期刊
SCIENCE SIGNALING
卷 14, 期 677, 页码 -出版社
AMER ASSOC ADVANCEMENT SCIENCE
DOI: 10.1126/scisignal.aav0320
关键词
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资金
- Wellcome Trust/DBT India Alliance [IA/S/20/1/504916]
- Swarnajayanti Fellowship of the Department of Science and Technology [DST/SJF/LSA-03/2017-18]
- Department of Biotechnology [DBT BT/PR29041/BRB/10/1697/2018]
- Science and Engineering Research Board [EMR/2017/003804]
- Young Scientist award from the Lady TATA Memorial Trust
- Indian Institute of Technology, Kanpur
- NIH [RO1MH61887, U19MH82441]
- NIMH Psychoactive Drug Screening Program
- Michael Hooker Distinguished Chair of Pharmacology [DA035764]
- NIDA [PO1 DA035764]
The opioid crisis has led to a search for safer and more effective opioids. The discovery of biased opioid ligands offers a potential alternative, but questions remain about their therapeutic benefits. More research is needed in this important area to understand the implications of biased agonism.
The opioid crisis represents a major worldwide public health crisis that has accelerated the search for safer and more effective opioids. Over the past few years, the identification of biased opioid ligands capable of eliciting selective functional responses has provided an alternative avenue to develop novel therapeutics without the side effects of current opioid medications. However, whether biased agonism or other pharmacological properties, such as partial agonism (or low efficacy), account for the therapeutic benefits remains questionable. Here, we provide a summary of the current status of biased opioid ligands that target the mu- and kappa-opioid receptors and highlight advances in preclinical and clinical trials of some of these ligands. We also discuss an example of structure-based biased ligand discovery at the.-opioid receptor, an approach that could revolutionize drug discovery at opioid and other receptors. Last, we briefly discuss caveats and future directions for this important area of research.
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