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ONCOgenic Receptor Network of Excellence and Training 2.0

Deliverables

Open meetings organised

Kick-off GPCR symposium [month 7]; Final meeting [m42].

Doctoral degrees

All ESRs have obtained a doctoral degree

Output

Abstracts for international conferences and publications submitted; Publications submitted to appropriate journals. Website and social media presence built, maintained and operated. Appropriate reporting and production of content delivered on time and in full

ONCORNET2.0 website

ONCORNET website updated and online wwwoncorneteu

Publications

Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies.

Author(s): Mark Soave; Mark Soave; Raimond Heukers; Barrie Kellam; Barrie Kellam; Jeanette Woolard; Jeanette Woolard; Martine J. Smit; Stephen J. Briddon; Stephen J. Briddon; Stephen J. Hill; Stephen J. Hill
Published in: VOLUME=27;ISSUE=10;STARTPAGE=1250;ENDPAGE=1261.e5;ISSN=2451-9456;TITLE=Cell Chemical Biology, Issue 15;27(10), 2020, Page(s) 1250-1261, ISSN 2451-9448
Publisher: Elsevier Inc.
DOI: 10.1016/j.chembiol.2020.06.006

Atypical opioid receptors: unconventional biology and therapeutic opportunities.

Author(s): Palmer CB, Meyrath M, Canals M, Kostenis E, Chevigné A, Szpakowska M.
Published in: Pharmacol Ther., Issue 233, 2022, Page(s) 108014, ISSN 0163-7258
Publisher: Pergamon Press
DOI: 10.1016/j.pharmthera.2021.108014

The Chemokine System in Oncogenic Pathways Driven by Viruses: Perspectives for Cancer Immunotherapy.

Author(s): Schlecht-Louf G, Deback C, Bachelerie F.
Published in: Cancers, Issue 14(3), 2022, Page(s) 848, ISSN 2072-6694
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cancers14030848

Multi-Tissue Characterization of GILZ Expression in Dendritic Cell Subsets at Steady State and in Inflammatory Contexts. 

Author(s): Docq M, Vétillard M, Gallego C, Jaracz-Ros A, Mercier-Nomé F, Bachelerie F, Schlecht-Louf G.
Published in: Cells, Issue 2021 Nov 13;10(11):3153, 2021, Page(s) 3153-, ISSN 2073-4409
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cells10113153

Differential activity and selectivity of N-terminal modified CXCL12 chemokines at the CXCR4 and ACKR3 receptors

Author(s): Jaracz-Ros A, Bernadat G, Cutolo P, Gallego C, Gustavsson M, Cecon E, Baleux F, Kufareva I, Handel TM, Bachelerie F, Levoye A.
Published in: J Leukoc Biol, Issue 107(6), 2020, Page(s) 1123-1135, ISSN 1938-3673
Publisher: Wiley Online Library
DOI: 10.1002/jlb.2ma0320-383rr

The G Protein-Coupled Receptor Kinases (GRKs) in Chemokine Receptor-Mediated Immune Cell Migration: From Molecular Cues to Physiopathology.

Author(s): Laganà M, Schlecht-Louf G, Bachelerie F.
Published in: Cells, Issue 10(1), 2021, Page(s) 75, ISSN 2073-4409
Publisher: MDPI
DOI: 10.3390/cells10010075

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

Author(s): Zarca A, Perez C, van den Bor J, Bebelman JP, Heuninck J, de Jonker RJF, Durroux T, Vischer HF, Siderius M, Smit MJ.
Published in: Cells, Issue 2021 Mar 11;10(3):618, 2021, Page(s) 618-, ISSN 2073-4409
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cells10030618

Phosphorylation-Dependent Differences in CXCR4-LASP1-AKT1 Interaction between Breast Cancer and Chronic Myeloid Leukemia

Author(s): 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.
Published in: Cells, Issue 2020 Feb 14;9(2), 2020, Page(s) 444, ISSN 2073-4409
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cells9020444

Modulation of CXCR4-Mediated Gi1 Activation by EGF Receptor and GRK2.

Author(s): Maria Neves; Cristina Perpiñá-Viciano; Petronila Penela; Petronila Penela; Carsten Hoffmann; Carsten Hoffmann; Federico Mayor; Federico Mayor
Published in: ACS Pharmacology & Translational Science, Issue 1, 2020, Page(s) 627-634, ISSN 2575-9108
Publisher: ACS Pharmacology & Translational Science
DOI: 10.1021/acsptsci.0c00021

New pairings and deorphanization among the atypical chemokine receptor family — physiological and clinical relevance

Author(s): Martyna Szpakowska, Giulia D’Uonnolo, Rafael Luı, Ana Alonso Bartolome, Marcus Thelen, Daniel F. Legler and Andy Chevigne
Published in: Front. Immunol., Issue 14, 2023, Page(s) 01-11, ISSN 1664-3224
Publisher: Frontiers
DOI: 10.3389/fimmu.2023.1133394

Optical control of Class A G protein-coupled receptors with photoswitchable ligands.

