Research Topic

Orphan GPCRs as emerging drug targets

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About this Research Topic

G protein coupled-receptors (GPCRs) have been proven to be the most successful class of druggable targets in the human genome. It is estimated that 30 to 50% of all medications in the market exert their effect via no more than 80 members of this receptor family. New molecular entities (NMEs) targeting GPCRs ...

G protein coupled-receptors (GPCRs) have been proven to be the most successful class of druggable targets in the human genome. It is estimated that 30 to 50% of all medications in the market exert their effect via no more than 80 members of this receptor family. New molecular entities (NMEs) targeting GPCRs continue gaining FDA approval in the recent years with three in 2013, seven in 2012, five in 2011, and five in 2010. GPCR-based drug discovery remains active campaigns in major pharmaceutical companies. Key advances in pharmacological assays have led to deorphanization of over 30 GPCRs in the past decade. In light of the past success elucidating the structure, signaling, and physiological and pathophysiological functions of these receptors, together with the discovery of cognate and surrogate ligands, shall offer new opportunities for discovering next-generation medicines.
This Research Topic aims to discuss GPCR deorphanization strategies, technologies for elucidating receptor pharmacology, biased agonism of GPCR ligands, the potential of newly deorphanized GPCRs as drug targets, and the preclinical and clinical progress of drug candidates targeting unproven GPCR targets. This Research Topic welcomes both review and research papers related to the following topics:
• GPCR deorphanization strategies
• New generation of pharmacological assays that enable orphan GPCR drug discovery and development
• Constitutively active receptors in the orphan screening process
• Discovery of cognate and surrogate orphan GPCR ligands
• Signaling, and physiological and pathophysiological roles of orphan GPCRs
• Target identification associated with orphan GPCRs
• Orphan GPCR lead discovery and medicinal chemistry optimization
• Orphan GPCR translational research
• Animal models
• Preclinical and clinical development of orphan GPCR drugs


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