Dissemination
Publications ONCORNET2.0 / 1.0:
2024
The C-terminus of the prototypical M2 muscarinic receptor localizes to the mitochondria and regulates cell respiration under stress conditions. Fasciani I, Petragnano F, Wang Z, Edwards R, Telugu N, Pietrantoni I, et al. (2024) PLoS Biol 22(4): e3002582. 29 Apr 24 https://doi.org/10.1371/journal.pbio.3002582
Design, synthesis and pharmacological characterization of the first photoswitchable small-molecule agonist for the Atypical Chemokine Receptor. Bérenger S*, Adamska JM*, Deflorian F, de Graaf C, Palmer CB, Szpakowska M, Chevigné A, de Esch IJP, Zarzycka B, Vischer HF, Wijtmans M and Leurs R. Published in bioRxiv Chemistry, Medicine 25 March 2024 Corpus ID: 268724444 DOI:10.1101/2024.03.20.585914
Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET. Adamska JM, Leftheriotis S, Bosma R, Vischer HF, Leurs R. Int J Mol Sci. 2024 May 4;25(9):5018. doi: 10.3390/ijms25095018. PMID: 38732237
G protein-coupled receptors: a gateway to targeting oncogenic EVs? Di Niro L, Linders AC, Glynn T, Pegtel DM, Siderius M, Crudden C, Smit MJ. Extracell Vesicles Circ Nucleic Acids 2024;5:233-48. http://dx.doi.org/10.20517/evcna.2024.10
Structural basis for selectivity and antagonism in extracellular GPCR-nanobodies. Schlimgen RR, Peterson FC, Heukers R, Smit MJ, McCorvy JD, Volkman BF. Nat Commun. 2024 May 30;15(1):4611. doi: 10.1038/s41467-024-49000-x. PMID: 3881642
Design, synthesis and pharmacological characterization of the first photoswitchable small-molecule agonist for the Atypical Chemokine Receptor Bérenger S*, Adamska JM*, Deflorian F, de Graaf C, Palmer CB, Szpakowska M, Chevigné A, de Esch IJP, Zarzycka B, Vischer HF, Wijtmans M and Leurs R. To be submitted on bioRxiv.
Optimized protocol for 3D epithelial cultures supporting human papillomavirus replication. Laganà M, Margolles GC, Jaracz-Ros A, Mercier-Nomé F, Roingeard P, Lambert PF, Schlecht-Louf G, Bachelerie F. STAR Protoc. 2024 Jan 19;5(1):102828. doi: 10.1016/j.xpro.2023.102828.
2023
New pairings and deorphanization among the atypical chemokine receptor family – physiological and clinical relevance Szpakowska M, D’Uonnolo G, Luís R, Alonso Bartolomé A, Thelen M, Legler D and Chevigné A. Front Immunol. 2023, Apr 20, 14:1133394, doi: 10.3389/fimmu.2023.1133394, PMID: 37153591
2022
Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells.Comez D, Glenn J, Anbuhl SM, Heukers R, Smit MJ, Hill SJ, Kilpatrick LE. Front Immunol. 2022 Nov 23;13:1006718. doi: 10.3389/fimmu.2022.1006718. PMID: 36505413; PMCID: PMC9726709.
Crosstalk between CXCR4/ACKR3 and EGFR Signaling in Breast Cancer Cells. Neves M, Marolda V, Mayor F Jr, Penela P.Int J Mol Sci. 2022 Oct 6;23(19):11887. doi: 10.3390/ijms231911887.
