Výsledky vyhledávání - "J.P. Bebelman"

Differential Involvement of ACKR3 C-Tail in β-Arrestin Recruitment, Trafficking and Internalization

Autor: Henry F. Vischer, Thierry Durroux, Rianna J F de Jonker, Martine J. Smit, J.P. Bebelman, Claudia Perez, Marco Siderius, Jelle van den Bor, Aurélien Zarca, Joyce Heuninck

Publikováno v: Cells
Cells, MDPI, 2021, 10 (3), pp.618. ⟨10.3390/cells10030618⟩
Cells, 2021, 10 (3), pp.618. ⟨10.3390/cells10030618⟩
Volume 10
Issue 3
Cells, Vol 10, Iss 618, p 618 (2021)
Cells, 10(3):618, 1-16. MDPI Multidisciplinary Digital Publishing Institute
Zarca, A, Perez, C, van den Bor, J, Bebelman, J P, Heuninck, J, de Jonker, R J F, Durroux, T, Vischer, H F, Siderius, M & Smit, M J 2021, ' Differential Involvement of ACKR3 C-Tail in β-Arrestin Recruitment, Trafficking and Internalization ', Cells, vol. 10, no. 3, 618, pp. 1-16 . https://doi.org/10.3390/cells10030618

Background: The atypical chemokine receptor 3 (ACKR3) belongs to the superfamily of G protein-coupled receptors (GPCRs). Unlike classical GPCRs, this receptor does not activate G proteins in most cell types but recruits β-arrestins upon activation.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6e425778b306e89aba4a082271aeb05
https://hal.archives-ouvertes.fr/hal-03193065/file/cells-10-00618-v2.pdf

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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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Photoswitching the Efficacy of a Small-Molecule Ligand for a Peptidergic GPCR: from Antagonism to Agonism

Autor: Rob Leurs, Daniel Da Costa Pereira, J.P. Bebelman, Prashanna Vijayachandran, Henry F. Vischer, Xavier Gómez-Santacana, Maikel Wijtmans, Sabrina M. de Munnik, Iwan J. P. de Esch

Publikováno v: Angewandte Chemie. International Edition, 57(36), 11608-11612. Wiley
Gómez-Santacana, X, de Munnik, S M, Vijayachandran, P, Da Costa Pereira, D, Bebelman, J P M, de Esch, I J P, Vischer, H F, Wijtmans, M & Leurs, R 2018, ' Photoswitching the Efficacy of a Small-Molecule Ligand for a Peptidergic GPCR : from Antagonism to Agonism ', Angewandte Chemie. International Edition, vol. 57, no. 36, pp. 11608-11612 . https://doi.org/10.1002/anie.201804875

For optical control of GPCR function, we set out to develop small-molecule ligands with photoswitchable efficacy in which both configurations bind the target protein but exert distinct pharmacological effects, that is, stimulate or antagonize GPCR ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::221cc8d5ce1032f8d8ce4521f2383ad0
https://research.vu.nl/en/publications/7dd8b7c3-e183-4792-943b-5f041161bd72

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Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases

Autor: Anitha Shanmugham, J.P. Bebelman, Rob Leurs, Tiffany van der Meer, Marco Siderius, A.R. Blaazer, Paul England, Iwan J. P. de Esch

Publikováno v: Analytical Biochemistry, 503, 41-49. Academic Press Inc.
Siderius, M H, Shanmugham, A, England, P, van der Meer, T K, Bebelman, J P, Blaazer, A R, de Esch, I J P & Leurs, R 2016, ' Surface plasmon resonance biosensor assay for the analysis of small-molecule inhibitor binding to human and parasitic phosphodiesterases. ', Analytical Biochemistry, vol. 503, pp. 41-49 . https://doi.org/10.1016/j.ab.2016.03.013

In the past decade, surface plasmon resonance (SPR) biosensor-based technology has been exploited more and more to characterize the interaction between drug targets and small-molecule modulators. Here, we report the successful application of SPR meth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5084cc91abf990a5a3ed5366359279f
https://research.vu.nl/en/publications/8e150f46-2a3e-40d1-a217-866eb207f384

