteagudo E. (2018) J…Development of a Broadly Applicable Assay for Measurement of Glycan-Directed Enzymatic Activity.By Bresciani, Alberto; Cecchetti, Ottavia; Missineo, Antonino; Pacifici, Pier Giorgio; Tomei, Licia; Rodems, Steven From…Identification and binding mode of a novel Leishmania Trypanothione reductase inhibitor from high throughput screeningBy Turcano, Lorenzo; Torrente, Esther; Missineo, Antonino; Andreini, Matteo; Gramiccia, Marina; Muccio, Trentina Di; Genovese,…Identification of novel multi-stage histone deacetylase (HDAC) inhibitors that impair Schistosoma mansoni viability and egg productionBy Guidi Alessandra; Saccoccia Fulvio; Gimmelli Roberto; Lalli Cristiana; Papoff Giuliana; Ruberti Giovina; Gennari Nadia;…Structure-Based Identification of HIV-1 Nucleocapsid Protein Inhibitors Active against Wild-Type and Drug-Resistant HIV-1 StrainsBy Mori Mattia; Dasso Lang Maria Chiara; Botta Maurizio; Kovalenko Lesia; Pires Manuel; Humbert Nicolas;…Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitroBy Ferrigno, Federica; Biancofiore, Ilaria; Malancona, Savina; Ponzi, Simona; Paonessa, Giacomo; Graziani, Rita; Bresciani, Alberto;…DNA replication and repair kinetics of Alu, LINE-1 and satellite III genomic repetitive elementsBy Natale Francesco; Scholl Annina; Rapp Alexander; Yu Wei; Rausch Cathia; Cardoso M Cristina; Natale…
Polypharmacy through Phage Display: Selection of Glucagon and GLP-1 Receptor Co-agonists from a Phage-Displayed Peptide Library.Demartis A, Lahm A, Tomei L, Beghetto E, Di Biasio V, Orvieto F, Frattolillo F,…Phosphorylation of huntingtin at residue T3 is decreased in Huntington’s disease and modulates mutant huntingtin protein conformation.By Cariulo, Cristina; Azzollini, Lucia; Verani, Margherita; Martufi, Paola; Boggio, Roberto; Chiki, Anass; Deguire, Sean…Validation of Ultrasensitive Mutant Huntingtin Detection in Human Cerebrospinal Fluid by Single Molecule Counting Immunoassay.By Fodale, Valentina; Boggio, Roberto; Daldin, Manuel; Cariulo, Cristina; Spiezia, Maria Carolina; Byrne, Lauren M.;…Crosstalk between mismatch repair and base excision repair in human gastric cancerBy Simonelli Valeria; Leuzzi Giuseppe; Basile Giorgia; D’Errico Mariarosaria; Fortini Paola; Franchitto Annapaola; Parlanti Eleonora;…Designing an effective peptide vaccineBy Bianchi, E.; Pessi, A. From RSC Drug Discovery Series (2017), 59(Peptide-Based Drug Discovery), 364-390.…Structure-Based Identification of HIV-1 Nucleocapsid Protein Inhibitors Active against Wild-Type and Drug-Resistant HIV-1 Strains.Mori M, Kovalenko L, Malancona S, Saladini F, De Forni D, Pires M, Humbert N,…Discovery by organism based high-throughput screening of new multi-stage compounds affecting Schistosoma mansoni viability, egg formation and production.By Guidi Alessandra; Lalli Cristiana; Gimmelli Roberto; Saccoccia Fulvio; Ruberti Giovina; Nizi Emanuela; Andreini Matteo;…Nuclear factor (erythroid-derived 2)-like 2 (NRF2) drug discovery: Biochemical toolbox to develop NRF2 activators by reversible binding of Kelch-like ECH-associated protein 1 (KEAP1).By Bresciani, Alberto; Missineo, Antonino; Gallo, Mariana; Cerretani, Mauro; Fezzardi, Paola; Tomei, Licia; Cicero, Daniel…Largazole Analogues as Histone Deacetylase Inhibitors and Anticancer Agents: An Overview of Structure-Activity Relationships.By Poli Giulio; Botta Maurizio; Di Fabio Romano; Ferrante Luca; Di Fabio Romano; Summa Vincenzo…Insights on the conformational dynamics of human frataxin through modifications of loop-1.By Noguera Martin E; Vazquez Diego S; Herrera Maria Georgina; Roman Ernesto A; Aran Martin;…Vitamin