Results 211 to 220 of about 37,429 (252)

Recent developments in CCR2 antagonists

Expert Opinion on Therapeutic Patents, 2009
Monocyte chemoattractant protein-1 (MCP-1) is a major chemoattractant for monocytes and memory T cells by means of their binding to its specific cell-surface receptor, CC-chemokine receptor-2 (CCR2). CCR2 belongs to the G-protein-coupled seven-transmembrane receptor superfamily.
Zhihua Sui
exaly   +3 more sources

CCR2 Antagonists

Current Topics in Medicinal Chemistry, 2010
Inhibition of CCR2 has been considered as a target for multiple therapeutic diseases including autoimmune disease, atherosclerosis, pain, and metabolic disease, based in part on the critical role this receptor plays on monocyte migration. Numerous companies have reported programs to identify CCR2 antagonists.
Mary, Struthers, Alexander, Pasternak
openaire   +2 more sources

CCR1 and CCR2 Antagonists

Current Topics in Medicinal Chemistry, 2014
Chemokines constitute a family of small heparin-binding proteins which orchestrate the infiltration of leukocytes during inflammation, but also directly influence other physiological and pathophysiological processes. In humans, more than 40 chemokines are known binding to around 18 G-protein-coupled receptors. A non-redundant role of certain chemokines
Henning W, Zimmermann, Viktor, Sterzer, Hacer, Sahin   +2 more
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Characterization of the CCR2 chemokine receptor: functional CCR2 receptor expression in B cells

The Journal of Immunology, 1997
Abstract We have derived anti-human CCR2-specific mAbs by immunization with synthetic peptides corresponding to CCR2 sequences presumably involved in the interaction with its ligand(s). The characterization of these mAbs includes the ability to recognize the CCR2 receptor specifically, as well as the function based on their ability to
J M, Frade, M, Mellado, G, del Real, J C, Gutierrez-Ramos, P, Lind, C, Martinez-A   +5 more
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Role of CCR2 in orthodontic tooth movement

American Journal of Orthodontics and Dentofacial Orthopedics, 2012
Cytokines and chemokines regulate bone remodeling during orthodontic tooth movement. CC chemokine ligand 2 (CCL2) is involved in osteoclast recruitment and activity, and its expression is increased in periodontal tissues under mechanical loading. In this study, we investigated whether the CC chemokine receptor 2 (CCR2)-CCL2 axis influences orthodontic ...
Silvana Rodrigues de Albuquerque, Taddei, Ildeu, Andrade, Celso Martins, Queiroz-Junior, Thiago Pompermaier, Garlet, Gustavo Pompermaier, Garlet, Fernando de Queiroz, Cunha, Mauro Martins, Teixeira, Tarcília Aparecida, da Silva   +7 more
openaire   +2 more sources

Myeloid CCR2 Promotes Atherosclerosis after AKI

Journal of the American Society of Nephrology, 2022
Background The risk of cardiovascular events rises after AKI. Leukocytes promote atherosclerotic plaque growth and instability. We established a model of enhanced remote atherosclerosis after renal ischemia-reperfusion (IR) injury and investigated the underlying inflammatory mechanisms. Methods
Anne M. Hüsing, Vera C. Wulfmeyer, Svenja Gaedcke, Susanne V. Fleig, Song Rong, David DeLuca, Hermann Haller, Roland Schmitt, Sibylle von Vietinghoff   +8 more
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Identification of a sulfonamide series of CCR2 antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
Simon, Peace, Joanne, Philp, Carl, Brooks, Val, Piercy, Kitty, Moores, Chris, Smethurst, Steve, Watson, Simon, Gaines, Mara, Zippoli, Claudette, Mookherjee, Robert, Ife   +10 more
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The discovery of novel cyclohexylamide CCR2 antagonists

Bioorganic & Medicinal Chemistry Letters, 2011
As a result of further SAR studies on a piperidinyl piperidine scaffold, we report the discovery of compound 44, a potent, orally bioavailable CCR2 antagonist. While having some in vitro hERG activity, this molecule was clean in an in vivo model of QT prolongation. In addition, it showed excellent efficacy when dosed orally in a transgenic murine model
James C, Lanter, Thomas P, Markotan, Xuqing, Zhang, Nalin, Subasinghe, Fu-An, Kang, Cuifen, Hou, Monica, Singer, Evan, Opas, Sandra, McKenney, Carl, Crysler, Dana, Johnson, Christopher J, Molloy, Zhihua, Sui   +12 more
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Role of CCR2 in immunobiology and neurobiology

Clinical and Experimental Neuroimmunology, 2011
AbstractChemokines and their receptors play crucial roles in the trafficking of leukocytes and are of particular interest in the context of the unique inflammatory responses elicited in the central nervous system (CNS). The chemokine receptor CCR2 and its ligand CCL2 have been implicated in a wide range of immunobiological processes and ...
Ryo Yamasaki, LiPing Liu, Jessica Lin, Richard M. Ransohoff   +3 more
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The CCR2 receptor as a therapeutic target

Expert Opinion on Therapeutic Patents, 2005
The strict control of cell recruitment during the physiological inflammatory response fails in autoimmune inflammatory diseases. The chemokine system is a complex and redundant network of small soluble proteins and G-protein-coupled cell surface receptors that participate in the inflammatory response, mainly attracting cells to the inflammatory foci ...
Manuel Feria, Federico Díaz-González
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