Search Results - "Courcambeck, Jerome"
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GNS561, a clinical-stage PPT1 inhibitor, is efficient against hepatocellular carcinoma via modulation of lysosomal functions
Published in Autophagy (04-03-2022)“…Hepatocellular carcinoma is the most frequent primary liver cancer. Macroautophagy/autophagy inhibitors have been extensively studied in cancer but, to date,…”
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2
GNS561, a new lysosomotropic small molecule, for the treatment of intrahepatic cholangiocarcinoma
Published in Investigational new drugs (01-12-2019)“…Summary Among the acquired modifications in cancer cells, changes in lysosomal phenotype and functions are well described, making lysosomes a potential target…”
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3
GNS561, a New Autophagy Inhibitor Active against Cancer Stem Cells in Hepatocellular Carcinoma and Hepatic Metastasis from Colorectal Cancer
Published in Journal of Cancer (01-01-2021)“…Patients with advanced hepatocellular carcinoma (HCC) or metastatic colorectal cancer (mCRC) have a very poor prognosis due to the lack of efficient…”
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4
Anti-hepatitis C virus potency of a new autophagy inhibitor using human liver slices model
Published in World journal of hepatology (28-07-2016)“…AIM: To evaluate the antiviral potency of a new antihepatitis C virus(HCV) antiviral agent targeting the cellular autophagy machinery. METHODS: Non-infected…”
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5
Mutation rate in hepatitis C virus NS3 protease is not influenced by HIV-1 protease inhibitor therapy
Published in AIDS (London) (20-08-2008)“…Limited analysis by population sequencing has been reported for the selection of isolates with mutations within the NS3 protease that confer resistance to the…”
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6
GNS561 acts as a potent anti-fibrotic and pro-fibrolytic agent in liver fibrosis through TGF-β1 inhibition
Published in Therapeutic advances in chronic disease (2020)“…Background: Hepatic fibrosis is the result of chronic liver injury that can progress to cirrhosis and lead to liver failure. Nevertheless, there are no…”
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Mechanistic Basis for Reduced Viral and Enzymatic Fitness of HIV-1 Reverse Transcriptase Containing Both K65R and M184V Mutations
Published in The Journal of biological chemistry (02-01-2004)“…HIV-1 drug resistance mutations are often inversely correlated with viral fitness, which remains poorly described at the molecular level. Some resistance…”
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Resistance of hepatitis C virus to NS3-4A protease inhibitors : mechanisms of drug resistance induced by R155Q, A156T, D168A and D168V mutations
Published in Antiviral therapy (01-01-2006)“…One of the main issues in the development of antiviral therapy is the emergence of drug-resistant viruses. In the case of hepatitis C virus (HCV), selection of…”
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Abstract 1914: GNS561 is a new quinoline derivative with high efficacy on cancer stem cells from colorectal liver metastasis and hepatocellular carcinoma
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Background: In spite of wide application of sorafenib for advanced hepatocellular carcinoma (HCC) treatment, and systemic chemotherapy cocktails…”
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10
Preclinical characterization of GNS561 as a novel first in class autophagy inhibitor to kill hepatocellular carcinoma cancer stem cells
Published in Journal of clinical oncology (20-05-2016)“…Abstract only…”
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Abstract 5124: GNS561 a new quinoline derivative inhibits the growth of hepatocellular carcinoma in a cirrhotic rat and human PDX orthotopic mouse models
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…Background: Hepatocellular carcinoma (HCC) remains a major health problem, often diagnosed at late stages with limited number of therapeutic options. New drugs…”
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12
Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2013)“…Herein, we report the synthesis and structure–activity relationship studies of new analogs of boceprevir 1 and telaprevir 2. Introduction of azetidine and…”
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13
Synthesis and Antiviral Activity of New Anti-HIV Amprenavir Bioisosteres
Published in Journal of medicinal chemistry (18-07-2002)“…Starting from the chemical structure of the recent FDA-approved anti-HIV drug Amprenavir (Agenerase), a potent HIV-protease inhibitor, we have designed new…”
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14
Hepatitis C virus RNA load in relapsed patients: week two of treatment is the best time to predict the complete response
Published in European journal of gastroenterology & hepatology (01-10-2003)“…OBJECTIVEAn early virological response has been shown to be predictive of a sustained virological response to antiviral treatment in chronic hepatitis C…”
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15
GNS561 acts as a potent anti-fibrotic and pro-fibrolytic agent in liver fibrosis through TGF-β1 inhibition
Published in Therapeutic advances in chronic disease (16-07-2020)“…Background: Hepatic fibrosis is the result of chronic liver injury that can progress to cirrhosis and lead to liver failure. Nevertheless, there are no…”
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A Loss of Viral Replicative Capacity Correlates with Altered DNA Polymerization Kinetics by the Human Immunodeficiency Virus Reverse Transcriptase Bearing the K65R and L74V Dideoxynucleoside Resistance Substitutions
Published in The Journal of biological chemistry (11-06-2004)“…Mechanisms governing viral replicative capacity are poorly understood at the biochemical level. Human immunodeficiency virus, type 1 reverse transcriptase…”
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Synthesis and Antiviral Evaluation of Cis-Substituted Cyclohexenyl and Cyclohexanyl Nucleosides
Published in Journal of medicinal chemistry (27-01-2005)“…Starting from commercially available (rac)-3-cyclohexene-1-carboxylic acid, a series of purine and pyrimidine cis-substituted cyclohexenyl and cyclohexanyl…”
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Stereoselective synthesis of (3 S,4 S)- tert-butyl- N-Boc-3-ethyl-4-hydroxy- l-prolinate and (3 S,4 R)- tert-butyl- N-Boc-3-ethyl-4-hydroxy- l-prolinate
Published in Tetrahedron (11-04-2005)“…Diastereomers of tert-butyl- N-Boc-3-ethyl-4-hydroxy- l-prolinate 1 and 2 have been synthesized in six steps starting from readily available Boc-protected…”
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