Amavu n'amavuko

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

Ibisobanuro

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

Muri Vitro

Thalidomide yabanje kuzamurwa mu rwego rwo kwikinisha, ifite immunomodulatory, anti-inflammatory na anti-angiogenic, 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) itanga imbaraga zo kurwanya ibibyimba bya icotinib kurwanya ikwirakwizwa rya selile zombi PC9 na A549, kandi iyi ngaruka ifitanye isano na apoptose no kwimuka kwakagari. Byongeye kandi, Thalidomide na icotinib bibuza inzira ya EGFR na VEGF-R2 muri selile PC9 [3].

Thalidomide (100 mg / kg, po) ibuza koleji ya kolagen, munsi-igenga imvugo ya mRNA yaα-SMA na kolagen I, kandi bigabanya cyane cytokine itera inflammatory imbeba za RILF. Thalidomide igabanya RILF ikoresheje guhagarika ROS no kumanura-TGF-β/ Inzira mbi 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 rw'ibibyimba [3].