Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

Targeting GPCRs & their Signaling as a Therapeutic Option in Melanoma

Version 1 : Received: 6 January 2022 / Approved: 10 January 2022 / Online: 10 January 2022 (13:41:08 CET)

A peer-reviewed article of this Preprint also exists.

Raymond, J.H.; Aktary, Z.; Larue, L.; Delmas, V. Targeting GPCRs and Their Signaling as a Therapeutic Option in Melanoma. Cancers 2022, 14, 706. Raymond, J.H.; Aktary, Z.; Larue, L.; Delmas, V. Targeting GPCRs and Their Signaling as a Therapeutic Option in Melanoma. Cancers 2022, 14, 706.

Journal reference: Cancers 2022, 14, 706
DOI: 10.3390/cancers14030706

Abstract

G protein-coupled receptors (GPCRs) serve prominent roles in melanocyte lineage physiology, with an impact at all stages of development, as well as on mature melanocyte functions. GPCR ligands are present in the skin and regulate melanocyte homeostasis, including pigmentation. The role of GPCRs in the regulation of pigmentation and, consequently, protection against external aggression, such as ultraviolet radiation, has long been established. However, evidence of new functions of GPCRs directly in melanomagenesis has been highlighted in recent years. GPCRs are coupled, through their intracellular domains, to heterotrimeric G proteins, which induce cellular signaling through various pathways. Such signaling modulates essential cellular processes of melanomagenesis, such as proliferation and migration. GPCR-associated signaling in melanoma can be activated by the binding of paracrine factors to their receptors or directly by activating mutations. In this review, we present melanoma-associated alterations of GPCRs and their downstream signaling and discuss the various preclinical models used to evaluate new therapeutic approaches against GPCR activity in melanoma. Recent striking advances in our understanding of the structure, function, and regulation of GPCRs will undoubtedly broaden treatment options in melanoma in the future.

Keywords

G protein-coupled receptor; mouse models; skin cancer; UVR; drug; network

Subject

LIFE SCIENCES, Cell & Developmental Biology

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