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.[1][2][3][4][5]
^Zhang S, Hu Z, Tanji H, Jiang S, Das N, Li J, et al. (January 2018). "Small-molecule inhibition of TLR8 through stabilization of its resting state". Nature Chemical Biology. 14 (1): 58–64. doi:10.1038/nchembio.2518. PMC5726935. PMID 29155428.
^Yang J, Lan J, Du H, Zhang X, Li A, Zhang X, et al. (March 2019). "Icariside II induces cell cycle arrest and differentiation via TLR8/MyD88/p38 pathway in acute myeloid leukemia cells". European Journal of Pharmacology. 846: 12–22. doi:10.1016/j.ejphar.2018.12.026. PMID 30579933. S2CID 58567568.
^Venegas FA, Köllisch G, Mark K, Diederich WE, Kaufmann A, Bauer S, et al. (September 2019). "The Bacterial Product Violacein Exerts an Immunostimulatory Effect Via TLR8". Scientific Reports. 9 (1): 13661. Bibcode:2019NatSR...913661V. doi:10.1038/s41598-019-50038-x. PMC6754391. PMID 31541142.
^Ehrnström B, Kojen JF, Giambelluca M, Ryan L, Moen SH, Hu Z, et al. (April 2020). "TLR8 and complement C5 induce cytokine release and thrombin activation in human whole blood challenged with Gram-positive bacteria". Journal of Leukocyte Biology. 107 (4): 673–683. doi:10.1002/JLB.3A0120-114R. PMID 32083344.
This pharmacology-related article is a stub. You can help Wikipedia by expanding it.
cpt9a, drug, which, acts, potent, selective, antagonist, toll, like, receptor, tlr8, with, ic50, activation, toll, like, receptors, triggers, release, cytokines, other, signalling, factors, leading, inflammation, this, essential, part, immune, system, response. 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 1 2 3 4 5 CU CPT9aIdentifiersIUPAC name 4 7 methoxyquinolin 4 yl 2 methylphenolCAS Number2165340 32 7PubChem CID135567383ChemSpider65323639Chemical and physical dataFormulaC 17H 15N O 2Molar mass265 312 g mol 13D model JSmol Interactive imageSMILES CC1 C C CC C1 C2 C3C CC CC3 NC C2 OC OInChI InChI 1S C17H15NO2 c1 11 9 12 3 6 17 11 19 14 7 8 18 16 10 13 20 2 4 5 15 14 16 h3 10 19H 1 2H3Key HNYBTVKYLVLWCB UHFFFAOYSA NSee also editCU CPT4a Imiquimod MotolimodReferences edit Zhang S Hu Z Tanji H Jiang S Das N Li J et al January 2018 Small molecule inhibition of TLR8 through stabilization of its resting state Nature Chemical Biology 14 1 58 64 doi 10 1038 nchembio 2518 PMC 5726935 PMID 29155428 Hu Z Tanji H Jiang S Zhang S Koo K Chan J et al October 2018 Small Molecule TLR8 Antagonists via Structure Based Rational Design Cell Chemical Biology 25 10 1286 1291 e3 doi 10 1016 j chembiol 2018 07 004 PMC 6195466 PMID 30100350 Yang J Lan J Du H Zhang X Li A Zhang X et al March 2019 Icariside II induces cell cycle arrest and differentiation via TLR8 MyD88 p38 pathway in acute myeloid leukemia cells European Journal of Pharmacology 846 12 22 doi 10 1016 j ejphar 2018 12 026 PMID 30579933 S2CID 58567568 Venegas FA Kollisch G Mark K Diederich WE Kaufmann A Bauer S et al September 2019 The Bacterial Product Violacein Exerts an Immunostimulatory Effect Via TLR8 Scientific Reports 9 1 13661 Bibcode 2019NatSR 913661V doi 10 1038 s41598 019 50038 x PMC 6754391 PMID 31541142 Ehrnstrom B Kojen JF Giambelluca M Ryan L Moen SH Hu Z et al April 2020 TLR8 and complement C5 induce cytokine release and thrombin activation in human whole blood challenged with Gram positive bacteria Journal of Leukocyte Biology 107 4 673 683 doi 10 1002 JLB 3A0120 114R PMID 32083344 nbsp This pharmacology related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title CU CPT9a amp oldid 1149049712, wikipedia, wiki, book, books, library,