Author(s): Wijtmans M, Josimovic I, Vischer HF, Leurs R.
Published in: Curr Opin Pharmacol., Issue 63, 2022, Page(s) 102192, ISSN 1471-4892
Publisher: Elsevier BV
DOI: 10.1016/j.coph.2022.102192

GRK2-Dependent HuR Phosphorylation Regulates HIF1α Activation under Hypoxia or Adrenergic Stress.

Author(s): Reglero C, Lafarga V, Rivas V, et al.
Published in: Cancers, Issue 12(5), 2020, Page(s) 1216, ISSN 2072-6694
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/cancers12051216

The CXCL12/CXCR4/ACKR3 Axis in the Tumor Microenvironment: Signaling, Crosstalk, and Therapeutic Targeting

Author(s): Martine J. Smit, Géraldine Schlecht-Louf, Maria Neves, Jelle van den Bor, Petronila Penela, Marco Siderius, Françoise Bachelerie, Federico Mayor
Published in: Annual Review of Pharmacology and Toxicology, Issue 61/1, 2021, Page(s) 541-563, ISSN 0362-1642
Publisher: Annual Reviews, Inc.
DOI: 10.1146/annurev-pharmtox-010919-023340

G protein-coupled receptors as promising targets in cancer

Author(s): Claudia V. Perez Almeria, Irfan M. Setiawan, Marco Siderius, Martine J. Smit
Published in: Current Opinion in Endocrine and Metabolic Research, Issue 16, 2021, Page(s) 119-127, ISSN 2451-9650
Publisher: Elsevier
DOI: 10.1016/j.coemr.2020.10.005

Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells

Author(s): Comez Dehan, Glenn Jacqueline, Anbuhl Stephanie M., Heukers Raimond, Smit Martine J., Hill Stephen J., Kilpatrick Laura E.
Published in: Frontiers in Immunology, Issue 13, 2022, Page(s) e, ISSN 1664-3224
Publisher: Frontiers Research Foundation
DOI: 10.3389/fimmu.2022.1006718

A new wrinkle for skin dendritic cell migration.

Author(s): Cook DN, Nakano H.
Published in: Blood, Issue 137(20), 2021, Page(s) 2716-2717, ISSN 0006-4971
Publisher: American Society of Hematology
DOI: 10.1182/blood.2020010619

HPV infection alters vaginal microbiome through down-regulating host mucosal innate peptides used by Lactobacilli as amino acid sources

Author(s): Alizee Lebeau, Diane Bruyere, Patrick Roncarati, Paul Peixoto, Eric Hervouet, Gael Cobraiville, Bernard Taminiau, Murielle Masson, Carmen Gallego, Gabriel Mazzucchelli, Nicolas Smargiasso, Maximilien Fleron, Dominique Baiwir, Elodie Hendrick, Charlotte Pilard, Thomas Lerho, Celia Reynders, Marie Ancion, Roland Greimers, Jean-Claude Twizere, Georges Daube, Geraldine Schlecht-Louf, Françoise Bachel
Published in: Nature Communications, Issue 2022 February 28, 2022, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41467-022-28724-8

CXCR4 as a novel target in immunology: moving away from typical antagonists

Author(s): Birgit Caspar; Pietro Cocchiara; Armelle Melet; Kristof Van Emelen; Annegret Van der Aa; Graeme Milligan; Jean-Philippe Herbeuval
Published in: Future Science, Issue 2, 2022, Page(s) e, ISSN 2056-5623
Publisher: Future Science Ltd
DOI: 10.4155/fdd-2022-0007

Kinetic Analysis of the Early Signaling Steps of the Human Chemokine Receptor CXCR4

Author(s): Cristina Perpiñá-Viciano, Ali Işbilir, Aurélien Zarca, Birgit Caspar, Laura E. Kilpatrick, Stephen J. Hill, Martine J. Smit, Martin J. Lohse, Carsten Hoffmann
Published in: Molecular Pharmacology, Issue 98/2, 2020, Page(s) 72-87, ISSN 0026-895X
Publisher: American Society for Pharmacology and Experimental Therapeutics
DOI: 10.1124/mol.119.118448

Advanced fluorescence microscopy reveals disruption of dynamic CXCR4 dimerization by subpocket-specific inverse agonists.

