Search Results - "PATTERSON, Adam V"
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Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects
Published in Journal of medicinal chemistry (28-03-2019)“…Hepatocellular carcinoma (HCC) is a lethal disease with limited therapeutic options and a particularly poor prognosis. Aberrant fibroblast growth factor 19…”
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TAS‐120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure
Published in ChemMedChem (19-02-2019)“…1‐[(3S)‐3‐[4‐Amino‐3‐[2‐(3,5‐dimethoxyphenyl)ethynyl]‐1H‐pyrazolo[3,4‐d]pyrimidin‐1‐yl]‐1‐pyrrolidinyl]‐2‐propen‐1‐one (TAS‐120) is an irreversible inhibitor…”
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Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes
Published in Clinical cancer research (01-03-2021)“…Approved therapies for exon 20, mutations, and fusions are currently lacking for non-small cell lung cancer and other cancers. Tarloxotinib is a prodrug that…”
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Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed
Published in Journal of structural biology (01-12-2015)“…The discovery of genetic drivers of lung cancer in patient sub-groups has led to their use as predictive biomarkers and as targets for selective drug therapy…”
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Nitroreductase gene-directed enzyme prodrug therapy: insights and advances toward clinical utility
Published in Biochemical journal (15-10-2015)“…This review examines the vast catalytic and therapeutic potential offered by type I (i.e. oxygen-insensitive) nitroreductase enzymes in partnership with…”
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Tumour Hypoxia-Mediated Immunosuppression: Mechanisms and Therapeutic Approaches to Improve Cancer Immunotherapy
Published in Cells (Basel, Switzerland) (24-04-2021)“…The magnitude of the host immune response can be regulated by either stimulatory or inhibitory immune checkpoint molecules. Receptor-ligand binding between…”
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Hypoxia-activated prodrugs and (lack of) clinical progress: The need for hypoxia-based biomarker patient selection in phase III clinical trials
Published in Clinical and translational radiation oncology (01-02-2019)“…•Hypoxia-activated prodrugs have yielded promising results up to phase II trials.•Implementation of hypoxia-activated prodrugs in the clinic has not been…”
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Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302
Published in Molecular cancer therapeutics (01-03-2012)“…TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-isophosphoramide mustard currently undergoing clinical evaluation. Here, we…”
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Structural Evaluation of a Nitroreductase Engineered for Improved Activation of the 5-Nitroimidazole PET Probe SN33623
Published in International journal of molecular sciences (15-06-2024)“…Bacterial nitroreductase enzymes capable of activating imaging probes and prodrugs are valuable tools for gene-directed enzyme prodrug therapies and targeted…”
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The Bioreductive Prodrug PR-104A Is Activated under Aerobic Conditions by Human Aldo-Keto Reductase 1C3
Published in Cancer research (Chicago, Ill.) (15-02-2010)“…PR-104, currently in phase II clinical trials, is a phosphate ester pre-prodrug which is converted in vivo to its cognate alcohol, PR-104A, a prodrug designed…”
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Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents
Published in Molecules (Basel, Switzerland) (01-06-2021)“…Phenanthroindolizidines, such as antofine and tylophorine, are a family of natural alkaloids isolated from different species of Asclepiadaceas. They are…”
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Bystander or no bystander for gene directed enzyme prodrug therapy
Published in Molecules (Basel, Switzerland) (10-11-2009)“…Gene directed enzyme prodrug therapy (GDEPT) of cancer aims to improve the selectivity of chemotherapy by gene transfer, thus enabling target cells to convert…”
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Mechanism of Action and Preclinical Antitumor Activity of the Novel Hypoxia-Activated DNA Cross-Linking Agent PR-104
Published in Clinical cancer research (01-07-2007)“…Purpose: Hypoxia is a characteristic of solid tumors and a potentially important therapeutic target. Here, we characterize the mechanism of action and…”
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Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling
Published in Frontiers in pharmacology (08-02-2022)“…Hypoxia-activated prodrugs are bioactivated in oxygen-deficient tumour regions and represent a novel strategy to exploit this pharmacological sanctuary for…”
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Subcellular Location of Tirapazamine Reduction Dramatically Affects Aerobic but Not Anoxic Cytotoxicity
Published in Molecules (Basel, Switzerland) (22-10-2020)“…Hypoxia is an adverse prognostic feature of solid cancers that may be overcome with hypoxia-activated prodrugs (HAPs). Tirapazamine (TPZ) is a HAP which has…”
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The third generation AKR1C3-activated prodrug, ACHM-025, eradicates disease in preclinical models of aggressive T-cell acute lymphoblastic leukemia
Published in Blood cancer journal (New York) (06-11-2024)“…T-cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy that expresses high levels of the enzyme aldo-keto reductase family 1…”
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Restoring Tumour Selectivity of the Bioreductive Prodrug PR-104 by Developing an Analogue Resistant to Aerobic Metabolism by Human Aldo-Keto Reductase 1C3
Published in Pharmaceuticals (Basel, Switzerland) (26-11-2021)“…PR-104 is a phosphate ester pre-prodrug that is converted in vivo to its cognate alcohol, PR-104A, a latent alkylator which forms potent cytotoxins upon…”
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Interrogation of the Structure-Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications
Published in Pharmaceuticals (Basel, Switzerland) (01-02-2022)“…PR-104A is a dual hypoxia/nitroreductase gene therapy prodrug by virtue of its ability to undergo either one- or two-electron reduction to its cytotoxic…”
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Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors
Published in Journal of medicinal chemistry (13-01-2022)“…Small molecule covalent kinase inhibitors (CKIs) have entered a new era in drug discovery, which have the advantage for sustained target inhibition and high…”
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Improved Strategy for the Synthesis of the Anticancer Agent Culicinin D
Published in European journal of organic chemistry (01-10-2015)“…The anticancer peptaibol culicinin D was synthesised via a newly developed pathway. This route included an improved attachment of a C‐terminal amino acid…”
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