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 …

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 …

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 …

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 …

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 …

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 …

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 …

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 …

New paradigms in chemokine receptor signal transduction: Moving beyond the two-site model

AB Kleist, AE Getschman, JJ Ziarek, AM Nevins… - Biochemical …, 2016 - Elsevier
Chemokine receptor (CKR) signaling forms the basis of essential immune cellular functions,
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 …