Therapeutic potential of β-arrestin-and G protein-biased agonists
EJ Whalen, S Rajagopal, RJ Lefkowitz - Trends in molecular medicine, 2011 - cell.com
Members of the seven-transmembrane receptor (7TMR), or G protein-coupled receptor
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …
(GPCR), superfamily represent some of the most successful targets of modern drug therapy …
β-Arrestin-biased ligands at seven-transmembrane receptors
JD Violin, RJ Lefkowitz - Trends in pharmacological sciences, 2007 - cell.com
Seven-transmembrane receptors (7TMRs), the most common molecular targets of modern
drug therapy, are critically regulated by β-arrestins, which both inhibit classic G-protein …
drug therapy, are critically regulated by β-arrestins, which both inhibit classic G-protein …
Synthetic single domain antibodies for the conformational trapping of membrane proteins
I Zimmermann, P Egloff, CAJ Hutter, FM Arnold… - elife, 2018 - elifesciences.org
Mechanistic and structural studies of membrane proteins require their stabilization in specific
conformations. Single domain antibodies are potent reagents for this purpose, but their …
conformations. Single domain antibodies are potent reagents for this purpose, but their …
Chemokine receptor CCR5: insights into structure, function, and regulation
M Oppermann - Cellular signalling, 2004 - Elsevier
CC chemokine receptor 5 (CCR5) is a seven-transmembrane, G protein-coupled receptor
(GPCR) which regulates trafficking and effector functions of memory/effector T-lymphocytes …
(GPCR) which regulates trafficking and effector functions of memory/effector T-lymphocytes …
WHIM syndromes with different genetic anomalies are accounted for by impaired CXCR4 desensitization to CXCL12
K Balabanian, B Lagane, JL Pablos, L Laurent… - Blood, 2005 - ashpublications.org
The WHIM syndrome is a rare immunodeficiency disorder characterized by warts,
hypogammaglobulinemia, infections, and myelokathexis. Dominant heterozygous mutations …
hypogammaglobulinemia, infections, and myelokathexis. Dominant heterozygous mutations …
Expression of CCR7 in multiple sclerosis: implications for CNS immunity
P Kivisäkk, DJ Mahad, MK Callahan… - Annals of Neurology …, 2004 - Wiley Online Library
It is unclear how immune cells traffic between the lymphoid compartment and the central
nervous system (CNS), which lacks lymphatic vessels and is shielded by the blood–brain …
nervous system (CNS), which lacks lymphatic vessels and is shielded by the blood–brain …
Chemokines: attractive mediators of the immune response
MM Wong, EN Fish - Seminars in immunology, 2003 - Elsevier
An effective inflammatory immune response first requires the recruitment of cells to the site of
inflammation and then their appropriate activation and regulation. Chemokines are critical in …
inflammation and then their appropriate activation and regulation. Chemokines are critical in …
Ligand-selective receptor conformations revisited: the promise and the problem
T Kenakin - Trends in pharmacological sciences, 2003 - cell.com
Ligand-selective receptor conformations introduce the concept of 'texture'to drug effects, with
respect to ligands possessing quality in addition to quantity of efficacy. This cell-dependent …
respect to ligands possessing quality in addition to quantity of efficacy. This cell-dependent …
New paradigms in chemokine receptor signal transduction: Moving beyond the two-site model
Chemokine receptor (CKR) signaling forms the basis of essential immune cellular functions,
and dysregulated CKR signaling underpins numerous disease processes of the immune …
and dysregulated CKR signaling underpins numerous disease processes of the immune …
Chemokines, chemokine receptors and small-molecule antagonists: recent developments
JJ Onuffer, R Horuk - Trends in pharmacological sciences, 2002 - cell.com
The physiological roles of chemokine receptors have expanded beyond host defense and
now represent important targets for intervention in several disease indications. Chemokine …
now represent important targets for intervention in several disease indications. Chemokine …