Author(s): 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. 
Published in: Proc Natl Acad Sci U S A., Issue 2020 Nov 4:202013319, 117 (46), 2020, Page(s) 29144-29154, ISSN 1091-6490
Publisher: National Academy of Science
DOI: 10.1073/pnas.2013319117

NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET

Author(s): Jelle van den Bor, Nick D. Bergkamp, Stephanie M. Anbuhl, Françoise Dekker, Dehan Comez, Claudia V. Perez Almeria, Reggie Bosma, Carl W. White, Laura E. Kilpatrick, Stephen J. Hill, Marco Siderius, Martine J. Smit, and Raimond Heukers
Published in: Cell Rep Methods., Issue 2023 Mar 27; 3(3): 100422., 2023, ISSN 2667-2375
Publisher: Cell Press
DOI: 10.1016/j.crmeth.2023.100422

Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor

Author(s): Sebastian Dekkers, Birgit Caspar, Joëlle Goulding, Nicholas D. Kindon, Laura E. Kilpatrick, Leigh A. Stoddart, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill, and Michael J. Stocks
Published in: J. Med.Chem, Issue 66, 2023, Page(s) 5208−5222, ISSN 0022-2623
Publisher: American Chemical Society
DOI: 10.1021/acs.jmedchem.3c00151

CXCR4 signaling controls dendritic cell location and activation at steady state and in inflammation.

Author(s): 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.
Published in: Blood, Issue 137(20), 2021, Page(s) 2770-2784, ISSN 0006-4971
Publisher: American Society of Hematology
DOI: 10.1182/blood.2020006675

Structural insights into recognition of chemokine receptors by Staphylococcus aureus leukotoxins.

Author(s): 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.
Published in: Elife, Issue 2022 Mar 21;11:e72555, 2022, Page(s) e72555, ISSN 2050-084X
Publisher: eLife Sciences Publications
DOI: 10.7554/elife.72555

Conformational selection guides β-arrestin recruitment at a biased G protein-coupled receptor. 

Author(s): 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.
Published in: Science, Issue 2022 Jul 8;377(6602), 2022, Page(s) 222-228, ISSN 0036-8075
Publisher: American Association for the Advancement of Science
DOI: 10.1126/science.abj4922

Optimized protocol for 3D epithelial cultures supporting human papillomavirus replication.

Author(s): Laganà M, Margolles GC, Jaracz-Ros A, et al.
Published in: STAR Protoc., Issue 5(1), 2024, Page(s) 102828, ISSN 2666-1667
Publisher: Elsevier
DOI: 10.1016/j.xpro.2023.102828

Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3)

Author(s): Sebastian Dekkers, Dehan Comez, Noemi Karsai, Marta Arimont-Segura, Meritxell Canals, Birgit Caspar, Chris de Graaf, Laura E. Kilpatrick, Rob Leurs, Barrie Kellam, Stephen J. Hill, Stephen J. Briddon, and Michael J. Stocks
Published in: ACS Med. Chem. Lett., Issue 8 dec 2023, 2023, Page(s) online, ISSN 1948-5875
Publisher: American Chemical Society
DOI: 10.1021/acsmedchemlett.3c00469

The atypical chemokine receptor 3 interacts with Connexin 43 inhibiting astrocytic gap junctional intercellular communication.

Author(s): 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.
Published in: Nat Commun., Issue 11(1), 2020, Page(s) 4855, ISSN 2041-1723
Publisher: Nature Publishing Group
DOI: 10.1038/s41467-020-18634-y

Crosstalk between CXCR4/ACKR3 and EGFR Signaling in Breast Cancer Cells.

Author(s): Neves M, Marolda V, Mayor F Jr, Penela P.
Published in: Int J Mol Sci., Issue 2022 Oct 6;23(19):11887, 2022, Page(s) 11887-, ISSN 1422-0067
Publisher: Multidisciplinary Digital Publishing Institute (MDPI)
DOI: 10.3390/ijms231911887

Molecular characterization of the CXCR4 / CXCR7 axis in germ cell tumors and its targetability using nanobody-drug-conjugates.2023;. Published 2023 Nov 23. doi:10.1186/s40164-023-00460-9

Author(s): Wakileh GA, Bierholz P, Kotthoff M, Skowron MA, Bremmer F, Stephan A, Anbuhl SM, Heukers R, Smit MJ, Ströbel P, Nettersheim D
Published in: Exp Hematol Oncol., Issue 12(1):96, 2023, Page(s) online, ISSN 2162-3619
Publisher: Springer Nature
DOI: 10.1186/s40164-023-00460-9

The Extended N-Terminal Domain Confers Atypical Chemokine Receptor Properties to CXCR3-B.