Conformational selection guides β-arrestin recruitment at a biased G protein-coupled receptor. Kleist AB, Jenjak S, Sente A, Laskowski LJ, Szpakowska M, Calkins MM, Anderson EI, McNally LM, Heukers R, Bobkov V, Peterson FC, Thomas MA, Chevigné A, Smit MJ, McCorvy JD, Babu MM, Volkman BF. Science. 2022 Jul 8;377(6602):222-228. doi: 10.1126/science.abj4922. Epub 2022 Jul 7. PMID: 35857540
CXCR4 as a novel target in immunology: moving away from typical antagonists; moving away from typical antagonists. Birgit Caspar, Pietro Cocchiara, Armelle Melet, Kristof Van Emelen, Annegret Van der Aa, Graeme Milligan & Jean-Philippe Herbeuval, Future Drug DiscoveryVolume 4, Issue 201 Jun 2022, Published Online:19 Jul 2022https://doi.org/10.4155/
The Extended N-Terminal Domain Confers Atypical Chemokine Receptor Properties to CXCR3-B D’Uonnolo G, Reynders N, Meyrath M, Abboud D, Uchański T, Laeremans T, Volkman BF, Janji B, Hanson J, Szpakowska M, Chevigné A.. Front Immunol. 2022, Jun 1, 13:868579, doi: 10.3389/fimmu.2022.868579, PMID: 35720349
Nanoluciferase-based complementation assay for systematic profiling of GPCR–GRK interactions Palmer C, D’Unnolo G, Luis R, Meyrath M, Uchański T, Szpakowska M and Chevigné A Methods in Cell Biol. 2022, May 4, 169:309., doi: 10.1016/bs.mcb.2022.04.001, PMID: 35623709
Atypical opioid receptors: unconventional biology and therapeutic opportunities Palmer CB, Meyrath M, Canals M, Kostenis E, Chevigné A, Szpakowska M.; Pharmacol Ther. 2022 May;233:108014doi: 10.1016/j.pharmthera.2021, PMID: 34624426
Nanoluciferase-based methods to monitor activation, modulation and trafficking of Atypical Chemokine Receptors Luis R, D’Uonnolo G, Palmer C, Meyrath M, Uchański T, Wantz M, Rogister B, Janji B, Chevigné A and Szpakowska M Methods in Cell Biol 2022, Apr 18, 169:279, doi: 10.1016/bs.mcb.2022.03.002, PMID: 35623707
Optical control of Class A G protein-coupled receptors with photoswitchable ligands. Wijtmans M, Josimovic I, Vischer HF, Leurs R. Curr Opin Pharmacol. 2022 Apr;63:102192. doi: 10.1016/j.coph.2022.102192. Epub 2022 Mar 4. PMID: 35255451
Structural insights into recognition of chemokine receptors by Staphylococcus aureus leukotoxins. Lambey P., Otun O., Cong X., Hoh F., Brunel L., Verdie P., Grison CM., Peysson F., Jeannot S., Durroux T., Bechara C., Granier S. and Leyrat C. (2022), Elife. 2022 Mar 21;11:e72555. doi: 10.7554/eLife.72555. PMID: 35311641; PMCID: PMC9005193.
The Chemokine System in Oncogenic Pathways Driven by Viruses: Perspectives for Cancer Immunotherapy. Schlecht-Louf G, Deback C, Bachelerie F.Cancers (Basel). 2022 Feb 8;14(3):848. doi: 10.3390/cancers14030848.
2021
Multi-Tissue Characterization of GILZ Expression in Dendritic Cell Subsets at Steady State and in Inflammatory Contexts. Docq M, Vétillard M, Gallego C, Jaracz-Ros A, Mercier-Nomé F, Bachelerie F, Schlecht-Louf G.Cells. 2021 Nov 13;10(11):3153. doi: 10.3390/cells10113153.
The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides. Meyrath M, Szpakowska M, Zeiner J, Massotte L, Merz MP, Benkel T, Simon K, Ohnmacht J, Turner JD, Krüger R, Seutin V, Ollert M, Kostenis E, Chevigné A.Nat Commun. 2020 Jun 19;11(1):3033. doi: 10.1038/s41467-020-16664-0.PMI
The natural analgesic conolidine targets the newly identified opioid scavenger ACKR3/CXCR7 Szpakowska M, Decker AM, Meyrath M, Palmer CB, Blough BE, Namjoshi OA, Chevigné A. Signal Transduct Target Ther. 2021 Jun 2;6(1):209. doi: 10.1038/s41392-021-00548-w. PM
CXCR4 signaling controls dendritic cell location and activation at steady state and in inflammation. Gallego C, Vétillard M, Calmette J, Roriz M, Marin-Esteban V, Evrard M, Aknin ML, Pionnier N, Lefrançois M, Mercier-Nomé F, Bertrand Y, Suarez F, Donadieu J, Ng LG, Balabanian K, Bachelerie F, Schlecht-Louf G. Blood. 2021 May 20;137(20):2770-2784. doi: 10.1182/blood.2020006675. PMID: 33512478.
Proadrenomedullin N-Terminal 20 Peptides (PAMPs) Are Agonists of the Chemokine Scavenger Receptor ACKR3/CXCR7 Meyrath M, Palmer CB, Reynders N, Vanderplasschen A, Ollert M, Bouvier M, Szpakowska M, Chevigné A. ACS Pharmacol Transl Sci. 2021 Mar 22;4(2):813-823. doi: 10.1021/acsptsci.1c00006. eCollection 2021 Apr 9. PMID: 33860204
Differential Involvement of ACKR3 C-Tail in β-Arrestin Recruitment, Trafficking and Internalization. Zarca A, Perez C, van den Bor J, Bebelman JP, Heuninck J, de Jonker RJF, Durroux T, Vischer HF, Siderius M, Smit MJ. Cells. 2021 Mar 11;10(3):618. doi: 10.3390/cells10030618.