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Quantitative expression profiling of G-protein-coupled receptors (GPCRs) in metastatic melanoma: the constitutively active orphan GPCR GPR18 as novel drug target

Autor: J.P. Bebelman, Cornelis P. Tensen, Marco Siderius, Yongjun Qin, Martine J. Smit, Susanne Osanto, Els M. E. Verdegaal, Rein Willemze, Rob Leurs

Publikováno v: Pigment Cell & Melanoma Research. 24:207-218

G-protein-coupled receptors (GPCRs) have been implicated in the tumorigenesis and metastasis of human cancers and are considered amongst the most desirable targets for drug development. Utilizing a robust quantitative PCR array, we quantified express

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9b042ad0fed6dc24780d357ba5b5ff4c
https://doi.org/10.1111/j.1755-148x.2010.00781.x

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Cdc37p is involved in osmoadaptation and controls high osmolarity-induced cross-talk via the MAP kinase Kss1p

Autor: Marco Siderius, Annemarie Meenhuis, Xiao-Xian Yang, J.P. Bebelman, Patricija Hawle, Saskia M. van der Vies

Publikováno v: FEMS Yeast Research. 7:796-807

Cdc37p, the p50 homolog of Saccharomyces cerevisiae, is an Hsp90 cochaperone involved in the targeting of protein kinases to Hsp90. Here we report a role for Cdc37p in osmoadaptive signalling in this yeast. The osmosensitive phenotype that is display

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f7a021115cc048e06dab58b601407d1
https://doi.org/10.1111/j.1567-1364.2007.00237.x

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Cdc37p Is Required for Stress-Induced High-Osmolarity Glycerol and Protein Kinase C Mitogen-Activated Protein Kinase Pathway Functionality by Interaction with Hog1p and Slt2p (Mpk1p)

Autor: Xiao Xian Yang, J.P. Bebelman, Patricija Hawle, Danielle Horst, Marco Siderius, Saskia M. van der Vies

Publikováno v: Eukaryotic Cell. 6:521-532

The yeast Saccharomyces cerevisiae utilizes rapidly responding mitogen-activated protein kinase (MAPK) signaling cascades to adapt efficiently to a changing environment. Here we report that phosphorylation of Cdc37p, an Hsp90 cochaperone, by casein k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbfdbbb4f61193ee832980f87487c0c9
https://doi.org/10.1128/ec.00343-06

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The CXCR3-CXCL11 signaling axis mediates macrophage recruitment and dissemination of mycobacterial infection

Autor: Martine J. Smit, Astrid M. van der Sar, Herman P. Spaink, J.P. Bebelman, Annemarie H. Meijer, Ralf Boland, Chao Cui, Vincenzo Torraca, Marco Siderius

Publikováno v: Torraca, V, Cui, C, Boland, R, Bebelman, J P, van der Sar, A M, Smit, M J, Siderius, M, Spaink, H P & Meijer, A H 2015, ' The CXCR3-CXCL11 signaling axis mediates macrophage recruitment and dissemination of mycobacterial infection ', Disease Models and Mechanisms, vol. 8, no. 3, pp. 253-269 . https://doi.org/10.1242/dmm.017756
Disease Models and Mechanisms, 8(3), 253-269. Company of Biologists Ltd
Disease Models & Mechanisms, Vol 8, Iss 3, Pp 253-269 (2015)
Disease Models & Mechanisms
Torraca, V, Cui, C, Boland, R, Bebelman, J P, van der Sar, A M, Smit, M J, Siderius, M H, Spaink, H P & Meijer, A H 2016, ' The CXCR3-CXCL11 signaling axis mediates macrophage recruitment and dissemination of mycobacterial infection. ', Disease Models and Mechanisms, vol. 8, no. 3, pp. 253-269 . https://doi.org/10.1242/dmm.017756

The recruitment of leukocytes to infectious foci depends strongly on the local release of chemoattractant mediators. The human CXC chemokine receptor 3 (CXCR3) is an important node in the chemokine signaling network and is expressed by multiple leuko

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fb510e753c4f07ffa3eb6da2dc3eb15
https://hdl.handle.net/1887/3196745

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