Search Results - "Finlay, Ray"
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Development of a quantification method for arginase inhibitors by LC-MS/MS with benzoyl chloride derivatization
Published in Journal of pharmaceutical and biomedical analysis (15-08-2024)“…Arginase is an enzyme responsible for converting arginine, a semi-essential amino acid, to ornithine and urea. Arginine depletion suppresses immunity via…”
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Abstract 1664: Inhibition of arginase in combination with radiation therapy shows increased immune-activation and anti-tumor activity in syngeneic tumor models
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Abstract The tumor microenvironment (TME) has multiple mechanisms of immune-suppression including recruitment of arginase (ARG) expressing myeloid cells. ARG…”
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Abstract 4523: Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+ T cells, NK cells, and CD103+ dendritic cells in mouse syngeneic tumor models
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…Abstract The tumor microenvironment (TME) has multiple mechanisms of immune-suppression, one being recruitment of arginase (ARG) expressing myeloid cells. ARG…”
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Influence of early discovery safety on eliminating off-target insulin receptor activity and selection of the candidate drug AZD9291
Published in Toxicology letters (10-09-2014)Get full text
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Abstract LB-C20: Lead generation and optimisation of a series of novel glutaminase (GLS) inhibitors
Published in Molecular cancer therapeutics (01-12-2015)“…Abstract Glutamine is an essential nutrient for cancer cells and is used to support cancer cell growth. Glutamine is converted to glutamate by the enzyme…”
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Abstract 4744: Structure-based development of covalent inhibitors of the activating and T790M gatekeeper mutant forms of the epidermal growth factor receptor (EGFR) leading to the discovery of AZD9291
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract Small molecule inhibitors of the Epidermal Growth Factor Receptor (EGFR) tyrosine kinase such as gefitinib and erlotinib have been employed…”
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Designed Epothilones: Combinatorial Synthesis, Tubulin Assembly Properties, abd Cytotoxic Action against Taxol-Resistant Tumor Cells
Published in Angewandte Chemie International Edition (17-10-1997)“…A library of epothilone A and B analogues, which was constructed by solid‐phase combinatorial synthesis using SMART Microreactors and solution chemistry, was…”
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Probing the Ring Size of Epothilones: Total Synthesis of [14]-, [15]-, [17]-, and [18]Epothilones A
Published in Angewandte Chemie International Edition (02-02-1998)“…Unfamiliar rings. The pharmocophore of epothilone A does not tolerate changes in ring size. The 14‐, 15‐, 17‐, and 18‐membered ring analogues 1 (n = 1, 2, 4,…”
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Total synthesis of 26-hydroxy-epothilone B and related analogs via a macrolactonization based strategy
Published in Tetrahedron (18-06-1998)“…The chemical synthesis of a series of 26-substituted epothilones B is described. Fully protected 26-hydroxydesoxy-epothilone B ( 7), prepared via the…”
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Chemistry, biology and medicine of selected tubulin polymerizing agents
Published in Pure and applied chemistry (30-06-1999)“…Abstract…”
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Metathesis vs metastasis: the chemistry and biology of epothilones
Published in Chemistry and industry (London) (15-12-1997)“…The chemistry and biology of epothilones are discussed, as well as the possibility of using them to treat cancer…”
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Variation der Ringgröße von Epothilonen – Totalsynthese von [14]‐, [15]‐, [17]‐ und [18]Epothilon A
Published in Angewandte Chemie (16-01-1998)“…Kaum tolerant gegenüber Änderungen der Ringgröße ist das Pharmakophor des Epothilons A: Die 14‐, 15‐, 17‐ und 18gliedrigen Ringanaloga 1 (n = 1, 2, 4 bzw. 5)…”
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Gezielt entworfene Epothilone: kombinatorische Synthese, Induktion der Tubulin‐Polymerisation und cytotoxische Wirkung gegen taxolresistente Tumorzellen
Published in Angewandte Chemie (02-10-1997)“…Eine Bibliothek von Epothilon‐A und ‐B‐Analoga, die durch kombinatorische Festphasensynthese mit SMART‐Mikroreaktoren sowie durch konventionelle Chemie in…”
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Variation der Ringgröße von Epothilonen - Totalsynthese von [14]-, [15]-, [17]- und [18]Epothilon A
Published in Angewandte Chemie (16-01-1998)Get full text
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Synthesis and biological properties of C12,13-cyclopropylepothilone A and related epothilones
Published in Chemistry & biology (01-07-1998)“…Background: The epothilones are natural substances that are potently cytotoxic, having an almost identical mode of action to Taxol TM as tubulin-polymerization…”
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