B12 ameliorates the phenotype of a mouse model of DiGeorge syndrome.By Lania Gabriella; Colonna Vincenza; Baldini Antonio; Bresciani Alberto; Bisbocci Monica; Francone Alessandra; Altamura Sergio;…High-Affinity “Click” RGD Peptidomimetics as Radiolabeled Probes for Imaging av ß3 Integrin.By Piras Monica; Testa Andrea; Fleming Ian N; Dall’Angelo Sergio; Andriu Alexandra; Zanda Matteo; Menta…Polyglutamine expansion affects huntingtin conformation in multiple Huntington’s disease models.By Daldin, Manuel; Fodale, Valentina; Cariulo, Cristina; Azzollini, Lucia; Verani, Margherita; Martufi, Paola; Spiezia, Maria…An efficient liquid chromatography-high resolution mass spectrometry approach for the optimization of the metabolic stability of therapeutic peptides.By Esposito, Simone; Mele, Riccardo; Ingenito, Raffaele; Bianchi, Elisabetta; Bonelli, Fabio; Monteagudo, Edith; Orsatti, Laura…PINK1 and BECN1 relocalize at mitochondria-associated membranes during mitophagy and promote ER-mitochondria tethering and autophagosome formation.By Gelmetti Vania; Valente Enza Maria; De Rosa Priscilla; Torosantucci Liliana; Marini Elettra Sara; Romagnoli…Mitotic cell death induction by targeting the mitotic spindle with tubulin-inhibitory indole derivative molecules.By Di Cesare Erica; Verrico Annalisa; Miele Andrea; Giubettini Maria; Rovella Paola; Cundari Enrico; Lavia…Identification by High-Throughput Screening of Pseudomonas Acyl-Coenzyme A Synthetase Inhibitors.By Turcano, Lorenzo; Visaggio, Daniela; Frangipani, Emanuela; Missineo, Antonino; Andreini, Matteo; Altamura, Sergio; Visca, Paolo;…Understanding the Molecular Determinant of Reversible Human Monoamine Oxidase B Inhibitors Containing 2H-Chromen-2-One Core: Structure-Based and Ligand-Based Derived Three-Dimensional Quantitative Structure-Activity Relationships Predictive Models.By Mladenovic Milan; Patsilinakos Alexandros; Pirolli Adele; Sabatino Manuela; Ragno Rino; Patsilinakos Alexandros; Ragno Rino;…Crosstalk between mismatch repair and base excision repair in human gastric cancer.Simonelli V, Leuzzi G, Basile G, D’Errico M, Fortini P, Franchitto A, Viti V, Brown…Conformational modulation mediated by polyglutamine expansion in CAG repeat expansion disease-associated proteins.By Verani, Margherita; Bustamante, Maria; Martufi, Paola; Daldin, Manuel; Cariulo, Cristina; Azzollini, Lucia; Fodale, Valentina;…Vitamin B12 ameliorates the phenotype of a mouse model of DiGeorge syndrome.By Lania Gabriella; Colonna Vincenza; Bresciani Alberto; Bisbocci Monica; Francone Alessandra; Altamura Sergio; Baldini Antonio…Discovery and Characterization of Novel Anti-schistosomal Properties of the Anti-anginal Drug, Perhexiline and Its Impact on Schistosoma mansoni Male and Female Reproductive Systems.By Guidi Alessandra; Lalli Cristiana; Ruberti Giovina; Perlas Emerald; Bolasco Giulia; Nibbio Martina; Monteagudo Edith;…MK-4101, a Potent Inhibitor of the Hedgehog Pathway, Is Highly Active against Medulloblastoma and Basal Cell Carcinoma.By Filocamo Gessica; Brunetti Mirko; Colaceci Fabrizio; Sasso Romina; Tanori Mirella; Pasquali Emanuela; Mancuso Mariateresa;…Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.By Ontoria, Jesus M.; Paonessa, Giacomo; Ponzi, Simona; Ferrigno, Federica; Nizi, Emanuela; Biancofiore, Ilaria; Malancona,…Use of ‘dilute-and-shoot’ liquid chromatography-high resolution mass spectrometry in preclinical research: application to a DMPK study of perhexiline in mouse plasma.By Esposito, Simone; Bracacel, Elena; Nibbio, Martina; Speziale, Roberto; Orsatti, Laura; Veneziano, Maria; Monteagudo, Edith;…Development