Historical perspectives and recent advances in small molecule ligands of selective/biased/multi-targeted μ/δ/κ opioid receptor (2019–2022)

Y He, Q Su, L Zhao, L Zhang, L Yu, J Shi - Bioorganic Chemistry, 2023 - Elsevier
The opioids have been used for more than a thousand years and are not only the most
widely prescribed drugs for moderate to severe pain and acute pain, but also the preferred …

Opioid ligands addressing unconventional binding sites and more than one opioid receptor subtype

A Drakopoulos, D Moianos, GM Prifti, G Zoidis… - …, 2022 - Wiley Online Library
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 …

[HTML][HTML] Opioids and Their Receptors: Present and Emerging Concepts in Opioid Drug Discovery II

RM Van Rijn, M Spetea - Molecules, 2022 - mdpi.com
A few neurotransmitter systems have fascinated the research community, as much as the
opioid system (ie, opioid ligands and their receptors). Over the years, scientific studies of the …

Identification of selective agonists and positive allosteric modulators for µ-and δ-opioid receptors from a single high-throughput screen

NT Burford, T Wehrman, D Bassoni… - Journal of …, 2014 - journals.sagepub.com
Hetero-oligomeric complexes of G protein–coupled receptors (GPCRs) may represent novel
therapeutic targets exhibiting different pharmacology and tissue-or cell-specific site of action …

Ligand-based discovery of a new scaffold for allosteric modulation of the μ-opioid receptor

P Bisignano, NT Burford, Y Shang… - Journal of chemical …, 2015 - ACS Publications
With the hope of discovering effective analgesics with fewer side effects, attention has
recently shifted to allosteric modulators of the opioid receptors. In the past two years, the first …

Discovery of μ, δ-opioid receptor dual-biased agonists that overcome the limitation of prior biased agonists

JH Lee, SY Shon, W Jeon, SJ Hong… - ACS Pharmacology & …, 2021 - ACS Publications
Morphine is widely used in pain management although the risk of side effects is significant.
The use of biased agonists to the G protein of μ-opioid receptors has been suggested as a …

Biased ligands at opioid receptors: Current status and future directions

T Che, H Dwivedi-Agnihotri, AK Shukla, BL Roth - Science signaling, 2021 - science.org
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 …

Designing safer analgesics via μ-opioid receptor pathways

HCS Chan, D McCarthy, J Li, K Palczewski… - Trends in …, 2017 - cell.com
Pain is both a major clinical and economic problem, affecting more people than diabetes,
heart disease, and cancer combined. While a variety of prescribed or over-the-counter …

[PDF][PDF] New pharmacological strategies for analgesic drug development: focus on biased µ-opioid receptor agonists

L Rullo, LM Losapio, C Morosini, S Candeletti… - …, 2022 - pharmadvances.com
Chronic pain affects more than 30% of people worldwide and although mortality rates are
highest for other pathologies, it is one of the main sources of human suffering and disability …

Structural insights accelerate the discovery of opioid alternatives

T Che, BL Roth - Annual review of biochemistry, 2021 - annualreviews.org
Opioids such as morphine and oxycodone are analgesics frequently prescribed for the
treatment of moderate or severe pain. Unfortunately, these medications are associated with …