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1.
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20 p, 15.9 MB |
Theoretical Study of the Arachidonic Acid Conversion into Leukotriene A4 Catalyzed by Human 5-Lipoxygenase : Hydroperoxidation and Epoxidation Mechanisms and Arachidonic Acid Active Site Access
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Cruz Saez, Alejandro (Universitat Autònoma de Barcelona. Departament de Química) ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
Inflammation is at the base of many different diseases. Leukotrienes (LTs) are pro-inflammatory mediators derived from arachidonic acid (AA), which play significant roles in acute inflammation. Lipoxins are specialized pro-resolving mediators (SPMs), also formed from AA, that promote the resolution of acute inflammation. [...]
2024 -  10.1021/acscatal.3c04954
ACS catalysis, Vol. 14, Issue 2 (January 2024) , p. 637-656
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2.
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25 p, 4.8 MB |
Functional Characterization of Mouse and Human Arachidonic Acid Lipoxygenase 15B (ALOX15B) Orthologs and of Their Mutants Exhibiting Humanized and Murinized Reaction Specificities
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Kakularam, Kumar R. (Charité-Universitätsmedizin Berlin. Department of Biochemistry) ;
Canyelles-Niño, Miquel (Universitat Autònoma de Barcelona. Departament de Química) ;
Chen, Xin (Charité-Universitätsmedizin Berlin. Department of Biochemistry) ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Kuhn, Hartmut (Charité-Universitätsmedizin Berlin. Department of Biochemistry)
The arachidonic acid lipoxygenase 15B (ALOX15B) orthologs of men and mice form different reaction products when arachidonic acid is used as the substrate. Tyr603Asp+His604Val double mutation in mouse arachidonic acid lipoxygenase 15b humanized the product pattern and an inverse mutagenesis strategy murinized the specificity of the human enzyme. [...]
2023 - 10.3390/ijms241210046
International journal of molecular sciences, Vol. 24, Issue 12 (June 2023) , art. 10046
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3.
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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?
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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
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4.
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29 p, 20.1 MB |
Hydroperoxidation of Docosahexaenoic Acid by Human ALOX12 and pigALOX15-mini-LOX
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Canyelles-Niño, Miquel (Universitat Autònoma de Barcelona. Departament de Química) ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
Human lipoxygenase 12 (hALOX12) catalyzes the conversion of docosahexaenoic acid (DHA) into mainly 14S-hydroperoxy-4Z,7Z,10Z,12E,16Z,19Z-docosahexaenoic acid (14S-H(p)DHA). This hydroperoxidation reaction is followed by an epoxidation and hydrolysis process that finally leads to maresin 1 (MaR1), a potent bioactive specialized pro-resolving mediator (SPM) in chronic inflammation resolution. [...]
2023 - 10.3390/ijms24076064
International journal of molecular sciences, Vol. 24, Issue 7 (April 2023) , art. 6064
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5.
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14 p, 13.3 MB |
Molecular Insights into the Regulation of 3-Phosphoinositide-Dependent Protein Kinase 1 : Modeling the Interaction between the Kinase and the Pleckstrin Homology Domains
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García Viloca, Mireia (Universitat Autònoma de Barcelona. Departament de Química) ;
Bayascas Ramírez, José Ramón (Universitat Autònoma de Barcelona. Institut de Neurociències) ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Departament de Química) ;
Universitat Autònoma de Barcelona.
Departament de Bioquímica i de Biologia Molecular
The 3-phosphoinositide-dependent protein kinase 1 (PDK1) K465E mutant kinase can still activate protein kinase B (PKB) at the membrane in a phosphatidylinositol-3,4,5-trisphosphate (PIP3, PtdIns(3,4,5)P3) independent manner. [...]
2022 - 10.1021/acsomega.2c02020
ACS omega, Vol. 7, Issue 29 (July 2022) , p. 25186-25199
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6.
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39 p, 2.7 MB |
Synthetic Photoswitchable Neurotransmitters Based on Bridged Azobenzenes
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Cabré Segura, Gisela (Universitat Autònoma de Barcelona. Departament de Química) ;
Garrido Charles, Aida (Institut de Bioenginyeria de Catalunya) ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Departament de Química) ;
Moormann, Widukind (Christian Albrechts University Kiel. Otto Diels-Institute of Organic Chemistry) ;
Langbehn, Daniel (Christian Albrechts University Kiel. Otto Diels-Institute of Organic Chemistry) ;
Egea, David (Universitat Autònoma de Barcelona. Departament de Química) ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Herges, Rainer (Christian Albrechts University Kiel. Otto Diels-Institute of Organic Chemistry) ;
Alibes, Ramón (Universitat Autònoma de Barcelona. Departament de Química) ;
Busqué Sánchez, Félix (Universitat Autònoma de Barcelona. Departament de Química) ;
Gorostiza, Pau (Institut de Bioenginyeria de Catalunya) ;
Hernando Campos, Jordi (Universitat Autònoma de Barcelona. Departament de Química)
Photoswitchable neurotransmitters of ionotropic kainate receptors were synthesized by tethering a glutamate moiety to disubstituted C2-bridged azobenzenes, which were prepared through a novel methodology that allows access to diazocines with higher yields and versatility. [...]
2019 - 10.1021/acs.orglett.9b01222
Organic Letters, Vol. 21, Issue 10 (May 2019) , p. 3780-3784
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7.
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8.
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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
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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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9.
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38 p, 2.0 MB |
The role of acetylated cyclooxygenase-2 in the biosynthesis of resolvin precursors derived from eicosapentaenoic acid
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Cebrián Prats, Anna (Universitat Autònoma de Barcelona. Departament de Química) ;
Pinto, Alexandre (Universidad de Porto. LAQV-Requimte) ;
González-Lafont, Àngels (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí") ;
Fernandes, Pedro A. (Universidad de Porto. LAQV-Requimte) ;
Lluch López, Josep Maria (Universitat Autònoma de Barcelona. Institut de Biotecnologia i de Biomedicina "Vicent Villar Palasí")
Specialized pro-resolving lipid mediators (SPMs) are natural bioactive agents actively involved in inflammation resolution. SPMs act when uncontrolled inflammatory processes are developed, for instance, in patients of COVID-19 or other diseases. [...]
2022 - 10.1039/D1OB01932E
Organic & biomolecular chemistry, Vol. 20, Issue 6 (February 2022) , p. 1260-1274
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