and validation of a luminescence-based, medium-throughput assay for drug screening in Schistosoma mansoni.By Lalli Cristiana; Guidi Alessandra; Ruberti Giovina; Gennari Nadia; Altamura Sergio; Bresciani Alberto From PLoS…Polyglutamine- and temperature-dependent conformational rigidity in mutant huntingtin revealed by immunoassays and circular dichroism spectroscopy.Fodale V, Kegulian NC, Verani M, Cariulo C, Azzollini L, Petricca L, Daldin M, Boggio…A single-run liquid chromatography mass spectrometry method to quantify neuroactive kynurenine pathway metabolites in rat plasma.By Orsatti, Laura; Speziale, Roberto; Orsale, Maria Vittoria; Caretti, Fulvia; Veneziano, Maria; Zini, Matteo; Monteagudo,…High Affinity Binders to EphA2 Isolated from Abdurin Scaffold Libraries; Characterization, Binding and Tumor Targeting.By Ullman Christopher; Mathonet Pascale; Oleksy Arkadiusz; Diamandakis Agata; Tomei Licia; Demartis Anna; Nardi Chiara;…Detection of huntingtin exon 1 phosphorylation by Phos-Tag SDS-PAGE: Predominant phosphorylation on threonine 3 and regulation by IKKß.By Bustamante, Maria Blaire; Ansaloni, Annalisa; Pedersen, Jeppe Falsig; Azzollini, Lucia; Cariulo, Cristina; Wang, Zhe-Ming;…A chemogenomic screening identifies CK2 as a target for pro-senescence therapy in PTEN-deficient tumours.By Kalathur Madhuri; Chen Jingjing; Revandkar Ajinkya; Alimonti Andrea; Toso Alberto; Guccini Ilaria; Alajati Abdullah;…Peptide nucleic acids targeting ß-globin mRNAs selectively inhibit hemoglobin production in murine erythroleukemia cells.By Montagner Giulia; Gemmo Chiara; Fabbri Enrica; Bianchi Nicoletta; Finotti Alessia; Breveglieri Giulia; Salvatori Francesca;…Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous RecombinationBy Philip Jones, Keith Wilcoxen, Michael Rowley, and Carlo Toniatti Journal of Medicinal Chemistry 2015…Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells.By Bridges Kathleen A; Liu Huifeng; Meyn Raymond E; Toniatti Carlo; Buser Carolyn A; Buchholz…Immunogenicity and therapeutic efficacy of a dual-component genetic cancer vaccine cotargeting carcinoembryonic antigen and HER2/neu in preclinical models.By Aurisicchio, Luigi; Peruzzi, Daniela; Koo, Gloria; Wei, Wei-Zen; La Monica, Nicola; Ciliberto, Gennaro From…Polyglutamine- and temperature-dependent conformational rigidity in mutant huntingtin revealed by immunoassays and circular dichroism spectroscopyBy Fodale, Valentina; Kegulian, Natalie C.; Verani, Margherita; Cariulo, Cristina; Azzollini, Lucia; Petricca, Lara; Daldin,…Development of a neuromedin U-human serum albumin conjugate as a long-acting candidate for the treatment of obesity and diabetes. Comparison with the PEGylated peptide.By Neuner, Philippe; Peier, Andrea M.; Talamo, Fabio; Ingallinella, Paolo; Lahm, Armin; Barbato, Gaetano; Di…A transgenic minipig model of Huntington’s DiseaseBy Baxa Monika; Macakova Monika; Hruska-Plochan Marian; Juhas Stefan; Pavlok Antonin; Juhasova Jana; Klima Jiri;…A PEGylated analog of the gut hormone oxyntomodulin with long-lasting antihyperglycemic, insulinotropic and anorexigenic activity.By Bianchi, Elisabetta; Carrington, Paul E.; Ingallinella, Paolo; Finotto, Marco; Santoprete, Alessia; Petrov, Aleksandr; Eiermann,…Further molecular characterisation of the OVT73 transgenic sheep model of Huntington’s disease identifies cortical aggregates.By Reid Suzanne J; Patassini Stefano; Handley Renee R; Waldvogel Henry J; Faull Richard L…PEGylation of Neuromedin U yields a promising candidate for the treatment of obesity and diabetes.By Ingallinella, Paolo; Peier, Andrea M.; Pocai, Alessandro; Di