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  • antagonist
  • The effect of a selective CCR2 antagonist, RS504393 on pain hypersensitivity was checked by behavioral testing. (biomedcentral.com)
  • Finally, intracisternal injection of CCR2 antagonist, RS504393 (1, 10 μg) significantly attenuated IAMNT-induced heat hyperalgesia. (biomedcentral.com)
  • Using these cell lines we confirm that eotaxin-1 and eotaxin-3 can act as an agonist and an antagonist, respectively, of CCR2. (docphin.com)
  • In addition, we show that eotaxin-2 is an antagonist of CCR2 and MCP-1 is an agonist of CCR3. (docphin.com)
  • Under the agreement: * Pfizer gains exclusive worldwide development and commercialization rights to Incyte's portfolio of CCR2 antagonist compounds, the most advanced of which is currently in Phase IIa studies in rheumatoid arthritis and insulin-resistant obese patients. (biospace.com)
  • We are excited about Incyte's CCR2 antagonist program and its potential use in treating a range of chronic diseases with significant unmet medical need. (biospace.com)
  • Paul A. Friedman, M.D., President and CEO of Incyte, stated: "Our CCR2 antagonist program has the potential to generate multiple products in a variety of major indications, and Pfizer, with its unique breadth of capabilities, is ideally positioned to maximize the value of the program to patients. (biospace.com)
  • The company's lead internal compounds include INCB3284, a proprietary oral CCR2 antagonist that is in Phase II development for a number of inflammation-driven diseases, and INCB7839, a proprietary oral sheddase inhibitor that is in Phase I development as a potential treatment for cancer. (biospace.com)
  • CCL2-CCR2
  • The data suggest that CCL2-CCR2 signaling may be involved in the maintenance of orofacial neuropathic pain via astroglial-neuronal interaction. (biomedcentral.com)
  • Targeting CCL2-CCR2 signaling may be a potentially important new treatment strategy for trigeminal neuralgia. (biomedcentral.com)
  • Targets of CCR2 signaling include mitogen-activated protein kinase (MAPK) [ 22 ], an important intracellular signaling in regulating neural plasticity and inflammatory responses [ 23 ], indicating CCL2-CCR2 may be involved in neuroinflammation and chronic pain. (biomedcentral.com)
  • The CCL2/CCR2 chemokine pathway is best known for regulating breast cancer progression through macrophage-dependent mechanisms. (aacrjournals.org)
  • Here, we demonstrated important biological roles for CCL2/CCR2 signaling in breast cancer cells. (aacrjournals.org)
  • This report sheds novel light on CCL2/CCR2 chemokine signaling as a mitogenic pathway and cell-cycle regulator in breast cancer cells. (aacrjournals.org)
  • Disrupting the CCL2-CCR2 axis in combination with radiotherapy holds promise for improving radiotherapy efficacy in PDAC. (aacrjournals.org)
  • mRNA
  • CFA administration induced marked up-regulation of CCR2 mRNA in the skin and a moderate increase in the sciatic nerve and dorsal root ganglia (DRG). (pnas.org)
  • In response to nerve ligation, persistent and marked up-regulation of CCR2 mRNA was evident in the nerve and DRG. (pnas.org)
  • agonist
  • AT 2 R (Angiotensin AT2 Receptor) Agonist, Compound 21, Prevents Abdominal Aortic Aneurysm Progression in the Rat. (nih.gov)
  • novel
  • Nov. 21 /PRNewswire-FirstCall/ -- Pfizer Inc, and Incyte Corporation announced today that the two companies have entered into a global collaborative research and license agreement for the development, manufacture and marketing of novel oral CCR2 antagonists. (biospace.com)
  • antagonists
  • Incyte will receive an upfront payment of $40 million and will be eligible to receive additional milestone payments of up to $743 million for the successful development and commercialization of CCR2 antagonists in multiple indications, as well as royalties on worldwide sales. (biospace.com)
  • whereas
  • one of two isoforms encoded by CCR2 ), endocytic recycling is important to sustain monocyte migration, whereas filamin A (FLNa) is essential for CCL2-induced monocyte migration. (biologists.org)
  • The results show that residues Trp98 2.60 and Thr292 7.40 contribute significantly to the efficacy of both TAK-779 and Teijin compound 1, whereas His121 3.33 and Ile263 6.55 contribute significantly only to the antagonistic effect of Teijin compound 1 at CCR2. (aspetjournals.org)
  • compound
  • Pfizer will also provide research funding to Incyte to support the continued expansion of the CCR2 compound portfolio. (biospace.com)
  • tissues
  • In blood, Ccr2(-/-) monocytes could traffic to sites of infection, demonstrating that CCR2 is not required for migration from the circulation into tissues. (nih.gov)
  • GPCR
  • Therefore, explaining the control of receptor sorting into different degradative or recycling endocytic pathways is fundamental to understand GPCR function. (biologists.org)
  • residues
  • Modeling studies support the hypothesis that the residues Tyr49 1.39 , Trp98 2.60 , Tyr120 3.32 , and Glu291 7.39 of CCR2 form a tight network of aromatic cluster and polar contacts between transmembrane helices 1, 2, 3, and 7. (aspetjournals.org)