The emerging mutational landscape of G proteins and G-protein-coupled receptors in cancer

M O'hayre, J Vázquez-Prado, I Kufareva… - Nature reviews …, 2013 - nature.com
Nature reviews cancer, 2013nature.com
Aberrant expression and activity of G proteins and G-protein-coupled receptors (GPCRs) are
frequently associated with tumorigenesis. Deep sequencing studies show that 4.2% of
tumours carry activating mutations in GNAS (encoding Gαs), and that oncogenic activating
mutations in genes encoding Gαq family members (GNAQ or GNA11) are present in∼ 66%
and∼ 6% of melanomas arising in the eye and skin, respectively. Furthermore, nearly 20%
of human tumours harbour mutations in GPCRs. Many human cancer-associated viruses …
Abstract
Aberrant expression and activity of G proteins and G-protein-coupled receptors (GPCRs) are frequently associated with tumorigenesis. Deep sequencing studies show that 4.2% of tumours carry activating mutations in GNAS (encoding Gαs), and that oncogenic activating mutations in genes encoding Gαq family members (GNAQ or GNA11) are present in ∼66% and ∼6% of melanomas arising in the eye and skin, respectively. Furthermore, nearly 20% of human tumours harbour mutations in GPCRs. Many human cancer-associated viruses also express constitutively active viral GPCRs. These studies indicate that G proteins, GPCRs and their linked signalling circuitry represent novel therapeutic targets for cancer prevention and treatment.
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