Marco, Annalise; Desai, Kunal; Zytko, Karolina;…Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.By Harper, Steven; McCauley, John A.; Rudd, Michael T.; Ferrara, Marco; DiFilippo, Marcello; Crescenzi, Benedetta;…Development of a scalable chiral synthesis of MK-3281, an inhibitor of the hepatitis C virus NS5B polymeraseBy Colarusso, Stefania; Conte, Immacolata; Di Filippo, Marcello; Ercolani, Caterina; MacKay, Angela C.; Palumbi, Maria…Mechanistic implications for LDL receptor degradation from the PCSK9/LDLR structure at neutral pH.By Lo Surdo, Paola; Bottomley, Matthew J.; Calzetta, Alessandra; Settembre, Ethan C.; Cirillo, Agostino; Pandit,…Structure of herpes simplex virus glycoprotein D bound to the human receptor nectin-1.By Di Giovine, Paolo; Settembre, Ethan C.; Bhargava, Arjun K.; Luftig, Micah A.; Lou, Huan;…Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.By Ontoria, Jesus M.; Bufi, Laura Llauger; Torrisi, Caterina; Bresciani, Alberto; Giomini, Claudia; Rowley, Michael;…N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.By Muraglia, Ester; Ontoria, Jesus M.; Branca, Danila; Dessole, Gabriella; Bresciani, Alberto; Fonsi, Massimiliano; Giuliano,…Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.By Malancona, Savina; Altamura, Sergio; Filocamo, Gessica; Kinzel, Olaf; Hernando, Jose Ignacio Martin; Rowley, Michael;…Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.By Kinzel, Olaf; Alfieri, Anna; Altamura, Sergio; Brunetti, Mirko; Bufali, Simone; Colaceci, Fabrizio; Ferrigno, Federica;…Intratumor RNA interference of cell cycle genes slows down tumor progression.By Dharmapuri, S.; Peruzzi, D.; Marra, E.; Palombo, F.; Bett, A. J.; Bartz, S. R.;…The discovery of Isentress, the first in class HIV integrase inhibitor: from hit to drugBy Summa, Vincenzo Edited By:Marcantoni, Enrico; Renzi, Gabriele From Seminars in Organic Synthesis, “A. Corbella”…Advances in the development of macrocyclic inhibitors of hepatitis C virus NS3-4A proteaseBy Avolio, Salvatore; Summa, Vincenzo From Current Topics in Medicinal Chemistry (Sharjah, United Arab Emirates)…Regioselective synthesis of 7,8-dihydropyrrolo[1,2-a]pyrimidin-4(6H)-ones and 7,8-dihydropyrrolo[1,2-a]pyrimidin-2(6H)-onesBy Donghi, Monica; Pesci, Silvia; Summa, Vincenzo; Koch, Uwe; Spieser, Stephane; Gardelli, Cristina From Synlett…Kinase bypass approach for the treatment of Hepatitis C virus infectionBy Narjes, Frank; Donghi, Monica; Meppen, Malte; Attenni, Barbara; Pacini, Barbara; Olsen, David B.; Carroll,…Growth delay of human bladder cancer cells by Prostate Stem Cell Antigen downregulation is associated with activation of immune signaling pathwaysBy Marra, Emanuele; Uva, Paolo; Viti, Valentina; Simonelli, Valeria; Dogliotti, Eugenia; De Rinaldis, Emanuele; Lahm,…Coadministration of telomerase genetic vaccine and a novel TLR9 agonist in nonhuman primates. [Erratum to document cited in CA151:356283]By Dharmapuri, Sridhar; Peruzzi, Daniela; Mennuni, Carmela; Calaruso, Francesco; Giampaoli, Saverio; Barbato, Gaetano; Kandimalla, Ekambar…The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease.By Monteagudo E; Fonsi M; Chu X; Bleasby K; Evers R; Pucci V; Orsale M…Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.By Ferrara, Marco; Fiore, Fabrizio; Summa, Vincenzo; Gardelli, Cristina From Bioorganic & Medicinal Chemistry Letters…Immunological markers of cancer vaccine efficacy and their clinical relevance.Cipriani B. (2009) Biomark Med. 2009 Jun;3(3):253-64. More info on PubMed.govEnhancement of intestinal absorption of 2-methyl cytidine prodrugs.By Cianetti, Simona; Cooper, Vincent