Resatorvid
 | |
| Clinical data | |
|---|---|
| Trade names | Resatorvid |
| Identifiers | |
| |
JSmol) | |
| |
| |
Resatorvid (TAK-242) is a
inhibitors of the receptor TLR4.[1] It binds directly to cysteine residue 747[1] intracellularly, preventing TLR4 binding with TIRAP and thus preventing downstream signal transduction.[2]
A randomized, double-blinded
tool compound in biological research.[1]
It has
neuroprotective effects in preclinical models.[3] It has been explored in preclinical studies of several forms of cancer, including multiple myeloma, breast cancer, and ovarian cancer,[4] and has been suggested for study in skin cancers.[5]
Efforts have been made to improve resatorvid by making
prodrugs and deuterated derivatives.[3]
See also
References
Further reading
- 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. S2CID 7818996.
- 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. 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. S2CID 21583205.
- Dickinson SE, Wondrak GT (2019). "TLR4-directed Molecular Strategies Targeting Skin Photodamage and Carcinogenesis". Current Medicinal Chemistry. 25 (40): 5487–5502. S2CID 670318.
- 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. S2CID 211048929.
- 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. S2CID 202689986.</ref>