Resatorvid

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Resatorvid
Resatorvid structure.png
Clinical data
Trade namesResatorvid
Legal status
Legal status
Identifiers
  • ethyl (6R)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H17ClFNO4S
Molar mass361.8 g·mol−1
3D model (JSmol)
  • CCOC(=O)C1=CCCC[C@H]1S(=O)(=O)NC2=C(C=C(C=C2)F)Cl
  • InChI=1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1
  • Key:LEEIJTHMHDMWLJ-CQSZACIVSA-N

Resatorvid (TAK-242) is a drug which acts as a selective antagonist of the receptor TLR4.[1] It has antiinflammatory[2] and neuroprotective effects following brain injury,[3] and also shows activity against some forms of skin cancer and some other cancers, and may show potential as an add-on treatment alongside conventional chemotherapy drugs.[4][5][6]

See also[edit]

References[edit]

  1. ^ Matsunaga N, Tsuchimori N, Matsumoto T, Ii M (January 2011). "TAK-242 (resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling, binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules". Molecular Pharmacology. 79 (1): 34–41. doi:10.1124/mol.110.068064. PMID 20881006. S2CID 7818996.
  2. ^ Samarpita S, Kim JY, Rasool MK, Kim KS (January 2020). "Investigation of toll-like receptor (TLR) 4 inhibitor TAK-242 as a new potential anti-rheumatoid arthritis drug". Arthritis Research & Therapy. 22 (1): 16. doi:10.1186/s13075-020-2097-2. PMC 6979396. PMID 31973752.
  3. ^ Feng Y, Gao J, Cui Y, Li M, Li R, Cui C, Cui J (January 2017). "Neuroprotective Effects of Resatorvid Against Traumatic Brain Injury in Rat: Involvement of Neuronal Autophagy and TLR4 Signaling Pathway". Cellular and Molecular Neurobiology. 37 (1): 155–168. doi:10.1007/s10571-016-0356-1. PMID 26961544. S2CID 21583205.
  4. ^ Dickinson SE, Wondrak GT (2019). "TLR4-directed Molecular Strategies Targeting Skin Photodamage and Carcinogenesis". Current Medicinal Chemistry. 25 (40): 5487–5502. doi:10.2174/0929867324666170828125328. PMID 28847267.
  5. ^ Kashani B, Zandi Z, Karimzadeh MR, Bashash D, Nasrollahzadeh A, Ghaffari SH (December 2019). "Blockade of TLR4 using TAK-242 (resatorvid) enhances anti-cancer effects of chemotherapeutic agents: a novel synergistic approach for breast and ovarian cancers". Immunologic Research. 67 (6): 505–516. doi:10.1007/s12026-019-09113-8. PMID 32026322.
  6. ^ Zandi Z, Kashani B, Bashash D, Poursani EM, Mousavi SA, Chahardoli B, Ghaffari SH (February 2020). "The anticancer effect of the TLR4 inhibition using TAK-242 (resatorvid) either as a single agent or in combination with chemotherapy: A novel therapeutic potential for breast cancer". Journal of Cellular Biochemistry. 121 (2): 1623–1634. doi:10.1002/jcb.29397. PMID 31535397. S2CID 202689986.