Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists

Autor: I.J.P. de Esch, Rob Leurs, Stephen J. Hill, M. Gozelle, Marta Arimont, Henry F. Vischer, Birgit Caspar, Aurélien Zarca, Ilze Adlere, Luc Roumen, Stephen J. Briddon, Maikel Wijtmans, Martine J. Smit, Shanliang Sun, C. Perpiñá Viciano, J.P. Bebelman, Carsten Hoffmann, C de Graaf

Publikováno v: European Journal of Medicinal Chemistry, 162, 631-649. Elsevier Masson SAS
Adlere, I, Sun, S, Zarca, A, Roumen, L, Gozelle, M, Viciano Perpiñá, C, Caspar, B, Arimont, M, Bebelman, J P, Briddon, S J, Hoffmann, C, Hill, S J, Smit, M J, Vischer, H F, Wijtmans, M, de Graaf, C, de Esch, I J P & Leurs, R 2019, ' Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists ', European Journal of Medicinal Chemistry, vol. 162, pp. 631-649 . https://doi.org/10.1016/j.ejmech.2018.10.060
European Journal of Medicinal Chemistry

Using the available structural information of the chemokine receptor CXCR4, we present hit finding and hit exploration studies that make use of virtual fragment screening, design, synthesis and structure activity relationship (SAR) studies. Fragment

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d98f9353f81b3d79daa353540428ab40
https://research.vu.nl/en/publications/45d9472d-608d-4e73-87f3-0d395b700372

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Growth factor–dependent phosphorylation of Gαi shapes canonical signaling by G protein–coupled receptors.

Autor: Roy, Suchismita, Sinha, Saptarshi, Silas, Ananta James, Ghassemian, Majid, Kufareva, Irina, Ghosh, Pradipta

Publikováno v: Science Signaling; 6/4/2024, Vol. 17 Issue 839, p1-20, 20p

Channelrhodopsin-2 Oligomerization in Cell Membrane Revealed by Photo-Activated Localization Microscopy.

Autor: Bestsennaia E; Institute of Biological Information Processing 1, IBI-1 (Molecular and Cellular Physiology), Forschungszentrum Jülich, 52428, Jülich, Germany., Maslov I; Dynamic Bioimaging Lab, Advanced Optical Microscopy Centre and the Biomedical Research Institute, Hasselt University, B3590, Diepenbeek, Belgium.; Laboratory for Photochemistry and Spectroscopy, Division for Molecular Imaging and Photonics, Department of Chemistry, KU Leuven, 3001, Leuven, Belgium., Balandin T; Institute of Biological Information Processing 7, IBI-7 (Structural Biochemistry), Forschungszentrum Jülich, 52428, Jülich, Germany., Alekseev A; Institute for Auditory Neuroscience and InnerEarLab, University Medical Center Göttingen, 37075, Göttingen, Germany., Yudenko A; Department of Biomedical Sciences, University Medical Center Groningen, University of Groningen, 9713 AV, Groningen, The Netherlands., Abu Shamseye A; Institute of Biological Information Processing 1, IBI-1 (Molecular and Cellular Physiology), Forschungszentrum Jülich, 52428, Jülich, Germany.; Institute of Biological Information Processing 7, IBI-7 (Structural Biochemistry), Forschungszentrum Jülich, 52428, Jülich, Germany., Zabelskii D; Institute of Biological Information Processing 7, IBI-7 (Structural Biochemistry), Forschungszentrum Jülich, 52428, Jülich, Germany.; European XFEL, 22869, Schenefeld, Germany., Baumann A; Institute of Biological Information Processing 1, IBI-1 (Molecular and Cellular Physiology), Forschungszentrum Jülich, 52428, Jülich, Germany., Catapano C; Institute of Physical and Theoretical Chemistry, Goethe-University Frankfurt, 60438, Frankfurt, Germany., Karathanasis C; Institute of Physical and Theoretical Chemistry, Goethe-University Frankfurt, 60438, Frankfurt, Germany., Gordeliy V; Institute of Biological Information Processing 7, IBI-7 (Structural Biochemistry), Forschungszentrum Jülich, 52428, Jülich, Germany., Heilemann M; Institute of Physical and Theoretical Chemistry, Goethe-University Frankfurt, 60438, Frankfurt, Germany., Gensch T; Institute of Biological Information Processing 1, IBI-1 (Molecular and Cellular Physiology), Forschungszentrum Jülich, 52428, Jülich, Germany., Borshchevskiy V; Institute of Biological Information Processing 7, IBI-7 (Structural Biochemistry), Forschungszentrum Jülich, 52428, Jülich, Germany.

Publikováno v: Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2024 Mar 11; Vol. 63 (11), pp. e202307555. Date of Electronic Publication: 2024 Feb 02.