Key publications

Smits RA, Lim HD, van der Meer T, Kuhne S, Bessembinder K, Zuiderveld OP, Wijtmans M, de Esch IJ, Leurs R.
Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.
Bioorg Med Chem Lett. 2012;22(1):461-467

Edink E, Rucktooa P, Retra K, Akdemir A, Nahar T, Zuiderveld O, van Elk R, Janssen E, van Nierop P, van Muijlwijk-Koezen J, Smit AB, Sixma TK, Leurs R, de Esch IJP.
Fragment growing induces conformational changes in acetylcholine-binding protein: A structural and thermodynamic analysis.
J. Am. Chem. Soc. 2011;133:5363-5371

de Kruijf P, Lim HD, Roumen L, Renjaän VA, Zhao J, Webb ML, Auld DS, Wijkmans JC, Zaman GJ, Smit MJ, de Graaf C, Leurs R.
Identification of a novel allosteric binding site in the CXCR2 chemokine receptor.
Mol Pharmacol.2011;80(6):1108-1118

de Graaf, C, Kooistra, AJ, Vischer HF, Katritch V, Kuijer M, Shiroishi M, Shimamura T,  Iwata S, Stevens RC, de Esch IJP, Leurs R.
Crystal structure-based virtual screening for novel fragment-like ligands of the human histamine H1 receptor.
J. Med. Chem. 2011;54:8195-8206

Slinger E, Langemeijer E, Siderius M, Vischer HF, Smit MJ.
Herpesvirus-encoded GPCRs rewire cellular signaling.
Mol Cell Endocrinol. 2011;331(2):179-184

Jähnichen S, Blanchetot C, Maussang D, Gonzalez-Pajuelo M, Chow KY, Bosch L, De Vrieze S, Serruys B, Ulrichts H, Vandevelde W, Saunders M, De Haard HJ, Schols D, Leurs R, Vanlandschoot P, Verrips T, Smit MJ.
CXCR4 nanobodies (VHH-based single variable domains) potently inhibit chemotaxis and HIV-1 replication and mobilize stem cells.
Proc Natl Acad Sci U S A. 2010;107(47):20565-20570

Slinger E, Maussang D, Schreiber A, Siderius M, Rahbar A, Fraile-Ramos A, Lira SA, Söderberg-Nauclér C, Smit MJ.
HCMV-encoded chemokine receptor US28 mediates proliferative signaling by establishing a positive feedback loop via activation of the IL-6/STAT3 axis.
Sci. Signal. 2010; 3: ra58

Bongers G, Maussang D, Muniz LR, Noriega VM, Fraile-Ramos A, Barker N, Marchesi F, Thirunarayanan N, Vischer HF, Qin L, Mayer L, Harpaz N, Leurs R, Furtado GC, Clevers H, Tortorella D, Smit MJ, Lira SA.
The cytomegalovirus-encoded chemokine receptor US28 promotes intestinal neoplasia in transgenic mice.
J Clin Invest. 2010;120(11):3969-3978

de Kloe GE, Bailey D, Leurs R, de Esch IJ.
Transforming fragments into candidates: small becomes big in medicinal chemistry.
Drug Discov. Today 2009;14:630-646