[HTML][HTML] Activation of the β2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6
JA Ballesteros, AD Jensen, G Liapakis… - Journal of Biological …, 2001 - ASBMB
The movements of transmembrane segments (TMs) 3 and 6 at the cytoplasmic side of the
membrane play an important role in the activation of G-protein-coupled receptors. Here we …
membrane play an important role in the activation of G-protein-coupled receptors. Here we …
[HTML][HTML] β2 adrenergic receptor activation: Modulation of the proline kink in transmembrane 6 by a rotamer toggle switch
In many rhodopsin-like G-protein-coupled receptors, agonist binding to a cluster of aromatic
residues in TM6 may promote receptor activation by altering the configuration of the TM6 Pro…
residues in TM6 may promote receptor activation by altering the configuration of the TM6 Pro…
[HTML][HTML] The forgotten serine: a critical role for Ser-2035.42 in ligand binding to and activation of the β2-adrenergic receptor
G Liapakis, JA Ballesteros, S Papachristou… - Journal of Biological …, 2000 - ASBMB
Previous work in the β 2 -adrenergic receptor demonstrated critical interactions between Ser-204
and Ser-207 in the fifth membrane-spanning segment and the meta-OH and para-OH, …
and Ser-207 in the fifth membrane-spanning segment and the meta-OH and para-OH, …
Mutation of a highly conserved aspartic acid in the β2 adrenergic receptor: constitutive activation, structural instability, and conformational rearrangement of …
SGF Rasmussen, AD Jensen, G Liapakis… - Molecular …, 1999 - ASPET
Movements of transmembrane segments (TMs) 3 and 6 play a key role in activation of G
protein-coupled receptors. However, the underlying molecular processes that govern these …
protein-coupled receptors. However, the underlying molecular processes that govern these …
[HTML][HTML] Constitutive activation of the β2 adrenergic receptor alters the orientation of its sixth membrane-spanning segment
JA Javitch, D Fu, G Liapakis, J Chen - Journal of Biological Chemistry, 1997 - ASBMB
The binding site of the β 2 adrenergic receptor, like that of other homologous G-protein-coupled
receptors, is contained within a water-accessible crevice formed among its seven …
receptors, is contained within a water-accessible crevice formed among its seven …
Synergistic contributions of the functional groups of epinephrine to its affinity and efficacy at the β2 adrenergic receptor
G Liapakis, WC Chan, M Papadokostaki… - Molecular pharmacology, 2004 - ASPET
The structural basis of ligand affinity can be approached by studying the interactions between
a drug and receptor residues; the basis for efficacy is more complex and must involve …
a drug and receptor residues; the basis for efficacy is more complex and must involve …
GnRH-Gemcitabine conjugates for the treatment of androgen-independent prostate cancer: pharmacokinetic enhancements combined with targeted drug delivery
Gemcitabine, a drug with established efficacy against a number of solid tumors, has
therapeutic limitations due to its rapid metabolic inactivation. The aim of this study was the …
therapeutic limitations due to its rapid metabolic inactivation. The aim of this study was the …
Novel long-acting somatostatin analog with endocrine selectivity: potent suppression of growth hormone but not of insulin
…, A Wolf, M Bracha, D Shohat, G Liapakis… - …, 2001 - academic.oup.com
Somatostatin, also known as somatotropin release-inhibiting factor (SRIF), is a natural cyclic
peptide inhibitor of pituitary, pancreatic, and gastrointestinal secretion. Its long-acting …
peptide inhibitor of pituitary, pancreatic, and gastrointestinal secretion. Its long-acting …
Lanthionine− somatostatin analogs: synthesis, characterization, biological activity, and enzymatic stability studies
…, KF Medzihradszky, DH Coy, G Liapakis… - Journal of medicinal …, 1997 - ACS Publications
A series of cyclic somatostatin analogs containing a lanthionine bridge have been subjected
to studies of structure−activity relationships. A direct synthesis of the thioether bridged …
to studies of structure−activity relationships. A direct synthesis of the thioether bridged …
Effects of cholesterol on GPCR function: insights from computational and experimental studies
S Kiriakidi, A Kolocouris, G Liapakis, S Ikram… - Direct mechanisms in …, 2019 - Springer
The extensive experimental and computational evidences revealed that cholesterol is involved
in the drug binding to G protein-coupled receptor (GPCR) targets that is influenced by the …
in the drug binding to G protein-coupled receptor (GPCR) targets that is influenced by the …