Regulation of µ-opioid receptors: desensitization, phosphorylation, internalization, and tolerance
Morphine and related µ-opioid receptor (MOR) agonists remain among the most effective
drugs known for acute relief of severe pain. A major problem in treating painful conditions is …
drugs known for acute relief of severe pain. A major problem in treating painful conditions is …
Signaling at G-protein-coupled serotonin receptors: recent advances and future research directions
The broadly distributed monoaminergic neurotransmitter serotonin (5-hydroxytryptamine, 5-
HT) exerts its actions via 14 classes of receptor. With the exception of 5-HT 3 receptors …
HT) exerts its actions via 14 classes of receptor. With the exception of 5-HT 3 receptors …
The significance of G protein-coupled receptor crystallography for drug discovery
JA Salon, DT Lodowski, K Palczewski - Pharmacological reviews, 2011 - ASPET
Crucial as molecular sensors for many vital physiological processes, seven-transmembrane
domain G protein-coupled receptors (GPCRs) comprise the largest family of proteins …
domain G protein-coupled receptors (GPCRs) comprise the largest family of proteins …
Constitutive activity among orphan class-A G protein coupled receptors
AL Martin, MA Steurer, RS Aronstam - PloS one, 2015 - journals.plos.org
The purpose of this study was to evaluate the extent of constitutive activity among orphan
class-A G protein coupled receptors within the cAMP signaling pathway. Constitutive …
class-A G protein coupled receptors within the cAMP signaling pathway. Constitutive …
Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery
RA Bond, AP IJzerman - Trends in pharmacological sciences, 2006 - cell.com
The concept of constitutively active G-protein-coupled receptors is now firmly rooted in
receptor pharmacology. Many independent research groups have contributed to its …
receptor pharmacology. Many independent research groups have contributed to its …
Two distinct conformations of helix 6 observed in antagonist-bound structures of a β1-adrenergic receptor
R Moukhametzianov, T Warne… - Proceedings of the …, 2011 - National Acad Sciences
The β 1-adrenergic receptor (β 1AR) is a G-protein-coupled receptor whose inactive state
structure was determined using a thermostabilized mutant (β 1AR–M23). However, it was …
structure was determined using a thermostabilized mutant (β 1AR–M23). However, it was …
The ibogaine medical subculture
KR Alper, HS Lotsof, CD Kaplan - Journal of ethnopharmacology, 2008 - Elsevier
AIM OF THE STUDY: Ibogaine is a naturally occurring psychoactive indole alkaloid that is
used to treat substance-related disorders in a global medical subculture, and is of interest as …
used to treat substance-related disorders in a global medical subculture, and is of interest as …
Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics
YX Tao - Pharmacology & therapeutics, 2008 - Elsevier
The existence of constitutive activity for G protein-coupled receptors (GPCRs) was first
described in 1980s. In 1991, the first naturally occurring constitutively active mutations in …
described in 1980s. In 1991, the first naturally occurring constitutively active mutations in …
Cysteinyl‐leukotrienes and their receptors in asthma and other inflammatory diseases: critical update and emerging trends
Abstract Cysteinyl‐leukotrienes (cysteinyl‐LTs), that is, LTC4, LTD4, and LTE4, trigger
contractile and inflammatory responses through the specific interaction with G protein …
contractile and inflammatory responses through the specific interaction with G protein …
Cholinergic interneurons control the excitatory input to the striatum
P Pakhotin, E Bracci - Journal of Neuroscience, 2007 - Soc Neuroscience
How the extent and time course of presynaptic inhibition depend on the action potentials of
the neuron controlling the terminals is unknown. We investigated this issue in the striatum …
the neuron controlling the terminals is unknown. We investigated this issue in the striatum …