To understand brain function, it is essential that we discover how cellular signaling specifies
normal and pathological brain function. In this regard, chemogenetic technologies represent …

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 …

▪ Abstract Opioid receptors belong to the large superfamily of seven transmembrane-
spanning (7TM) G protein-coupled receptors (GPCRs). As a class, GPCRs are of …

In a screen of drugs previously tested in humans we identified itraconazole, a systemic
antifungal, as a potent antagonist of the Hedgehog (Hh) signaling pathway that acts by a …

G protein-coupled, seven-transmembrane segment receptors (GPCRs or 7TM receptors),
with more than 1000 different members, comprise the largest superfamily of proteins in the …

G protein-coupled receptors (GPCRs) represent the largest family of cell-surface receptors.
These receptors are natural allosteric proteins because agonist-mediated signaling by …

Binding, gating, a nity and e cacy Page 1 SEMINAR Binding, gating, a nity and e cacy The nature
of the problem Some history The classical era The interaction between binding and conformation …

Cell-surface receptors are the targets for more than 60% of current drugs. Traditionally,
optimizing the interaction of lead molecules with the binding site for the endogenous agonist …

Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are
2 concepts in contemporary pharmacology that have major implications for the use of drugs …

The aim of this review is to provide a systematic overview on constitutively active G-protein-
coupled receptors (GPCRs), a rapidly evolving area in signal transduction research. We will …