Search Results - "Ciavolella, Antonella"
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A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity
Published in Nature chemical biology (01-06-2008)“…Cdc7 is an essential kinase that promotes DNA replication by activating origins of replication. Here, we characterized the potent Cdc7 inhibitor PHA-767491 ( 1…”
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Identification of 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazoline Derivatives as a New Class of Orally and Selective Polo-Like Kinase 1 Inhibitors
Published in Journal of medicinal chemistry (13-05-2010)“…Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is…”
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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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Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships
Published in Journal of medicinal chemistry (23-07-2009)“…Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective…”
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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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Antitumor Efficacy of Edotecarin as a Single Agent and in Combination with Chemotherapy Agents in a Xenograft Model
Published in Clinical cancer research (01-05-2006)“…The novel indolocarbazole edotecarin (J-107088, formerly ED-749) differs from other topoisomerase I inhibitors both pharmacokinetically 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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Abstract 509: The MPS1/TTK inhibitor, NMS-01940153, synergizes with tisotumab vedotin in colorectal cancer
Published in Cancer research (Chicago, Ill.) (22-03-2024)“…Abstract Background: MPS1 kinase plays a crucial role in maintaining genomic integrity by controlling the spindle assembly checkpoint (SAC). MPS1 is highly…”
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Abstract 1223: NMS-P293, a novel potent and selective PARP-1 inhibitor with high antitumor efficacy and tolerability
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Abstract 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 oncology…”
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Abstract 1615: NMS-812, a novel potent PERK inhibitor that also inhibits GCN2, exhibits strong anti-tumor activity as single agent and in combination in preclinical models
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract PERK and GCN2 are eIF-2α serine-threonine kinases activated by endoplasmic reticulum (ER) stress and amino acid deprivation respectively. These…”
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Cell-cycle inhibitor profiling by high-content analysis
Published in Advances in experimental medicine and biology (2007)“…The discovery of agents which disrupt cancer cell division by specifically targeting key components of the cell-cycle machinery represents a major focus of…”
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Abstract 2851: Preclinical characterization of NMS-P648, a novel and potent PARP-1/-3 inhibitor
Published in Cancer research (Chicago, Ill.) (01-08-2015)“…Abstract PARP-1 and PARP-2 are nuclear enzymes activated by DNA strand breaks and are involved in recruitment of DNA repair proteins to sites of damage. PARP-1…”
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Abstract 3259: Novel isoquinolinone derivatives with dual PARP-1/PARP-3 inhibitory activity are highly active against pTEN mutated colorectal cancer and glioblastoma models
Published in Cancer research (Chicago, Ill.) (15-04-2013)“…Abstract Inhibitors of the poly(ADP-ribose) polymerases (PARPs) family of proteins are currently in clinical trials as potential anticancer agents. PARP-1 is a…”
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Abstract 1775: Characterization of new highly selective and potent PARP-1 inhibitors
Published in Cancer research (Chicago, Ill.) (15-04-2012)“…Abstract Poly (ADP-ribose) polymerase 1 (PARP-1) is a key nuclear enzyme that is activated by DNA-strand breaks; activation of PARP-1 protects DNA breaks and…”
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9-Fluorenone-2-Carboxylic Acid as a Scaffold for Tubulin Interacting Compounds
Published in ChemPlusChem (Weinheim, Germany) (01-07-2013)“…The introduction of a hydrophobic group at position 7 of 9‐fluorenone‐2‐carboxylic acid generates new tubulin binders, the design of which is suggested by…”
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Abstract DD01-01: NMS-1116354: More than an inhibitor of Cdc 7 kinase in S-phase
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract Most of the widely used anticancer drugs target the elongation step of DNA synthesis, either directly, for example by restricting the pool of dNTPs or…”
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Abstract 691: In vitro and in vivo characterization of selective orally available Parp-1 inhibitors with demonstrated antitumor efficacy in BRCA negative cancer models
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…Abstract Poly (ADP-ribose) polymerase 1 and 2 (Parp-1 and Parp-2) are nuclear enzymes responsible for signaling the presence of DNA damages by catalyzing the…”
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