Molecular basis of opioid receptor signaling

T Che, BL Roth - Cell, 2023 - cell.com
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 …

Chemogenetics for cell-type-specific modulation of signalling and neuronal activity

HJ Kang, T Minamimoto, J Wess, BL Roth - Nature Reviews Methods …, 2023 - nature.com
Chemogenetics is an approach for engineering proteins to enable their modulation by
otherwise inert small molecules. Although kinases, enzymes and ion channels have been …

Structure of the nanobody-stabilized active state of the kappa opioid receptor

T Che, S Majumdar, SA Zaidi, P Ondachi, JD McCorvy… - Cell, 2018 - cell.com
The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric,
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …

[HTML][HTML] A new DREADD facilitates the multiplexed chemogenetic interrogation of behavior

E Vardy, JE Robinson, C Li, RHJ Olsen, JF DiBerto… - Neuron, 2015 - cell.com
DREADDs are chemogenetic tools widely used to remotely control cellular signaling,
neuronal activity, and behavior. Here we used a structure-based approach to develop a new …

Ligand and G-protein selectivity in the κ-opioid receptor

J Han, J Zhang, AL Nazarova, SM Bernhard… - Nature, 2023 - nature.com
The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not
only pain but also addiction and affective disorders. However, the development of KOR …

Structural basis for apelin control of the human apelin receptor

Y Ma, Y Yue, Y Ma, Q Zhang, Q Zhou, Y Song, Y Shen… - Structure, 2017 - cell.com
Apelin receptor (APJR) is a key regulator of human cardiovascular function and is activated
by two different endogenous peptide ligands, apelin and Elabela, each with different …

Opioid receptors: Structural and mechanistic insights into pharmacology and signaling

Y Shang, M Filizola - European journal of pharmacology, 2015 - Elsevier
Opioid receptors are important drug targets for pain management, addiction, and mood
disorders. Although substantial research on these important subtypes of G protein-coupled …

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 …

Design of κ-opioid receptor agonists for the development of potential treatments of pain with reduced side effects

F Santino, L Gentilucci - Molecules, 2023 - mdpi.com
The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for
the development of pain medications, without deleterious side effects associated with the μ …

Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues

AP Riley, CE Groer, D Young, AW Ewald… - Journal of medicinal …, 2014 - ACS Publications
The neoclerodane diterpene salvinorin A, found in the leaves of Salvia divinorum, is a potent
κ-opioid receptor agonist, making it an attractive scaffold for development into a treatment for …