G protein-coupled receptors as novel therapeutic targets in non-small-cell lung cancer

G protein-coupled receptors (GPCRs) actively participate in crucial cellular processes such as cell proliferation, differentiation, and communication. GPCRs play a pivotal role in the initiation and progression of tumors. In this review, focusing on non-small-cell lung cancer (NSCLC), one of the most prevalent cancers, we highlight the roles of GPCRs including understudied receptors in cancer oncogenesis and progression. We summarize current knowledge on GPCR functions in NSCLC, detailing their contributions to tumor development, progression, and therapy resistance. Furthermore, we evaluate the therapeutic potential of agents targeting GPCR-driven tumorigenic signaling in lung cancer. Critical knowledge gaps in understanding GPCR involvement in NSCLC biology are identified, and we address the limitations and challenges of targeting GPCRs for NSCLC treatment. This review provides insights into the current landscape, recent progress, and persisting challenges in developing GPCR-targeted anticancer therapies.