CXCL10 Is an Agonist of the CC Family Chemokine Scavenger Receptor ACKR2/D6 Chevigné A, Janji B, Meyrath M, Reynders N, D’Uonnolo G, Uchański T, Xiao M, Berchem G, Ollert M, Kwon YJ, Noman MZ, Szpakowska M. Cancers (Basel). 2021 Mar 2;13(5):1054. doi:10.3390/cancers13051054. P
The CXCL12/CXCR4/ACKR3 Axis in the Tumor Microenvironment: Signaling, Crosstalk, and Therapeutic Targeting Smit MJ, Schlecht-Louf G, Neves M, van den Bor J, Penela P, Siderius M, Bachelerie F, Mayor F Jr. Annu Rev Pharmacol Toxicol. 2021 Jan 6;61:541-563. doi: 10.1146/annurev-pharmtox-
The G Protein-Coupled Receptor Kinases (GRKs) in Chemokine Receptor-Mediated Immune Cell Migration: From Molecular Cues to Physiopathology. Laganà M, Schlecht-Louf G, Bachelerie F. Cells. 2021 Jan 5;10(1):75. doi: 10.3390/cells10010075. PMID: 33466410; PMCID: PMC7824814.
2020
G protein-coupled receptors as promising targets in cancer. Perez Almeria CV, Setiawan IM, Siderius M, Smit MJ. Current Opinion in Endocrine and Metabolic Research, 2020, 16. doi: 10.1016/j.coemr.2020.10.005
The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides. Meyrath M, Szpakowska M, Zeiner J, Massotte L, Merz MP, Benkel T, Simon K, Ohnmacht J, Turner JD, Krüger R, Seutin V, Ollert M, Kostenis E, Chevigné A.Nat Commun. 2020 Jun 19;11(1):3033. doi: 10.1038/s41467-020-16664-0.
Differential activity and selectivity of N-terminal modified CXCL12 chemokines at the CXCR4 and ACKR3 receptors. Jaracz-Ros A, Bernadat G, Cutolo P, Gallego C, Gustavsson M, Cecon E, Baleux F, Kufareva I, Handel TM, Bachelerie F, Levoye A.J Leukoc Biol. 2020 Jun;107(6):1123-1135. doi: 10.1002/JLB.2MA0320-383RR. Epub 2020 May 6.PMID: 32374043
Modulation of CXCR4-Mediated Gi1 Activation by EGF Receptor and GRK2 Neves M, Perpiñá-Viciano C, Penela P, Hoffmann C, Mayor F Jr. ACS Pharmacol Transl Sci. 2020 Apr 27;3(4):627-634. doi: 10.1021/acsptsci.0c00021. eCollection 2020 Aug 14. PMID: 33073183
Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists Işbilir A, Möller J, Arimont M, Bobkov V, Perpiñá-Viciano C, Hoffmann C, Inoue A, Heukers R, de Graaf C, Smit MJ, Annibale P, Lohse MJ. Proc Natl Acad Sci U S A. 2020 Nov 4:202013319. doi: 10.1073/pnas.2013319117. [Epub ahead of print] PMID: 33148803
The atypical chemokine receptor 3 interacts with Connexion 43 inhibiting astrocytic gap junctional intercellular communication Fumagalli A, Heuninck J, Pizzoccaro A, Moutin E, Koenen J, Séveno M, Durroux T, Junier MP, Schlecht-Louf G, Bachelerie F, Schütz D, Stumm R, Smit MJ, Guérineau NC, Chaumont-Dubel S, Marin P.
