Traditionally, drugs are monovalent, targeting only one site on the protein surface. This
includes orthosteric and allosteric drugs, which bind the protein at orthosteric and allosteric …

G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …

Drugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the
treatment of pain, but activation of MOR with current opioid analgesics also produces …

Opioids are used for pain management despite the side effects that contribute to the opioid
crisis. The pursuit of non-addictive opioid analgesics remains unattained due to the …

Abstract Background and Purpose The illicit use of fentanyl‐like drugs (fentanyls), which are
μ opioid receptor agonists, and the many overdose deaths that result, has become a major …

The United States is experiencing the most profound and devastating opioid crisis in history,
with the number of deaths involving opioids, including prescription and illegal opioids …

G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …

Cannabis sativa is known for its therapeutic benefit in various diseases including pain relief
by targeting cannabinoid receptors. The primary component of cannabis, Δ9 …

Allosteric regulation, induced by perturbations at an allosteric site topographically distinct
from the orthosteric site, is one of the most direct and efficient ways to fine-tune …