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Dis Model Mech 2015 Oct 01;810:1237-46. doi: 10.1242/dmm.021071.
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A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models.

Lappano R , Rosano C , Pisano A , Santolla MF , De Francesco EM , De Marco P , Dolce V , Ponassi M , Felli L , Cafeo G , Kohnke FH , Abonante S , Maggiolini M .

Estrogens regulate numerous pathophysiological processes, mainly by binding to and activating estrogen receptor (ER)α and ERβ. Increasing amounts of evidence have recently demonstrated that G-protein coupled receptor 30 (GPR30; also known as GPER) is also involved in diverse biological responses to estrogens both in normal and cancer cells. The classical ER and GPER share several features, including the ability to bind to identical compounds; nevertheless, some ligands exhibit opposed activity through these receptors. It is worth noting that, owing to the availability of selective agonists and antagonists of GPER for research, certain differential roles elicited by GPER compared with ER have been identified. Here, we provide evidence on the molecular mechanisms through which a calixpyrrole derivative acts as a GPER antagonist in different model systems, such as breast tumor cells and cancer-associated fibroblasts (CAFs) obtained from breast cancer patients. Our data might open new perspectives toward the development of a further class of selective GPER ligands in order to better dissect the role exerted by this receptor in different pathophysiological conditions. Moreover, calixpyrrole derivatives could be considered in future anticancer strategies targeting GPER in cancer cells.

PubMed ID: 26183213
PMC ID: PMC4610237
Article link: Dis Model Mech

Species referenced: Xenopus
Genes referenced: akt1 ccn1 ccn2 egr1 fos mapk1 tbx1 tff3.1

Article Images: [+] show captions
References [+] :
Aboussekhra, Role of cancer-associated fibroblasts in breast cancer development and prognosis. 2011, Pubmed