CU-CPT9a
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CU-CPT9a
CU-CPT9a is a drug which acts as a potent and selective antagonist of Toll-like receptor 8 (TLR8), with an IC50 of 0.5nM. Activation of toll-like receptors triggers release of cytokines and other signalling factors, leading to inflammation. This is an essential part of the immune system's response to infection, but chronic activation of TLR signalling is thought to be involved in various inflammatory and autoimmune disorders. CU-CPT9a has immunosuppressant properties, and may have applications in the treatment of autoimmune disorders, as well as being used in scientific research into the function of TLR8. See also * CU-CPT4a * Imiquimod Imiquimod, sold under the brand name Aldara among others, is a medication that acts as an immune response modifier that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. Scientists at 3M's pharmaceuticals ... * Motolimod References Receptor antagonists {{pharm-stub ...
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Toll-like Receptor 8
Toll-like receptor 8 is a protein that in humans is encoded by the ''TLR8'' gene. TLR8 has also been designated as CD288 (cluster of differentiation 288). It is a member of the toll-like receptor (TLR) family. Function TLR8 seems to function differently in humans and mice. Until recently, TLR8 was believed to be nonfunctional in mice, but it seems to counteract TLR7 activity The TLR family plays a fundamental role in pathogen recognition and activation of innate immunity. TLRs are highly conserved from ''Drosophila'' to humans and share structural and functional similarities. They recognize pathogen-associated molecular patterns (PAMPs) that are expressed on infectious agents, and mediate the production of cytokines necessary for the development of effective immunity. The various TLRs exhibit different patterns of expression. This gene is predominantly expressed in lung and peripheral blood leukocytes, and lies in close proximity to another family member, TLR7, on chromosome ...
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CU-CPT4a
CU-CPT4a is a drug which acts as a selective antagonist of Toll-like receptor 3 (TLR3), with an IC50 of 3.44 μM. It is used for research into the function of TRL3 and its role in inflammation, autoimmune disorders and cancer. See also * CU-CPT9a CU-CPT9a is a drug which acts as a potent and selective antagonist of Toll-like receptor 8 (TLR8), with an IC50 of 0.5nM. Activation of toll-like receptors triggers release of cytokines and other signalling factors, leading to inflammation. This ... References Receptor antagonists Benzothiophenes Carboxylic acids Organofluorides Organochlorides Amides {{pharm-stub ...
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Cytokine
Cytokines are a broad and loose category of small proteins (~5–25 kDa) important in cell signaling. Cytokines are peptides and cannot cross the lipid bilayer of cells to enter the cytoplasm. Cytokines have been shown to be involved in autocrine, paracrine and endocrine signaling as immunomodulating agents. Cytokines include chemokines, interferons, interleukins, lymphokines, and tumour necrosis factors, but generally not hormones or growth factors (despite some overlap in the terminology). Cytokines are produced by a broad range of cells, including immune cells like macrophages, B lymphocytes, T lymphocytes and mast cells, as well as endothelial cells, fibroblasts, and various stromal cells; a given cytokine may be produced by more than one type of cell. They act through cell surface receptors and are especially important in the immune system; cytokines modulate the balance between humoral and cell-based immune responses, and they regulate the maturation, growth, and res ...
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Inflammation
Inflammation (from la, wikt:en:inflammatio#Latin, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or Irritation, irritants, and is a protective response involving immune cells, blood vessels, and molecular mediators. The function of inflammation is to eliminate the initial cause of cell injury, clear out necrotic cells and tissues damaged from the original insult and the inflammatory process, and initiate tissue repair. The five cardinal signs are heat, pain, redness, swelling, and Functio laesa, loss of function (Latin ''calor'', ''dolor'', ''rubor'', ''tumor'', and ''functio laesa''). Inflammation is a generic response, and therefore it is considered as a mechanism of innate immune system, innate immunity, as compared to adaptive immune system, adaptive immunity, which is specific for each pathogen. Too little inflammation could lead to progressive tissue destruction by the harmful stimulus (e.g. b ...
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Immune System
The immune system is a network of biological processes that protects an organism from diseases. It detects and responds to a wide variety of pathogens, from viruses to parasitic worms, as well as cancer cells and objects such as wood splinters, distinguishing them from the organism's own healthy tissue. Many species have two major subsystems of the immune system. The innate immune system provides a preconfigured response to broad groups of situations and stimuli. The adaptive immune system provides a tailored response to each stimulus by learning to recognize molecules it has previously encountered. Both use molecules and cells to perform their functions. Nearly all organisms have some kind of immune system. Bacteria have a rudimentary immune system in the form of enzymes that protect against virus infections. Other basic immune mechanisms evolved in ancient plants and animals and remain in their modern descendants. These mechanisms include phagocytosis, antimicrobial pe ...
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Immunosuppressant
Immunosuppressive drugs, also known as immunosuppressive agents, immunosuppressants and antirejection medications, are drugs that inhibit or prevent activity of the immune system. Classification Immunosuppressive drugs can be classified into five groups: * glucocorticoids * cytostatics * antibodies * drugs acting on immunophilins * other drugs Glucocorticoids In pharmacologic (supraphysiologic) doses, glucocorticoids, such as prednisone, dexamethasone, and hydrocortisone are used to suppress various allergic, inflammatory, and autoimmune disorders. They are also administered as posttransplantory immunosuppressants to prevent the acute transplant rejection and graft-versus-host disease. Nevertheless, they do not prevent an infection and also inhibit later reparative processes. Immunosuppressive mechanism Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines Interleukin 1 (IL-1), IL-2, IL-3, IL-4, IL-5, IL- ...
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Imiquimod
Imiquimod, sold under the brand name Aldara among others, is a medication that acts as an immune response modifier that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. Scientists at 3M's pharmaceuticals division discovered the drug and 3M obtained the first FDA approval in 1997. As of 2015, imiquimod is generic and is available worldwide under many brands. Medical uses Imiquimod is a patient-applied cream prescribed to treat genital warts, Bowens disease ( squamous cell carcinoma in situ), and, secondary to surgery, for basal cell carcinoma, as well as actinic keratosis. Imiquimod 5% cream is indicated for the topical treatment of: * external genital and perianal warts (condylomata acuminata) in adults; * small superficial basal-cell carcinomas (sBCCs) in adults; * clinically typical, non-hyperkeratotic, non-hypertrophic actinic keratoses (AKs) on the face or scalp in immunocompetent adults when size or number of lesions limit the effica ...
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Motolimod
Motolimod (VTX-2337) is a drug which acts as a potent and selective agonist of toll-like receptor 8 (TLR8), a receptor involved in the regulation of the immune system. It is used to stimulate the immune system, and has potential application as an adjuvant therapy in cancer chemotherapy, although clinical trials have shown only modest benefits. It also worsens neuropathic pain in animal models and has been used to research the potential of targeting TLR8 in some kinds of chronic pain syndromes. See also * Imiquimod * Vesatolimod Vesatolimod (GS-9620) is an antiviral drug developed by Gilead Sciences, which acts as a potent and selective agonist of Toll-like receptor 7 (TLR7), a receptor involved in the regulation of the immune system. It is used to stimulate the immune ... References Nitrogen heterocycles Amides Amines {{antineoplastic-drug-stub ...
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