RT Journal Article
SR Electronic
T1 From insight to modulation of CXCR4 and ACKR3 (CXCR7) function
JF Molecular Pharmacology
JO Mol Pharmacol
FD American Society for Pharmacology and Experimental Therapeutics
SP mol.119.118364
DO 10.1124/mol.119.118364
A1 Martine J Smit
A1 Jacqueline E van Muilwijk-Koezen
YR 2019
UL http://molpharm.aspetjournals.org/content/early/2019/10/17/mol.119.118364.abstract
AB Chemokine receptors CXCR4 and Atypical chemokine receptor 3 (ACKR3/CXCR7) are highly expressed in a range of tumours. Yet, their role in cancer progression is not well understood. This mini review series 'From insight to modulation of CXCR4 and ACKR3 function' encompasses seven comprehensive reviews focusing on modulators (small molecules, pepducins, antibodies), structural aspects, spatio-temporal signalling properties, phosphorylation/interactome of CXCR4 and ACKR3. Moreover, different (patho)physiological aspects and roles of these receptors in immunological and oncogenic processes are discussed.SIGNIFICANCE STATEMENT CXCR4 and ACKR3 are two oncogenic GPCRs that are highly upregulated in various tumours. Insight into the signalling properties of these receptors and the availability of modulators targeting these receptors are essential to assess their role in cancer.