[HTML][HTML] G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a HDAC6-Pin1 axis

L Nogués, C Reglero, V Rivas, A Salcedo, V Lafarga… - …, 2016 - thelancet.com
L Nogués, C Reglero, V Rivas, A Salcedo, V Lafarga, M Neves, P Ramos, M Mendiola…
EBioMedicine, 2016thelancet.com
In addition to oncogenic drivers, signaling nodes can critically modulate cancer-related
cellular networks to strength tumor hallmarks. We identify G-protein-coupled receptor kinase
2 (GRK2) as a relevant player in breast cancer. GRK2 is up-regulated in breast cancer cell
lines, in spontaneous tumors in mice, and in a proportion of invasive ductal carcinoma
patients. Increased GRK2 functionality promotes the phosphorylation and activation of the
Histone Deacetylase 6 (HDAC6) leading to de-acetylation of the Prolyl Isomerase Pin1, a …
Abstract
In addition to oncogenic drivers, signaling nodes can critically modulate cancer-related cellular networks to strength tumor hallmarks. We identify G-protein-coupled receptor kinase 2 (GRK2) as a relevant player in breast cancer. GRK2 is up-regulated in breast cancer cell lines, in spontaneous tumors in mice, and in a proportion of invasive ductal carcinoma patients. Increased GRK2 functionality promotes the phosphorylation and activation of the Histone Deacetylase 6 (HDAC6) leading to de-acetylation of the Prolyl Isomerase Pin1, a central modulator of tumor progression, thereby enhancing its stability and functional interaction with key mitotic regulators. Interestingly, a correlation between GRK2 expression and Pin1 levels and de-acetylation status is detected in breast cancer patients. Activation of the HDAC6-Pin1 axis underlies the positive effects of GRK2 on promoting growth factor signaling, cellular proliferation and anchorage-independent growth in both luminal and basal breast cancer cells. Enhanced GRK2 levels promote tumor growth in mice, whereas GRK2 down-modulation sensitizes cells to therapeutic drugs and abrogates tumor formation. Our data suggest that GRK2 acts as an important onco-modulator by strengthening the functionality of key players in breast tumorigenesis such as HDAC6 and Pin1.
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