Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor

MM Rosenkilde, LO Gerlach, JS Jakobsen… - Journal of Biological …, 2004 - ASBMB
AMD3100 is a symmetric bicyclam, prototype non-peptide antagonist of the CXCR4
chemokine receptor. Mutational substitutions at 16 positions located in TM-III,-IV,-V,-VI, and …

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor

C Watson, S Jenkinson, W Kazmierski, T Kenakin - Molecular pharmacology, 2005 - ASPET
4-{[4-({(3 R)-1-Butyl-3-[(R)-cyclohexyl (hydroxy) methyl]-2, 5dioxo-1, 4, 9-triazaspiro [5.5]
undec-9-yl} methyl) phenyl] oxy} benzoic acid hydrochloride (873140) is a potent …

Eotaxin and the attraction of eosinophils to the asthmatic lung

DM Conroy, TJ Williams - Respiratory research, 2001 - Springer
Eosinophilic leukocytes accumulate in high numbers in the lungs of asthmatic patients, and
are believed to be important in the pathogenisis of asthma. A potent eosinophil …

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 …

Structure-function relationship between the human chemokine receptor CXCR3 and its ligands

I Clark-Lewis, I Mattioli, JH Gong, P Loetscher - Journal of Biological …, 2003 - ASBMB
I-TAC, IP10, and Mig are interferon-γ inducible CXC chemokines that share the same G-
protein-coupled receptor CXCR3, which is preferentially expressed on Th1 lymphocytes. We …

I want a new drug: G-protein-coupled receptors in drug development

S Schlyer, R Horuk - Drug discovery today, 2006 - Elsevier
Huey Lewis and the News summed it up nicely in their 1980s hit record:'I want a new drug,
one that won't make me sick, one that won't make me crash my car, or make me feel three …

Cytokine modulators as novel therapies for asthma

PJ Barnes - Annual review of pharmacology and toxicology, 2002 - annualreviews.org
Cytokines play a critical role in orchestrating and perpetuating inflammation in asthmatic
airways and several specific cytokine and chemokine inhibitors are now in development for …

CXCL4/Platelet Factor 4 is an agonist of CCR1 and drives human monocyte migration

JM Fox, F Kausar, A Day, M Osborne, K Hussain… - Scientific reports, 2018 - nature.com
Activated platelets release micromolar concentrations of the chemokine CXCL4/Platelet
Factor-4. Deposition of CXCL4 onto the vascular endothelium is involved in atherosclerosis …

Small, nonpeptide p75NTR ligands induce survival signaling and inhibit proNGF-induced death

SM Massa, Y Xie, T Yang, AW Harrington… - Journal of …, 2006 - Soc Neuroscience
Studies showing that neurotrophin binding to p75NTR can promote cell survival in the
absence of Trk (tropomyosin-related kinase) receptors, together with recent structural data …

CCL26/eotaxin-3 is more effective to induce the migration of eosinophils of asthmatics than CCL11/eotaxin-1 and CCL24/eotaxin-2

V Provost, MC Larose, A Langlois… - Journal of leukocyte …, 2013 - academic.oup.com
ABSTRACT CCL11, CCL24, and CCL26 are chemokines involved in the recruitment of
eosinophils into tissues and mainly activate CCR3. Whereas the genomic or …