Brett; Attenni, Barbara; Pucci, Vincenzo; Fiore, Fabrizio; Giuliano, Claudio; Laufer,…Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: structure-based design and synthesis of new templates.By Malancona, Savina; Donghi, Monica; Ferrara, Marco; Martin Hernando, Jose I.; Pompei, Marco; Pesci, Silvia;…Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).By Pescatore, Giovanna; Branca, Danila; Fiore, Fabrizio; Kinzel, Olaf; Bufi, Laura Llauger; Muraglia, Ester; Orvieto,…Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.By Ferrigno, Federica; Branca, Danila; Kinzel, Olaf; Lillini, Samuele; Llauger Bufi, Laura; Monteagudo, Edith; Muraglia,…Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).By Torrisi, Caterina; Bisbocci, Monica; Ingenito, Raffaele; Ontoria, Jesus M.; Rowley, Michael; Schultz-Fademrecht, Carsten; Toniatti,…Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.By Scarpelli, Rita; Boueres, Julia K.; Cerretani, Mauro; Ferrigno, Federica; Ontoria, Jesus M.; Rowley, Michael;…Telomerase and HER-2/neu as targets of genetic cancer vaccines in dogs.By Peruzzi, Daniela; Mesiti, Giuseppe; Ciliberto, Gennaro; La Monica, Nicola; Aurisicchio, Luigi From Vaccine (2010),…Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy.By Pompei, Marco; Di Francesco, Maria Emilia; Pesci, Silvia; Koch, Uwe; Vignetti, Sue Ellen; Veneziano,…Novel potent apoA-I peptide mimetics that stimulate cholesterol efflux and pre-β particle formation in vitroBy Ingenito, Raffaele; Burton, Charlotte; Langella, Annunziata; Chen, Xun; Zytko, Karolina; Pessi, Antonello; Wang, Jun;…Turbulent flow chromatography TFC-tandem mass spectrometry supporting in vitro/vivo studies of NCEs in high throughput fashion.By Verdirame, Maria; Veneziano, Maria; Alfieri, Anna; Di Marco, Annalise; Monteagudo, Edith; Bonelli, Fabio From…
A vaccine targeting telomerase enhances survival of dogs affected by B-cell lymphoma.Peruzzi D, Gavazza A, Mesiti G, Lubas G, Scarselli E, Conforti A, Bendtsen C, Ciliberto…Identification of novel, selective, and stable inhibitors of class II histone deacetylases. 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(2009) Anal Biochem. 2009 Oct 1;393(1):126-8. More info on…Cyclic phosphoramidates as prodrugs of 2′-C-methylcytidine.Meppen M, Pacini B, Bazzo R, Koch U, Leone JF, Koeplinger KA, Rowley M, Altamura…Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.Kinzel O, Llauger-Bufi L, Pescatore G, Rowley M, Schultz-Fademrecht C, Monteagudo E, Fonsi M, Gonzalez…Smoothened antagonists: a promising new class of antitumor agents.Gallinari P, Filocamo G, Jones P, Pazzaglia S, Steinkühler C. (2009) Expert Opin Drug Discov.…A peptide vaccine based on retro-inverso beta-amyloid sequences fails to elicit a cross-reactive immune response.Bianchi E, Ingallinella P, Finotto M, Liang X, Kinney GG, Pessi A. 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(2009) Cancer…Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM,…A therapeutic cancer vaccine targeting carcinoembryonic antigen in intestinal carcinomas.Mori F, Giannetti P, Peruzzi D, Lazzaro D, Giampaoli S, Kaufman HL, Ciliberto G, La…Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.Attenni B, Ontoria JM, Cruz JC, Rowley M, Schultz-Fademrecht C, Steinkühler C, Jones P. Histone…High-throughput microsomal stability assay for screening new chemical entities in drug discovery.Fonsi M, Orsale MV, Monteagudo E. (2008) J Biomol Screen. 2008 Oct;13(9):862-9. More info on…2 Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.Muraglia E, Altamura S, Branca D, Cecchetti O, Ferrigno F, Orsale MV, Palumbi MC, Rowley…