Author(s): D'Uonnolo G, Reynders N, Meyrath M, et al.
Published in: Front Immunol., Issue 13, 2022, Page(s) 868579, ISSN 1664-3224
Publisher: EPMC
DOI: 10.3389/fimmu.2022.868579

Reduced G protein signaling despite impaired internalization and β-arrestin recruitment in patients carrying a CXCR4Leu317fsX3 mutation causing WHIM syndrome.

Author(s): Kumar R, Milanesi S, Szpakowska M, et al.
Published in: JCI Insight, Issue 8(5), 2023, Page(s) e145688, ISSN 2379-3708
Publisher: ASCI
DOI: 10.1172/jci.insight.145688

Reprogramming of connexin landscape fosters fast gap junction intercellular communication in human papillomavirus-infected epithelia

Author(s): Carmen Gallego, Agnieszka Jaracz-Ros, Marta Laganà, Françoise Mercier-Nomé, Séverine Domenichini, Amos Fumagalli, Philippe Roingeard, Michael Herfs, Guillaume Pidoux, Françoise Bachelerie, Géraldine Schlecht-Louf
Published in: Front Cell Infect Microbiol ., Issue 2023 May 16;13:1138232., 2023, ISSN 2235-2988
Publisher: Frontiers Media S. A.
DOI: 10.3389/fcimb.2023.1138232

The C-terminus of the prototypical M2 muscarinic receptor localizes to the mitochondria and regulates cell respiration under stress conditions

Author(s): Fasciani I, Petragnano F, Wang Z, Edwards R, Telugu N, Pietrantoni I, et al.
Published in: PLoS Biol, Issue 22(4), 2024, Page(s) e3002582, ISSN 1545-7885
Publisher: x
DOI: 10.1371/journal.pbio.3002582

Pharmacological characterization and radiolabeling of VUF15485, a high-affinity small-molecule agonist for the atypical chemokine receptor ACKR3

Author(s): Aurelien M. Zarca, Ilze Adlere, Cristina P. Viciano, Marta Arimont-Segura, Max Meyrath, Icaro A. Simon, Jan Paul Bebelman, Dennis Laan, Hans G. J. Custers, Elwin Janssen, Kobus L. Versteegh, Reggie Bosma, Iwan J. P. de Esch, Henry F. Vischer, Maikel Wijtmans, Martyna Szpakowska, Andy Chevigné, Carsten Hoffmann, Chris de Graaf, Barbara A. Zarzycka, Albert D. Windhorst, Martine J. Sm
Published in: Molecular Pharmacology, Issue 2024 Feb 12:MOLPHARM-AR-2023-000835, 2024, Page(s) online, ISSN 1521-0111
Publisher: ASPET
DOI: 10.1124/molpharm.123.000835

Conformational dynamics underlying Atypical Chemokine Receptor 3 activation.

Author(s): Omolade Otun, Christelle Aljamous, Elise Del Nero, Marta Arimont-Segura, Reggie Bosma, Barbara Zarzycka, Tristan Girbau, Cédric Leyrat, Chris de Graaf, Rob Leurs, Thierry Durroux, Sebastien Granier, Xiaojing Cong, Cherine Bechara.
Published in: BioRxiv, 2023, ISSN 2692-8205
Publisher: Cold Spring Harbor Laboratory
DOI: 10.1101/2023.07.17.549382

GRK specificity and Gβγ dependency determines a GPCR’s potential in biased agonism

Author(s): Edda S. F. Matthees, Jenny C. Filor, Natasha Jaiswal, Mona Reichel, Noureldine Youssef, Julia Drube, Amod Godbole, Carsten Hoffmann
Published in: BioRxiv, 2023, ISSN 2692-8205
Publisher: Cold Sprink Harbor Laboratory
DOI: 10.1101/2023.07.14.548990

Nanoluciferase-based complementation assay for systematic profiling of GPCR-GRK interactions.

Author(s): Palmer CB, D'Uonnolo G, Luís R, et al.
Published in: Methods Cell Biol, Issue 169, 2022, Page(s) 309-321, ISBN 9780128233542
Publisher: Elsevier
DOI: 10.1016/bs.mcb.2022.04.001

Nanoluciferase-based methods to monitor activation, modulation and trafficking of atypical chemokine receptors

Author(s): Luís R, D'Uonnolo G, Palmer CB, et al.
Published in: Methods Cell Biol, Issue 169, 2022, Page(s) 279-294, ISBN 9780128233535
Publisher: Elsevier
DOI: 10.1016/bs.mcb.2022.03.002

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