The present Research Topic of Frontiers in Endocrinology is dedicated to the importance of G protein-coupled receptors (GPCRs) and their therapeutic interests in chronic inflammatory and cancer diseases. The GPCR protein family, which exhibits an important role in human physiological and pathological contexts, represents the largest class of membrane receptors displaying a very wide molecular diversity in terms of extracellular stimuli. GPCRs-targeted drugs currently depict about 35% of prescribed medication for the treatment of various human diseases. With the recent advances in GPCR structural biology and the development of allosteric and biased ligands, the past decade has seen the blooming of GPCR-related drug discovery.
Chronic inflammatory diseases and cancers are the most significant causes of death in the world. It is widely recognized that chronic inflammatory diseases represent a fertile base to the development of certain types of cancer. For many years, a great accumulation of data has clearly demonstrated that GPCRs were involved in a large number of pathologies including cardiovascular dysfunction, asthma, neurological/neurodegenerative disorders, metabolic diseases and diabetes but also in chronic inflammatory and cancers. The expression of GPCRs in immune system reveals their pivotal role in inflammatory processes such as immune cell activity (i.e. cytokine production and chemotaxis), modulation of specific signaling pathway (i.e. NF?B), angiogenesis and tissue repair. Alongside, various GPCRs which are under- and/or overexpressed in cancer cells, play a role from the initiation to the progression of cancer by regulating either proliferative or apoptotic processes.
In this Research Topic, we will point out the impact of GPCRs in the pathophysiology of chronic inflammatory and cancer diseases. Through relevant examples, and via means of review articles, our goal is to provide readers with a set of ideas to consider GPCRs as very promising targets having potential therapeutic applications in the treatment of the aforementioned human diseases.
The present Research Topic of Frontiers in Endocrinology is dedicated to the importance of G protein-coupled receptors (GPCRs) and their therapeutic interests in chronic inflammatory and cancer diseases. The GPCR protein family, which exhibits an important role in human physiological and pathological contexts, represents the largest class of membrane receptors displaying a very wide molecular diversity in terms of extracellular stimuli. GPCRs-targeted drugs currently depict about 35% of prescribed medication for the treatment of various human diseases. With the recent advances in GPCR structural biology and the development of allosteric and biased ligands, the past decade has seen the blooming of GPCR-related drug discovery.
Chronic inflammatory diseases and cancers are the most significant causes of death in the world. It is widely recognized that chronic inflammatory diseases represent a fertile base to the development of certain types of cancer. For many years, a great accumulation of data has clearly demonstrated that GPCRs were involved in a large number of pathologies including cardiovascular dysfunction, asthma, neurological/neurodegenerative disorders, metabolic diseases and diabetes but also in chronic inflammatory and cancers. The expression of GPCRs in immune system reveals their pivotal role in inflammatory processes such as immune cell activity (i.e. cytokine production and chemotaxis), modulation of specific signaling pathway (i.e. NF?B), angiogenesis and tissue repair. Alongside, various GPCRs which are under- and/or overexpressed in cancer cells, play a role from the initiation to the progression of cancer by regulating either proliferative or apoptotic processes.
In this Research Topic, we will point out the impact of GPCRs in the pathophysiology of chronic inflammatory and cancer diseases. Through relevant examples, and via means of review articles, our goal is to provide readers with a set of ideas to consider GPCRs as very promising targets having potential therapeutic applications in the treatment of the aforementioned human diseases.