Resatorvid
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]
![]() | |
Clinical data | |
---|---|
Trade names | Resatorvid |
Legal status | |
Legal status | |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
DrugBank | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C15H17ClFNO4S |
Molar mass | 361.8 g·mol−1 |
3D model (JSmol) | |
| |
|
References
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.