Background

Thalidomide yakatangwa sedative drug, immunomodulatory agent uye inoferefetwa pakurapa zviratidzo zvekenza dzakawanda. Thalidomide inhibits an E3 ubiquitin ligase.,inova CRBN-DDB1-Cul4A yakaoma.

Tsanangudzo

Thalidomide inotanga kusimudzirwa sedative, inhibits cereblon (CRBN), chikamu che cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ine Kd ye∼250 nM, uye ine immunomodulatory, anti-inflammatory uye anti-angiogenic cancer zvivakwa.

In Vitro

Thalidomide inotanga kusimudzirwa sedative, ine immunomodulatory, anti-inflammatory uye anti-angiogenic cancer properties, uye inotarisira cereblon (CRBN), chikamu che cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ine Kd ye∼250 nM[1]. Thalidomide (50μg/mL) inogona kuita basa rekurwisa bundu reicotinib rinopesana nekupararira kwesero PC9 neA549 masero, uye izvi zvinokonzeresa neapoptosis uye kutama kwesero. Mukuwedzera, Thalidomide uye icotinib inhibits EGFR uye VEGF-R2 nzira muPC9 masero [3].

Thalidomide (100 mg/kg, po) inhibits the collagen deposition, pasi-inoronga mRNA yekutaura level yeα-SMA uye collagen I, uye zvakanyanya kuderedza pro-inflammatory cytokines muRILF mice. Thalidomide inoderedza RILF kuburikidza nekudzvinyirira kweROS uye pasi-mutemo weTGF-β/Smad nzira inotsamira paNrf2 chimiro[2]. Thalidomide (200 mg/kg, po) yakasanganiswa neicotinib inoratidza synergistic anti-bundu mhedzisiro mumasikirwo emakonzo ane PC9 maseru, kudzvanyirira bundu kukura uye kukurudzira kufa kwebundu[3].