Resultats globals: 2 registres trobats en 0.02 segons.
Articles, 2 registres trobats
Articles 2 registres trobats  
1.
21 p, 4.8 MB Different Structures-Similar Effect : Do Substituted 5-(4-Methoxyphenyl)-1 H -indoles and 5-(4-Methoxyphenyl)-1 H -imidazoles Represent a Common Pharmacophore for Substrate Selective Inhibition of Linoleate Oxygenase Activity of ALOX15? / Zhuravlev, Alexander (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Cruz Saez, Alejandro (Universitat Autònoma de Barcelona. Departament de Química) ; Aksenov, Vladislav (Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry) ; Golovanov, Alexey (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ; Kuhn, Hartmut (Charite-University Medicine Berlin. Department of Biochemistry) ; González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ; Ivanov, Igor (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies)
Mammalian 15-lipoxygenases (ALOX15) are lipid peroxidizing enzymes that exhibit variable functionality in different cancer and inflammation models. The pathophysiological role of linoleic acid- and arachidonic acid-derived ALOX15 metabolites rendered this enzyme a target for pharmacological research. [...]
2023 - 10.3390/molecules28145418
Molecules, Vol. 28, Issue 14 (July 2023) , art. 5418  
2.
29 p, 3.4 MB N-Substituted 5-(1H-Indol-2-yl)-2-methoxyanilines Are Allosteric Inhibitors of the Linoleate Oxygenase Activity of Selected Mammalian ALOX15 Orthologs : Mechanism of Action / Golovanov, Alexey (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Zhuravlev, Alexander (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Cruz, Alejandro (Universitat Autònoma de Barcelona. Departament de Química) ; Aksenov, Vladislav (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Shafiullina, Rania (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies) ; Kakularam, Kumar R. (University Medicine Berlin. Department of Biochemistry, Charité) ; Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ; Kuhn, Hartmut (University Medicine Berlin. Department of Biochemistry, Charité) ; González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ; Ivanov, Igor (Russian Technological University. Lomonosov Institute of Fine Chemical Technologies)
Here, we describe the first systematic study on the mechanism of substrate-selective inhibition of mammalian ALOX15 orthologs. For this purpose, we prepared a series of N-substituted 5-(1H-indol-2-yl)anilines and found that (N-(5-(1H-indol-2-yl)-2-methoxyphenyl)sulfamoyl)carbamates and their monofluorinated analogues are potent and selective inhibitors of the linoleate oxygenase activity of rabbit and human ALOX15. [...]
2022 - 10.1021/acs.jmedchem.1c01563
Journal of Medicinal Chemistry, Vol. 65, Issue 3 (February 2022) , p. 1979-1995  

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