Kinase cascades and ligand-directed signaling at the kappa opioid receptor

MR Bruchas, C Chavkin - Psychopharmacology, 2010 - Springer
Abstract Background and Rationale The dynorphin/kappa opioid receptor (KOR) system has
been implicated as a critical component of the stress response. Stress-induced activation of …

Drug efficacy at G protein–coupled receptors

T Kenakin - Annual review of pharmacology and toxicology, 2002 - annualreviews.org
Efficacy has been defined in receptor pharmacology as a proportionality factor denoting the
amount of physiological response a given ligand imparts to a biological system for a given …

[PDF][PDF] Heterodimerization of μ and δ opioid receptors: a role in opiate synergy

I Gomes, BA Jordan, A Gupta… - The Journal of …, 2000 - Soc Neuroscience
Opiate analgesics are widely used in the treatment of severe pain. Because of their
importance in therapy, different strategies have been considered for making opiates more …

Mitogen-activated protein kinase regulates dopamine transporter surface expression and dopamine transport capacity

JA Morón, I Zakharova, JV Ferrer, GA Merrill… - Journal of …, 2003 - Soc Neuroscience
The dopamine transporter (DAT) regulates the clearance of dopamine (DA) released into the
extracellular space and is an important site on which psychostimulants act to produce their …

Oligomerization of opioid receptors with β2-adrenergic receptors: A role in trafficking and mitogen-activated protein kinase activation

BA Jordan, N Trapaidze, I Gomes… - Proceedings of the …, 2001 - National Acad Sciences
G-protein-coupled receptors (GPCRs) have recently joined the list of cell surface receptors
that dimerize. Dimerization has been shown to alter the ligand-binding, signaling, and …

G-protein-coupled receptor dimerization: modulation of receptor function

CD Rios, BA Jordan, I Gomes, LA Devi - Pharmacology & therapeutics, 2001 - Elsevier
G-protein-coupled receptors (GPCRs) comprise the largest family of transmembrane
receptors in the human genome that respond to a plethora of signals, including …

Targeting opioid dysregulation in depression for the development of novel therapeutics

CA Browne, I Lucki - Pharmacology & therapeutics, 2019 - Elsevier
Since the serendipitous discovery of the first class of modern antidepressants in the 1950's,
all pharmacotherapies approved by the Food and Drug Administration for major depressive …

[HTML][HTML] Opioids and their complicated receptor complexes

BA Jordan, S Cvejic, LA Devi - Neuropsychopharmacology, 2000 - Elsevier
No field more eagerly awaits a molecular clarification for G-protein coupled receptor (GPCR)
dimerization than the opioid receptor field. Extensive evidence of pharmacological and …

Agonist-selective recruitment of engineered protein probes and of GRK2 by opioid receptors in living cells

M Stoeber, D Jullié, J Li, S Chakraborty, S Majumdar… - Elife, 2020 - elifesciences.org
G protein-coupled receptors (GPCRs) signal through allostery, and it is increasingly clear
that chemically distinct agonists can produce different receptor-based effects. It has been …

Targeting dynorphin/kappa opioid receptor systems to treat alcohol abuse and dependence

BM Walker, GR Valdez, JP McLaughlin, G Bakalkin - Alcohol, 2012 - Elsevier
This review represents the focus of a symposium that was presented at the “Alcoholism and
Stress: A Framework for Future Treatment Strategies” conference in Volterra, Italy on May 3 …