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Structural commonality of C1q TNF‐related proteins and their potential to activate relaxin/insulin‐like family peptide receptor 1 signalling pathways in cancer cells
Author(s) -
Klonisch Thomas,
Glogowska Aleksandra,
Thanasupawat Thatchawan,
Burg Maxwell,
Krcek Jerry,
Pitz Marshall,
Jaggupilli Appalaraju,
Chelikani Prashen,
Wong G William,
HombachKlonisch Sabine
Publication year - 2017
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.13559
Subject(s) - relaxin , receptor , g protein coupled receptor , biology , microbiology and biotechnology , signal transduction , gene isoform , cancer research , biochemistry , gene
We established the role of the GPCR relaxin/insulin-like family peptide receptor 1 (RXFP1 receptor) as a novel active receptor in human glioblastoma (GB), a fatal brain tumour. We identified C1q/TNF-related protein 8 (CTRP8) as a novel agonist of the RXFP1 receptor. CTRP8 enhanced the motility and matrix invasion of GB, and this involved PKC-mediated up-regulation of cathepsin B, a marker for poor prognosis in GB patients. We conclude that the absence of relaxin isoforms does not preclude the activation of the RXFP1 receptor, as the least known member of the CTRP family, CTRP8, can effectively target and activate RXFP1 receptors.