Opioid Ligands Addressing Unconventional Binding Sites and More Than One Opioid Receptor Subtype. (31st May 2022)

• Record Type: Journal Article
• Authors: Drakopoulos, Antonios; Moianos, Dimitrios; Prifti, Georgia‐Myrto; Zoidis, Grigoris; Decker, Michael
• Is Part Of: ChemMedChem. Volume 17:Number 14(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-05-31
• Subjects: Opioids -- Allosteric ligands -- Bitopic ligands -- Bivalent ligands -- GPCR dimerization; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.202200169
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: Opioid receptors (ORs) represent one of the most significant groups of G‐protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function. In a constant effort to develop drugs with less side effects, and tools to explore the ORs nature and function, various (poly)pharmacological ligand design approaches have been performed. That is, besides classical ligands, a great number of bivalent ligands (i. e. aiming on two distinct OR subtypes), univalent heteromer‐selective ligands and bitopic and allosteric ligands have been synthesized for the ORs. The scope of our review is to present the most important of the aforementioned ligands, highlight their properties and exhibit the current state‐of‐the‐art pallet of promising drug candidates or useful molecular tools for the ORs. Abstract : Opioid receptors (ORs) are among the most important G‐protein coupled receptor (GPCR) drug targets. Except classical OR ligands, a great number of ligands with unconventional binding modes has been developed, i. e. bivalent ligands, univalent heteromer‐selective ligands, allosteric and bitopic ligands. This review presents the above categories, highlights the most important ligands, summarizes their properties and showcases their suggested mode of action.