Search Results - "ORSINI, Paolo"
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Present Scenario and Future Landscape of Payloads for ADCs: Focus on DNA-Interacting Agents
Published in Pharmaceuticals (Basel, Switzerland) (07-10-2024)“…ADCs have emerged as a promising class of therapeutics, combining the targeting specificity of monoclonal antibodies with the cytotoxic potency of…”
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Discovery of Entrectinib: A New 3‑Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c‑ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor
Published in Journal of medicinal chemistry (14-04-2016)“…Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for the development of different tumor types. Despite the remarkable clinical…”
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Two-Photon Polymerization of Sub-micrometric Patterned Surfaces: Investigation of Cell-Substrate Interactions and Improved Differentiation of Neuron-like Cells
Published in ACS applied materials & interfaces (26-12-2013)“…Direct Laser Writing (DLW) is an innovative tool that allows the photofabrication of high resolution 3D structures, which can be successfully exploited for the…”
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An antibody-drug conjugate directed to the ALK receptor demonstrates efficacy in preclinical models of neuroblastoma
Published in Science translational medicine (13-03-2019)“…Enthusiasm for the use of antibody-drug conjugates (ADCs) in cancer therapy has risen over the past few years. The success of this therapeutic approach relies…”
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Discovery of 2‑[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro‑1H‑isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP‑1 Inhibitor for Cancer Therapy
Published in Journal of medicinal chemistry (10-09-2015)“…The nuclear protein poly(ADP-ribose) polymerase-1 (PARP-1) has a well-established role in the signaling and repair of DNA and is a prominent target in…”
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Effects of a short period of postural training on postural stability and vestibulospinal reflexes
Published in PloS one (12-06-2023)“…The effects of postural training on postural stability and vestibulospinal reflexes (VSRs) were investigated in normal subjects. A period (23 minutes) of…”
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Pupil Data Upon Stimulation by Auditory Stimuli
Published in Data (Basel) (01-03-2024)“…Evaluating hearing in newborns and uncooperative patients can pose a considerable challenge. One potential solution might be to employ the Pupil Dilation…”
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EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors
Published in Pharmaceutics (02-04-2021)“…HER-3 is becoming an attractive target for antibody-drug conjugate (ADC)-based therapy. Indeed, this receptor and its ligands are found to be overexpressed in…”
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Measuring the elastic properties of living cells through the analysis of current–displacement curves in scanning ion conductance microscopy
Published in Pflügers Archiv (01-09-2012)“…Knowledge of mechanical properties of living cells is essential to understand their physiological and pathological conditions. To measure local cellular…”
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Weak hydrostatic forces in far-scanning ion conductance microscopy used to guide neuronal growth cones
Published in Neuroscience research (01-03-2011)“…▶ The electrolyte level in SICM pipette determines the presence of hydrostatic forces. ▶ We measured these forces by means of a combined system AFM–SICM. ▶…”
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Cdc7 Kinase Inhibitors: 5-Heteroaryl-3-Carboxamido-2-Aryl Pyrroles as Potential Antitumor Agents. 1. Lead Finding
Published in Journal of medicinal chemistry (28-10-2010)“…Cdc7 serine/threonine kinase is a key regulator of DNA synthesis in eukaryotic organisms. Cdc7 inhibition through siRNA or prototype small molecules causes p53…”
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Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potential Antitumor Agents. 1. Synthesis and Structure–Activity Relationships
Published in Journal of medicinal chemistry (14-02-2008)“…Cdc7 kinase is an essential protein that promotes DNA replication in eukaryotic organisms. Genetic evidence indicates that Cdc7 inhibition can cause selective…”
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Optimization of 6,6-dimethyl pyrrolo[3,4- c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing
Published in Bioorganic & medicinal chemistry (01-03-2010)“…We describe the synthesis of compounds with interesting biochemical and cellular characteristics. Optimization of the physico-chemical properties led to the…”
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First Cdc7 Kinase Inhibitors: Pyrrolopyridinones as Potent and Orally Active Antitumor Agents. 2. Lead Discovery
Published in Journal of medicinal chemistry (22-01-2009)“…Cdc7 kinase is a key regulator of the S-phase of the cell cycle, known to promote the activation of DNA replication origins in eukaryotic organisms. Cdc7…”
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3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding
Published in Journal of medicinal chemistry (17-06-2004)“…Abnormal proliferation mediated by disruption of the normal cell cycle mechanisms is a hallmark of virtually all cancer cells. Compounds targeting complexes…”
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3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 2. Lead Optimization
Published in Journal of medicinal chemistry (21-04-2005)“…Inhibitors of cyclin-dependent kinases (CDK) such as CDK2/cyclin A−E are currently undergoing clinical trials to verify their potential as new anticancer…”
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Poly(ADP-ribose) polymerase inhibition in cancer therapy: are we close to maturity?
Published in Expert opinion on therapeutic patents (01-10-2009)“…During the last few years an increasing number of poly(ADP-ribose) polymerase (PARP) inhibitors have been appearing in the context of cancer therapy. This is…”
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Total Synthesis of Spongistatin 1: A Synthetic Strategy Exploiting Its Latent Pseudo-Symmetry
Published in Angewandte Chemie International Edition (26-08-2005)“…The challenging structure and potent growth inhibition properties against a variety of human cancer cell lines make Spongistatin 1 (1) an exciting target for…”
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Synthesis of the C-1−C-28 ABCD Unit of Spongistatin 1
Published in Organic letters (11-12-2003)“…The synthesis of the C-1−C-28 ABCD fragment of spongistatin is described. Anti-selective boron-mediated aldol coupling of a CD spiroketal ketone fragment to an…”
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Nonlinear indentation of single human erythrocytes under application of a localized mechanical force
Published in Micron (Oxford, England : 1993) (01-12-2019)“…•The local elasticity of single human erythrocytes was measured.•The Young’s modulus ranged from 0.2 to 1.5 kPa for 20 to 500 pN forces.•We observed a…”
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