Uncovering molecular mechanisms involved in activation of G protein-coupled receptors

U Gether - Endocrine reviews, 2000 - academic.oup.com
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 …

Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis …

K Kristiansen - Pharmacology & therapeutics, 2004 - Elsevier
The superfamily of G-protein-coupled receptors (GPCRs) could be subclassified into 7
families (A, B, large N-terminal family B-7 transmembrane helix, C, Frizzled/Smoothened …

Evolutionarily conserved networks of residues mediate allosteric communication in proteins

GM Süel, SW Lockless, MA Wall… - Nature structural …, 2003 - nature.com
A fundamental goal in cellular signaling is to understand allosteric communication, the
process by which signals originating at one site in a protein propagate reliably to affect …

G protein-coupled receptors: I. diversity of receptor-ligand interactions

TH Ji, M Grossmann, I Ji - Journal of biological chemistry, 1998 - jbc.org
Nearly 2000 G protein-coupled receptors (GPCRs) 1 have been reported since bovine opsin
was cloned in 1983 (1) and the-adrenergic receptor in 1986 (2). They are classified into over …

Molecular basis of receptor/G-protein-coupling selectivity

J Wess - Pharmacology & therapeutics, 1998 - Elsevier
Molecular cloning studies have shown that G-protein-coupled receptors form one of the
largest protein families found in nature, and it is estimated that approximately 1000 different …

α1-Adrenergic receptors: new insights and directions

MT Piascik, DM Perez - The Journal of pharmacology and experimental …, 2001 - Elsevier
The adrenergic receptors play a key role in the modulation of sympathetic nervous system
activity as well as a site of action for many therapeutic agents. The α 1-adrenergic receptor …

Residues crucial for maintaining short paths in network communication mediate signaling in proteins

A Del Sol, H Fujihashi, D Amoros… - Molecular systems …, 2006 - embopress.org
Here, we represent protein structures as residue interacting networks, which are assumed to
involve a permanent flow of information between amino acids. By removal of nodes from the …

Inverse, protean, and ligand‐selective agonism: matters of receptor conformation

T Kenakin - The FASEB journal, 2001 - Wiley Online Library
Concepts regarding the mechanisms by which drugs activate receptors to produce
physiological response have progressed beyond considering the re¬ ceptor as a simple on …

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 …

How and why do GPCRs dimerize?

VV Gurevich, EV Gurevich - Trends in pharmacological sciences, 2008 - cell.com
Dimerization is fairly common in the G-protein-coupled receptor (GPCR) superfamily. First
attempts to rationalize this phenomenon gave rise to an idea that two receptors in a dimer …