Nat Commun. 2020 Sep 25;11(1):4855. doi: 10.1016/j.chembiol.2020.06.006 PMID: 32978390
Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4 Perpiñá-Viciano C, Işbilir A, Zarca A, Caspar B, Kilpatrick LE, Hill SJ, Smit MJ, Lohse MJ, Hoffmann C Mol Pharmacol. 2020 Aug;98(2):72-87. doi: 10.1124/mol.119.118448. Epub 2020 May 30. PMID: 32474443
Monitoring Allosteric Interactions with CXCR4 Using NanoBit Conjugated Nanobodies Soave M, Heukers R, Kellam B, Woolard J, Smit MJ, Briddon SJ, Hill SJ. Cell Chem Biol. 2020 Jun 29:S2451-9456(20)30229-4. doi: 10.1016/j.chembiol.2020.06.006 [Epub ahead of print] PMID: 32610042
Phosphorylation-Dependent Differences in CXCR4-LASP1-AKT1 Interaction between Breast Cancer and Chronic Myeloid Leukemia Butt E, Stempfle K, Lister L, Wolf F, Kraft M, Herrmann AB, Viciano CP, Weber C, Hochhaus A, Ernst T, Hoffmann C, Zernecke A, Frietsch JJ. Cells. 2020 Feb 14;9(2):444. doi: 10.3390/cells9020444 PMID: 32075106
2019
From insight to modulation of CXCR4 and ACKR3 (CXCR7) function
Smit MJ, van Muilwijk-Koezen JE. Mol Pharmacol. 2019 Oct 17. pii: mol.119.118364. doi: 10.1124/mol.119.118364 [Epub ahead of print] PMID: 31624136
Modulators of CXCR4 and CXCR7/ACKR3 function
Adlere I, Caspar B, Arimont M, Dekkers S, Visser K, Stuijt J, de Graaf C, Stocks M, Kellam B, Briddon S, Wijtmans M, de Esch I, Hill S, Leurs R. Mol Pharmacol. 2019 Sep 23. pii: mol.119.117663. doi: 10.1124/mol.119.117663 [Epub ahead of print] PMID: 31548340
Antibodies targeting chemokine receptors CXCR4 and ACKR3
Bobkov V, Arimont M, Zarca A, De Groof T, van der Woning B, de Haard H, Smit MJ. Mol Pharmacol. 2019 Sep 3. pii: mol.119.116954. doi: 10.1124/mol.119.116954 [Epub ahead of print] PMID: 31481460
Chemokine receptor crystal structures: what can be learnt from them?
Arimont M, Hoffmann C, de Graaf C, Leurs R. Mol Pharmacol. 2019 Jul 2. pii: mol.119.117168. doi: 10.1124/mol.119.117168 [Epub ahead of print] PMID: 31266800
Context-dependent signalling of CXC chemokine receptor 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3)
Heuninck J, Perpina Viciano C, Işbilir A, Caspar B, Capoferri D, Briddon SJ, Durroux T, Hill SJ, Lohse MJ, Milligan G, Pin JP, Hoffmann C. Mol Pharmacol. 2019 May 15. pii: mol.118.115477. doi:10.1124/mol.118.115477 [Epub ahead of print] PMID: 31092552
Atypical chemokine receptor 3 (ACKR3): a comprehensive overview of its expression and potential roles in the immune system
Koenen J, Bachelerie F, Balabanian K, Schlecht-Louf G, Gallego C. Mol Pharmacol. 2019 April 30, mol.118.115329; DOI: https://doi.org/10.1124/mol.118.115329
Time-Resolved FRET-Based Assays to Characterize G Protein-Coupled Receptor Hetero-oligomer Pharmacology
Heuninck J, Hounsou C, Dupuis E, Trinquet E, Mouillac B, Pin JP, Bonnet D, Durroux T.
Methods Mol Biol. 2019;1947:151-168. doi:10.1007/978-1-4939-9121-1_8 PMID:30969415
Nanobodies: New avenues for imaging, stabilizing and modulating GPCRs
De Groof TWM, Bobkov V, Heukers R, Smit MJ.
Mol Cell Endocrinol. 2019 March 15;484: 15-24. DOI: 10.1016/j.mce.2019.01.021 Epub 2019 Jan 26
CXCR4/ACKR3 phosphorylation and recruitment of interacting proteins: key mechanisms regulating their functional status
Fumagalli A, Zarca A, Neves M, Casper B, Hill S, Mayor F Jr., Smit MJ, Marin P. Mol Pharmacol. 2019 March 5 [Epub ahead of print], mol.118.115360, DOI: https://doi.org/10.1124/mol.118.115360
The role of ACKR3 in breast, lung and brain cancer
Neves M, Fumagalli A, van den Bor J, Marin P, Smit MJ, Mayor F Jr.
Mol Pharmacol. 2019 Feb 11 (Epub ahead of print). DOI: 10.1124/mol.118.115279
Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists
Adlere I, Sun S, Zarca A, Roumen L, Gozelle M, Viciano CP, Caspar B, Arimont M, Bebelman JP, Briddon SJ, Hoffmann
C, Hill SJ, Smit MJ, Vischer HF, Wijtmans M, de Graaf C, de Esch IJP, Leurs R.
