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Monitoring endogenous GPCRs: lessons for drug design
G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed i...
Novel Molecular Targets for the Treatment of Pain
Topic Editor John Streicher is a co-founder and equity partner of Teleport Pharmaceuticals, LLC. All other Topic Editors declare no competing interests with regards to the Research Topic subject.
Opioids and Their Receptors
The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistr...
The G Protein-Coupled Receptors Handbook
A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.
Cannabinoids in Health and Disease
This book provides a comprehensive overview of current knowledge of cannabinoid activity in human physiology and points out the importance of endocannabinoid system for the maintenance of human health and treatment of diseases. Each chapter has been organized with the aim to cover basic concepts in the modulation of endocannabinoid system in both physiological and pathological conditions, thanks to the integration of data from experimental animal models and clinical observations. A special focus has been put on the medical use of cannabinoids and on the targeting of endocannabinoid system as new therapeutic strategy for the prevention and treatment of human diseases. Taken together, this book targets a wide audience of basic and clinical scientists, teachers and students interested in gaining a better understanding in the field of cannabinoids.
