Results 221 to 230 of about 22,074 (250)

Role of the Chemokine Receptors CXCR3 and CCR4 in Human Pulmonary Fibrosis

American Journal of Respiratory and Critical Care Medicine, 2006
Abstract Rationale The chemokine receptors CXCR3 and CCR4 have recently been described as playing a pivotal role in the mouse model of bleomycin-induced fibrosis. Objectives To evaluate the role of these receptors in ...
Pignatti P., Brunetti G., Moretto D., Yacoub M. -R., Fiori M., Balbi B., Balestrino A., Cervio G., Nava S., Moscato G.   +9 more
openaire   +3 more sources

Special ergolines efficiently inhibit the chemokine receptor CXCR3 in blood

Bioorganic & Medicinal Chemistry Letters, 2011
The structure-activity relationship of highly potent special ergolines which selectively block the chemokine receptor CXCR3 is reported. The most potent compounds showed IC(50) values below 10nM in both ligand binding and Ca(2+)-mobilization assays.
Gebhard, Thoma, Rolf, Baenteli, Ian, Lewis, Darryl, Jones, Jiri, Kovarik, Markus B, Streiff, Hans-Guenter, Zerwes   +6 more
openaire   +2 more sources

Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3

Bioorganic & Medicinal Chemistry Letters, 2008
Modification of a 2-iminobenzimidazole series derived from an HTS hit resulted in compounds with improved in-vitro species selectivity. Incorporation of an 8-quinoline amide and conformational rigidification of an aliphatic tether furnished potent compounds suitable for further lead optimization.
Martin E, Hayes, Eric C, Breinlinger, Grier A, Wallace, Pintipa, Grongsaard, Wenyan, Miao, Michael J, McPherson, Robert H, Stoffel, David W, Green, Gregory P, Roth   +8 more
openaire   +2 more sources

Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3

Bioorganic & Medicinal Chemistry Letters, 2008
High-throughput screening identified a low molecular weight antagonist of CXCR3 displaying micromolar activity in a membrane filtration-binding assay. Systematic modification of the benzimidazole core and tethered acetophenone moiety established tractable SAR of analogs with improved physicochemical properties and sub-micromolar activity across both ...
Martin E, Hayes, Grier A, Wallace, Pintipa, Grongsaard, Agnieszka, Bischoff, Dawn M, George, Wenyan, Miao, Michael J, McPherson, Robert H, Stoffel, David W, Green, Gregory P, Roth   +9 more
openaire   +2 more sources

Discovery and Characterization of Biased Allosteric Agonists of the Chemokine Receptor CXCR3

Journal of Medicinal Chemistry, 2016
In this work we report a design, synthesis, and detailed functional characterization of unique strongly biased allosteric agonists of CXCR3 that contain tetrahydroisoquinoline carboxamide cores. Compound 11 (FAUC1036) is the first strongly biased allosteric agonist of CXCR3 that selectively induces weak chemotaxis and leads to receptor internalization ...
Milanos, Lampros, Brox, Regine, Frank, Theresa, Poklukar, Gašper, Palmisano, Ralf, Waibel, Reiner, Einsiedel, Jürgen, Dürr, Maximilian, Ivanović-Burmazović, Ivana, Larsen, Olav, Hjortø, Gertrud Malene, Rosenkilde, Mette Marie, Tschammer, Nuska   +12 more
openaire   +3 more sources

Identification of CXCR3 receptor agonists in combinatorial small-molecule libraries

Biochemical and Biophysical Research Communications, 2006
In a high-throughput screen of four million compounds from combinatorial libraries for small-molecule modulators of the chemokine receptor CXCR3, two classes of receptor agonists, based on tetrahydroisoquinoline and piperidinyl diazepanone templates, were identified.
Ilana L, Stroke, Andrew G, Cole, Srilatha, Simhadri, Marc-Raleigh, Brescia, Madhuri, Desai, Joan J, Zhang, J Robert, Merritt, Kenneth C, Appell, Ian, Henderson, Maria L, Webb   +9 more
openaire   +2 more sources

N-terminal region of human chemokine receptor CXCR3: Structural analysis of CXCR3(1–48) by experimental and computational studies

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2014
Our study on the highly charged N-terminal peptide of the human chemokine receptor CXCR3 by spectroscopic methods in solution and by means of molecular dynamics simulations showed that the charge content modulates the intrinsic structural preference of its flexible backbone.
Raucci R, Colonna G, GIOVANE, Alfonso, Castello G, Costantini S.   +4 more
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The expression of chemokine receptor CXCR3: relevance to disease activity of rheumatoid arthritis

Modern Rheumatology, 2003
Abstract  CXC chemokine receptor 3 (CXCR3) is selectively expressed on T helper 1 (Th1) type T cells and has been shown to be responsible for Th1-dominant immune responses. In this study, we analyzed the expression of CXCR3 on peripheral blood T lymphocytes of patients with rheumatoid arthritis (RA) by FACS analysis using antihuman CXCR3 monoclonal ...
Yumi, Motoki, Kenji, Tani, Teruki, Shimizu, Hiroyuki, Tamiya, Kayoko, Hase, Yasukazu, Ohmoto, Kouji, Matsushima, Saburo, Sone   +7 more
openaire   +2 more sources

Modulatory effects of peroxisome proliferator-activated receptor-γ on CXCR3 chemokines.

Recent patents on inflammation & allergy drug discovery, 2014
An increasing body of evidence shows the importance of the chemokine (C-X-C motif) receptor (CXCR)3 and cognate chemokines (C-X-C motif) ligand (CXCL)9, CXCL10 and CXCL11 in the T helper 1 immune response, and in inflammatory diseases such as bowel inflammatory disorders, allograft rejection, thyroid autoimmune disorders, vascular and renal ...
FERRARI, Silvia Martina, Antonelli, Alessandro, Di Domenicantonio, Andrea, MANFREDI, Andreina Teresa, FERRI, Clodoveo, Fallahi, Poupak   +5 more
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[Significance of chemokine receptor CXCR3 expression in breast cancer].

Zhonghua bing li xue za zhi = Chinese journal of pathology, 2011
To investigate the expression of CXCR3 and its association with clinicopathologic features in breast carcinoma.The expression level of CXCR3 in 18 samples of breast cancer and corresponding normal tissues was investigated using reverse transcriptase-polymerase chain reaction (RT-PCR) and real-time RT-PCR analysis.
Lei, Li, Jie, Chen, Zhao-hui, Lu, Shuang-ni, Yu, Yu-feng, Luo, Wu-gan, Zhao, Yi-hui, Ma, Cong-wei, Jia   +7 more
openaire   +1 more source