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GPCRs: Emerging anti-cancer drug targets
Ainhoa Nieto Gutierrez1, Patricia H McDonald1
1The Scripps Research Institute, Department of Molecular Medicine, 130 Scripps Way, Jupiter, FL 33458, United States.
Abstract:
G protein-coupled receptors (GPCRs) constitute the largest and most diverse protein family in the human genome with over 800 members identified to date. They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis. Consequently, aberrant receptor activity has been demonstrated in numerous disorders/diseases, and as a result GPCRs have become the most successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic disorders. Many independent studies have also demonstrated a key role for GPCRs in tumourigenesis, establishing their involvement in cancer initiation, progression, and metastasis. Given the growing appreciation of the role(s) that GPCRs play in cancer pathogenesis, it is surprising to note that very few GPCRs have been effectively exploited in pursuit of anti-cancer therapies. The present review provides a broad overview of the roles that various GPCRs play in cancer growth and development, highlighting the potential of pharmacologically modulating these receptors for the development of novel anti-cancer therapeutics.
Insights
G protein-coupled receptors (GPCRs) are crucial in cell functions and disease. This review explores their role in cancer, highlighting potential for new anti-cancer drugs by targeting these key receptors.
Area of Science:
- Molecular Biology
- Pharmacology
- Oncology
Background:
- G protein-coupled receptors (GPCRs) represent the largest human protein family, vital for cellular processes and implicated in various diseases.
- Aberrant GPCR activity is linked to numerous disorders, making them prime pharmaceutical targets for conditions like pain, inflammation, and metabolic diseases.
- GPCRs are increasingly recognized for their significant roles in cancer initiation, progression, and metastasis.
Purpose of the Study:
- To provide a comprehensive overview of GPCR involvement in cancer pathogenesis.
- To highlight the therapeutic potential of targeting GPCRs for novel anti-cancer strategies.
Main Methods:
- Literature review of studies investigating GPCRs in cancer.
- Analysis of GPCR roles in tumor growth, development, and metastasis.
- Evaluation of pharmacological modulation of GPCRs as anti-cancer therapeutics.
Main Results:
- GPCRs play diverse and critical roles in various stages of cancer development.
- Despite their established involvement, few GPCRs have been therapeutically exploited for cancer treatment.
- Pharmacological targeting of GPCRs presents a promising avenue for developing innovative anti-cancer therapies.
Conclusions:
- GPCRs are significant players in cancer biology, offering substantial opportunities for therapeutic intervention.
- Further research into GPCRs in oncology could lead to the development of novel anti-cancer drugs.
- Modulating GPCR activity holds promise for future cancer treatment strategies.