LS102是一种选择性的E3连接酶synoviolin(Syvn1)抑制剂。LS-102抑制Syvn1自泛素化，IC50约为35μM，有研究类风湿关节炎的潜力。
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment[1][2].
LS-102 inhibits proliferation of RSCs with an IC50 of 5.4 µM[1].LS-102 suppresses proliferation of rheumatoid synovial cells (RSCs) in a Syvn1-dependent manner. LS-102 suppresses polyubiquitination of target proteins of Syvn1, including nuclear factor erythroid 2-related factor 2 (NRF2), V247M α-sarcoglycan mutant, and PGC-1β. LS-102 inhibits E3 ligase activity of Synoviolin (Syvn1)[2]. Cell Viability Assay[1] Cell Line: Rheumatoid synovial cells (RSCs)
LS-102 (1.3-4 mg/kg; i.p.; daily for 4 weeks) reduces clinical severity scores in a CIA model[1]. Animal Model: 7-week-old DBA/1 male mice (CIA model)[1]
[1]. Yagishita N, et al. RING-finger type E3 ubiquitin ligase inhibitors as novel candidates for the treatment of rheumatoidarthritis. Int J Mol Med. 2012 Dec;30(6):1281-6. [2]. Fujita H, et al. Identification of the inhibitory activity of walnut extract on the E3 ligase Syvn1. Mol Med Rep. 2018 Dec;18(6):5701-5708.
动态评分
0.0