Biased allosteric modulators: new frontiers in GPCR drug discovery
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …
Oxycodone in the opioid epidemic: high 'liking','wanting', and abuse liability
It is estimated that nearly a third of people who abuse drugs started with prescription opioid
medicines. Approximately, 11.5 million Americans used prescription drugs recreationally in …
medicines. Approximately, 11.5 million Americans used prescription drugs recreationally in …
Targeting multiple opioid receptors–improved analgesics with reduced side effects?
T Günther, P Dasgupta, A Mann, E Miess… - British journal of …, 2018 - Wiley Online Library
Classical opioid analgesics, including morphine, mediate all of their desired and undesired
effects by specific activation of the μ‐opioid receptor (μ receptor). The use of morphine for …
effects by specific activation of the μ‐opioid receptor (μ receptor). The use of morphine for …
New paradigms in GPCR drug discovery
KA Jacobson - Biochemical pharmacology, 2015 - Elsevier
G protein-coupled receptors (GPCRs) remain a major domain of pharmaceutical discovery.
The identification of GPCR lead compounds and their optimization are now structure-based …
The identification of GPCR lead compounds and their optimization are now structure-based …
Strategies towards safer opioid analgesics—A review of old and upcoming targets
BR Varga, JM Streicher… - British journal of …, 2023 - Wiley Online Library
Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target
the μ opioid receptor whose activation results in adverse effects like respiratory depression …
the μ opioid receptor whose activation results in adverse effects like respiratory depression …
Molecular pharmacology of δ-opioid receptors
Opioids are among the most effective analgesics available and are the first choice in the
treatment of acute severe pain. However, partial efficacy, a tendency to produce tolerance …
treatment of acute severe pain. However, partial efficacy, a tendency to produce tolerance …
Structural insights accelerate the discovery of opioid alternatives
Opioids such as morphine and oxycodone are analgesics frequently prescribed for the
treatment of moderate or severe pain. Unfortunately, these medications are associated with …
treatment of moderate or severe pain. Unfortunately, these medications are associated with …
Activation mechanism of the μ-opioid receptor by an allosteric modulator
S Kaneko, S Imai, N Asao, Y Kofuku… - Proceedings of the …, 2022 - National Acad Sciences
Allosteric modulators of G-protein-coupled receptors (GPCRs) enhance signaling by binding
to GPCRs concurrently with their orthosteric ligands, offering a novel approach to overcome …
to GPCRs concurrently with their orthosteric ligands, offering a novel approach to overcome …
Allostery at opioid receptors: modulation with small molecule ligands
KE Livingston, JR Traynor - British journal of pharmacology, 2018 - Wiley Online Library
Opioid receptors are 7‐transmembrane domain receptors that couple to heterotrimeric G
proteins. The endogenous ligands for opioid receptors are peptides which bind to the …
proteins. The endogenous ligands for opioid receptors are peptides which bind to the …
Endogenous opioids regulate moment-to-moment neuronal communication and excitability
BL Winters, GC Gregoriou, SA Kissiwaa… - Nature …, 2017 - nature.com
Fear and emotional learning are modulated by endogenous opioids but the cellular basis for
this is unknown. The intercalated cells (ITCs) gate amygdala output and thus regulate the …
this is unknown. The intercalated cells (ITCs) gate amygdala output and thus regulate the …