Cookies make it easier for us to provide you with our services. With the usage of our services you permit us to use cookies.


  ONCOgenic GPCR Network of Excellence and Training


Publications ONCORNET:

The CXCL12/CXCR4/ACKR3 Axis in the Tumor Microenvironment: Signaling, Crosstalk, and Therapeutic Targeting
Smit MJ, Schlecht-Louf G, Neves M, den Bor JV, Penela P, Siderius M, Bachelerie F, Mayor F Jr.
Annu Rev Pharmacol Toxicol. 2020 Sep 21. doi: 10.1146/annurev-pharmtox-010919-023340 [Epub ahead of print]
PMID: 32956018


The atypical chemokine receptor 2 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

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


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


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


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:


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


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:


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


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


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


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


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


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


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


G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a novel HDAC6-Pin1
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

Contact details

Please contact us at:

ONCORNET Coordinator
VU University Amsterdam
The Netherlands

Funded by

marie curie actions   Marie Curie Actions



EU Horizon 2020



european union logo   European Union