Amavu n'amavuko

Thalidomide yatangijwe nk'umuti utera imbaraga, imiti ikingira kandi ikanakorerwa iperereza ku kuvura ibimenyetso bya kanseri nyinshi. Talidomide ibuza E3 ubiquitin ligase，akaba ari CRBN-DDB1-Cul4A.

Ibisobanuro

Thalidomide yabanje kuzamurwa nkumuti, ibuza cereblon (CRBN), igice cya cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, hamwe na Kd ya∼250 nM, kandi ifite immunomodulatory, anti-inflammatory na anti-angiogenic kanseri.

Muri Vitro

Thalidomide yabanje kuzamurwa nkigishitsi, ifite immunomodulatory, anti-inflammatory na anti-angiogenic kanseri, kandi yibasira cereblon (CRBN), igice cya cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, hamwe na Kd ya∼250 nM [1].Thalidomide (50)μg / mL) yongerera imbaraga ibikorwa byo kurwanya ibibyimba bya icotinib kurwanya ikwirakwizwa rya selile zombi PC9 na A549, kandi iyi ngaruka ifitanye isano na apoptose no kwimuka kwakagari.Mubyongeyeho, Thalidomide na icotinib bibuza inzira ya EGFR na VEGF-R2 muri selile PC9 [3].

Thalidomide (100 mg / kg, po) ibuza kolagen kubika, munsi-igenga imvugo ya mRNA yaα-SMA na kolagen I, kandi bigabanya cyane cytokine itera inflammatory mu mbeba za RILF.Thalidomide igabanya RILF ikoresheje guhagarika ROS no kumanura-TGF-β/ Inzira ya Smad iterwa na Nrf2 imiterere [2].Thalidomide (200 mg / kg, po) ifatanije na icotinib yerekana ingaruka ziterwa no kurwanya ibibyimba mu mbeba zambaye ubusa zifite selile PC9, guhagarika ikibyimba no guteza urupfu rwibibyimba [3].