Ingemuva

I-Thalidomide yethulwa njengesidakamizwa esilalisa umzimba, i-immunomodulatory agent futhi iyaphenywa ukwelapha izimpawu zemidladla eminingi.I-Thalidomide ivimbela i-E3 ubiquitin ligase.,okuyinkimbinkimbi ye-CRBN-DDB1-Cul4A.

Incazelo

I-Thalidomide iqala ukukhuthazwa njenge-sedative, inhibits cereblon (CRBN), ingxenye ye-cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ene-Kd∼250 nM, futhi inomdlavuza we-immunomodulatory, anti-inflammatory kanye ne-anti-angiogenic cancer.

Ku-Vitro

I-Thalidomide iqala ukukhuthazwa njenge-sedative, ine-immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, futhi ihlose i-cereblon (CRBN), ingxenye ye-cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ene-Kd∼250 nM[1].I-Thalidomide (50μg/mL) inika amandla umsebenzi wokulwa nesimila we-icotinib ngokumelene nokwanda kwawo womabili amaseli e-PC9 kanye ne-A549, futhi lo mphumela uhlotshaniswa ne-apoptosis nokufuduka kwamaseli.Ngaphezu kwalokho, i-Thalidomide ne-icotinib ivimbela izindlela ze-EGFR kanye ne-VEGF-R2 kumaseli e-PC9[3].

I-Thalidomide (100 mg/kg, po) ivimbela ukwakheka kwe-collagen, iqondise phansi izinga lokuvezwa kwe-mRNAα-I-SMA ne-collagen I, futhi inciphisa kakhulu ama-cytokines ane-pro-inflammatory kumagundane e-RILF.I-Thalidomide inciphisa i-RILF ngokucindezelwa kwe-ROS kanye nokulawulwa phansi kwe-TGF-β/Indlela ye-Smad incike esimweni se-Nrf2[2].I-Thalidomide (200 mg/kg, po) ihlanganiswe ne-icotinib ikhombisa imiphumela yokulwa nesimila kumagundane anqunu anamaseli e-PC9, icindezela ukukhula kwesimila kanye nokukhuthaza ukufa kwesimila[3].