Eur J Med Chem. 2019 Jan 15;162:631-649. DOI: 10.1016/j.ejmech.2018.10.060 Epub 2018 Oct 30
2018
CXCR4-targeting nanobodies differentially inhibit CXCR4 function and HIV entry
Van Hout A, Klarenbeek A, Bobkov V, Doijen J, Arimont M, Zhao C, Heukers R, Rimkunas R, de Graaf C, Verrips T, van
der Woning B, de Haard H, Rucker JB, Vermeire K, Handel T, Van Loy T, Smit MJ, Schols D.
Biochem Pharmacol. 2018 Dec;158:402-412. DOI: 10.1016/j.bcp.2018.10.015 Epub 2018 Oct 17
Nanobody-Fc constructs targeting chemokine receptor CXCR4 potently inhibit signaling and CXCR4-
mediated HIV-entry and induce antibody effector functions
Bobkov V, Zarca AM, Van Hout A, Arimont M, Doijen J, Bialkowska M, Toffoli E, Klarenbeek A, van der Woning B, van
der Vliet HJ, Van Loy T, de Haard H, Schols D, Heukers R, Smit MJ.
Biochem Pharmacol. 2018 Dec;158:413-424. DOI: 10.1016/j.bcp.2018.10.014 Epub 2018 Oct 17
2017
G-Protein-Coupled Receptor Kinase 2 as a Potential Modulator of the Hallmarks of Cancer
Nogués L, Reglero C, Rivas V, Neves M, Penela P, Mayor F Jr.
Mol Pharmacol. 2017 Mar;91(3):220-228. doi: 10.1124/mol.116.107185 Epub 2016 Nov 28
Peripheral Interaction of Resolvin D1 and E1 with Opioid Receptor Antagonists for Antinociception in
Inflammatory Pain in Rats
Oehler B, Mohammadi M, Perpiñá Viciano C, Hackel D, Hoffmann C, Brack A, Rittner HL.
Front Mol Neurosci. 2017 Aug 3;10:242. DOI: 10.3389/fnmol.2017.00242 eCollection 2017
CXCR4-Specific Nanobodies as Potential Therapeutics for WHIM syndrome
de Wit RH, Heukers R, Brink HJ, Arsova A, Maussang D, Cutolo P, Strubbe B, Vischer HF, Bachelerie F, Smit MJ.
J Pharmacol Exp Ther. 2017 Oct;363(1):35-44. DOI: 10.1124/jpet.117.242735 Epub 2017 Aug 2
Fluorescent-Based Strategies to Investigate G Protein-Coupled Receptors: Evolution of the Techniques to a Better Understanding
Faklaris O, Heuninck J, Falco A, Goyet E, Zwier JM, Pin JP, Mouillac B, Perroy J, Durroux T.
Topics in Medicinal Chemistry, chapter May 2017 DOI: 10.1007/7355_2017_2
G protein-coupled receptor kinases (GRKs) in tumorigenesis and cancer progression: GPCR regulators and signaling hubs
Nogués L, Palacios-García J, Reglero C, Rivas V, Neves M, Ribas C, Penela P, Mayor F Jr. Semin Cancer Biol 2018
Feb;48:78-90. DOI: 10.1016/j.semcancer.2017.04.013 Epub 2017 May 1
Structural Analysis of Chemokine Receptor-Ligand Interactions
Arimont M, Sun SL, Leurs R, Smit M, de Esch IJP, de Graaf C. J Med Chem. 2017 Jun 22;60(12):4735-4779. doi: 10.1021/acs.jmedchem.6b01309 Epub 2017 Mar 10
2016
G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a novel HDAC6-Pin1
axis
Nogués L, Reglero C, Rivas V, Salcedo A, Lafarga V2, Neves M, Ramos P, Mendiola M, Berjón A, Stamatakis K, Zhou XZ, Lu KP, Hardisson D, Mayor F Jr, Penela P.
EBioMedicine. 2016 Nov;13:132-145. DOI: 10.1016/j.ebiom.2016.09.030 Epub 2016 Oct 1
DNA immunization combined with scFv phage display identifies antagonistic GCGR specific antibodies and reveals new epitopes on the small extracellular loops
van der Woning B, De Boeck G, Blanchetot C, Bobkov V, Klarenbeek A, Saunders M, Waelbroeck M, Laeremans T,
Steyaert J, Hultberg A, De Haard H. MAbs. 2016 Aug-Sep;8(6):1126-35. doi: 10.1080/19420862.2016.1189050 Epub 2016 May 21
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e.v.langemeijer@vu.nl
ONCORNET Coordinator
Vrije Universiteit Amsterdam