Search Results - "CUCCHI, Ulisse"
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Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death
Published in Nature chemical biology (01-09-2013)“…The VCP ATPase has been linked to cancer, but the lack of well-defined, selective inhibitors has limited further investigation. A million-molecule screen now…”
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A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action
Published in Nature communications (09-06-2017)“…The prolyl isomerase PIN1, a critical modifier of multiple signalling pathways, is overexpressed in the majority of cancers and its activity strongly…”
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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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Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase
Published in Cancer research (Chicago, Ill.) (15-12-2010)“…MPS1 kinase is a key regulator of the spindle assembly checkpoint (SAC), a mitotic mechanism specifically required for proper chromosomal alignment and…”
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Abstract 5805: A novel platform of diversified payloads to drive ADC innovation
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract First generation of antibody drug conjugates (ADCs) for anticancer therapy has been described more than two decades ago with gemtuzumab-ozogamicin…”
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NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies
Published in Molecular cancer therapeutics (01-04-2012)“…Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase considered to be the master player of cell-cycle regulation during mitosis. It is indeed…”
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Identification of unprecedented ATP-competitive choline kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2021)“…[Display omitted] In this article we describe the identification of unprecedented ATP-competitive ChoKα inhibitors starting from initial hit NMS-P830 that…”
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Thiol-peptide level and proteomic changes in response to cadmium toxicity in Oryza sativa L. roots
Published in Environmental and experimental botany (2007)“…In the present study, rice seedlings were exposed to a range of Cd concentrations (0.1 μM, 1 μM, 10 μM, 100 μM and 1 mM) for 15 days and a combination of…”
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Abstract 4790: Identification and characterization of ATP-mimetic choline kinase inhibitors
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Abstract Introduction: Choline kinase alpha (ChoKα), the first enzyme in the Kennedy pathway that catalyzes the phosphorylation of free choline to…”
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Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design
Published in Biochemistry (Easton) (17-09-2013)“…Maternal embryonic leucine zipper kinase (MELK) is upregulated in several types of tumor, including breast, prostate, and brain tumors. Its expression is…”
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Abstract 734: Thienoindoles: New highly promising agents for antibody-drug conjugates generation
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Thienoindoles are a new proprietary class of highly potent DNA minor groove alkylating agents. This class is characterized by a fused thiophene ring…”
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Abstract 2690: A novel antibody-drug conjugate directed to the ALK receptor tyrosine kinase demonstrates efficacy in models of neuroblastoma
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract Activated ALK by mutation or amplification is a validated therapeutic target in a subset of patients with high-risk neuroblastoma, and tyrosine kinase…”
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Phosphorylation of TCTP as a Marker for Polo-like Kinase-1 Activity In Vivo
Published in Anticancer research (01-12-2010)“…Polo-like kinase 1 (PLK1) is the master regulator of mitosis and a target for anticancer therapy. To develop a marker of PLK1 activity in cells and tumour…”
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Abstract A149: NMS-P945, a highly active payload for antibody drug conjugates generation
Published in Molecular cancer therapeutics (01-12-2015)“…Abstract Antibody-drug conjugates (ADCs) are increasingly employed in different oncology settings with more than forty products in clinical evaluation at…”
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Targeting Integrin αVβ3 with Theranostic RGD‐Camptothecin Conjugates Bearing a Disulfide Linker: Biological Evaluation Reveals a Complex Scenario
Published in ChemistrySelect (Weinheim) (12-06-2017)“…Theranostic RGD‐camptothecin conjugates, possessing a disulfide linker and a fluorescent naphthalimide moiety, were synthesized and biologically evaluated. The…”
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Abstract 822: Thienoindoles, a novel class of DNA minor groove alkylating agents highly suited for the generation of novel antibody drug conjugates (ADCs)
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract The rapidly growing field of Antibody-Drug Conjugates (ADCs) has recently spurred the study of novel drug payloads. In particular, much interest has…”
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Abstract 2940: Identification of potent VCP/p97/CDC48 inhibitors with distinct biochemical mechanisms including a reversible, allosteric inhibitor that activates the unfolded protein response, induce autophagy and cancer cell death
Published in Cancer research (Chicago, Ill.) (15-04-2012)“…Abstract Valosin Containing Protein (VCP), also called p97 in mammals and cdc48 in yeast, is an ubiquitously expressed and essential AAA ATPase important in…”
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