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LMT-28
LMT-28 is an experimental drug which was the first molecule discovered that acts as an antagonist of IL6R, the receptor for Interleukin-6, and so blocks its activity in the body. Interleukin-6 is a cytokine signalling molecule which plays a key role in inflammation, so blocking IL6R is useful for alleviating a number of disease processes in which inflammation plays a part. Previously it has only been possible to block cytokine activity using biologics such as targeted antibodies which have various disadvantages, so the development of small molecule inhibitors is a considerable advance. LMT-28 is of relatively low potency and is unlikely to be developed as a medicine, but is useful for pharmaceutical research into the processes mediated by IL6R, and as a successful proof of concept it makes it likely that more potent small molecule antagonists for IL6R and other interleukin receptors will be developed in future. See also * IL-4-inhibitor-1 * Sarilumab * Tocilizumab Tocil ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IL6R
Interleukin 6 receptor (IL6R) also known as CD126 (Cluster of Differentiation 126) is a type I cytokine receptor. Function Interleukin 6 (IL6) is a potent pleiotropic cytokine that regulates cell growth and differentiation and plays an important role in immune response. Dysregulated production of IL6 and this receptor are implicated in the pathogenesis of many diseases, such as multiple myeloma, autoimmune diseases and prostate cancer. In melanocytes IL6R gene expression may be regulated by MITF. Structure The IL6 receptor is a protein complex consisting of an IL-6 receptor subunit (IL6R) and interleukin 6 signal transducer Glycoprotein 130. IL6R also denotes the human gene encoding this subunit. Alternatively spliced transcript variants encoding distinct isoforms have been reported. IL6R subunit is also shared by many other cytokines. Interactions Interleukin-6 receptor has been shown to interact with Interleukin 6 and ciliary neurotrophic factor. See also * Clust ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IL-4-inhibitor-1
IL-4-inhibitor-1 is an experimental drug which was the first molecule discovered that interferes with the binding between interleukin-4 and the Interleukin-4 receptor, and so blocks its activity in the body. Interleukin-4 is a cytokine signalling molecule which has an important role in processes such as inflammation and wound repair, but excessive IL-4 activity is a feature of some forms of cancer as well as some inflammatory conditions such as asthma, so blocking IL-4 activity may have several potential medical applications. IL-4-inhibitor-1 binds with reasonable affinity but is unlikely to be potent enough for clinical use, however its development is likely to lead to the development of more potent related drugs. The interleukin-4 receptor is also the target for a different cytokine interleukin-13, but it remains unclear at this stage whether IL-4-inhibitor-1 is selective for inhibition of IL-4 while sparing IL-13 activity, or if it blocks the activity of both cytokines. See a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antagonist (pharmacology)
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include s, |
Interleukin-6
Interleukin 6 (IL-6) is an interleukin that acts as both a pro-inflammatory cytokine and an anti-inflammatory myokine. In humans, it is encoded by the ''IL6'' gene. In addition, osteoblasts secrete IL-6 to stimulate osteoclast formation. Smooth muscle cells in the tunica media of many blood vessels also produce IL-6 as a pro-inflammatory cytokine. IL-6's role as an anti-inflammatory myokine is mediated through its inhibitory effects on TNF and IL-1 and its activation of IL-1ra and IL-10. There is some early evidence that IL-6 can be used as an inflammatory marker for severe COVID-19 infection with poor prognosis, in the context of the wider coronavirus pandemic. Function Immune system IL-6 is secreted by macrophages in response to specific microbial molecules, referred to as pathogen-associated molecular patterns ( PAMPs). These PAMPs bind to an important group of detection molecules of the innate immune system, called pattern recognition receptors (PRRs), includ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cytokine
Cytokines () are a broad and loose category of small proteins (~5–25 kDa) important in cell signaling. Cytokines are produced by a broad range of cells, including immune cells like macrophages, B cell, B lymphocytes, T cell, T lymphocytes and mast cells, as well as Endothelium, endothelial cells, fibroblasts, and various stromal cells; a given cytokine may be produced by more than one type of cell. Due to their size, cytokines cannot cross the lipid bilayer of cells to enter the cytoplasm and therefore typically exert their functions by interacting with specific cytokine receptor, cytokine receptors on the target cell surface. Cytokines are especially important in the immune system; cytokines modulate the balance between humoral immunity, humoral and cell-mediated immunity, cell-based immune responses, and they regulate the maturation, growth, and responsiveness of particular cell populations. Some cytokines enhance or inhibit the action of other cytokines in complex way ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sarilumab
Sarilumab, sold under the brand name Kevzara, is a human monoclonal antibody medication against the interleukin-6 receptor. Regeneron Pharmaceuticals and Sanofi developed the drug for the treatment of rheumatoid arthritis (RA), for which it received US FDA approval on 22 May 2017 and European Medicines Agency approval on 23 June 2017. Development in ankylosing spondylitis has been suspended after the drug failed to show clinical benefit over methotrexate in a phase II trial. Medical uses Sarilumab is used for the treatment of moderately to severely active rheumatoid arthritis in people who have not responded to, or did not tolerate, more conventional treatments. It can be used alone or in combination with methotrexate or other disease-modifying antirheumatic drugs (DMARDs). Drugs.com: Sarilumab . Accessed 29 November 2017. Contraindications In the European Union, sarilumab is contraindicated in people with active, severe infections. While this is not listed as a contraindi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tocilizumab
Tocilizumab, sold under the brand name Actemra among others, is an immunosuppressive drug, used for the treatment of rheumatoid arthritis, systemic juvenile idiopathic arthritis, polyarticular juvenile idiopathic arthritis, giant cell arteritis, cytokine release syndrome, COVID19, and systemic sclerosis-associated interstitial lung disease (SSc-ILD). It is a recombinant humanized monoclonal antibody of the immunoglobulin IgG1 subclass against the interleukin-6 receptor (IL-6R). Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such as autoimmune diseases, multiple myeloma and prostate cancer. Tocilizumab was jointly developed by Osaka University and Chugai, and was licensed in 2003 by Hoffmann-La Roche. Tocilizumab was approved for medica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isopropyl Compounds
In organic chemistry, a propyl group is a three-carbon alkyl substituent with chemical formula for the linear form. This substituent form is obtained by removing one hydrogen atom attached to the terminal carbon of propane. A propyl substituent is often represented in organic chemistry with the symbol Pr (not to be confused with the element praseodymium). An isomeric form of propyl is obtained by moving the point of attachment from a terminal carbon atom to the central carbon atom, named isopropyl or 1-methylethyl. To maintain four substituents on each carbon atom, one hydrogen atom has to be moved from the middle carbon atom to the carbon atom which served as attachment point in the ''n''-propyl variant, written as . Linear propyl is sometimes termed normal and hence written with a prefix ''n''- (i.e., ''n-''propyl), as the absence of the prefix ''n''- does not indicate which attachment point is chosen, i.e. absence of prefix does not automatically exclude the possibility of i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
