ndabere

Ewebata Thalidomide dị ka ọgwụ na-eme ka ahụ sie ike, onye na-ahụ maka immunomodulatory ma na-enyocha ya maka ọgwụgwọ mgbaàmà nke ọtụtụ ọrịa cancer. Thalidomide na-egbochi E3 ubiquitin ligase.,nke bụ CRBN-DDB1-Cul4A mgbagwoju.

Nkọwa

A na-akwalite Thalidomide na mbụ dị ka ihe na-eme ka ahụ sie ike, na-egbochi cereblon (CRBN), akụkụ nke cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, na Kd nke∼250 nM, ma nwee immunomodulatory, mgbochi mkpali na mgbochi ọrịa cancer angiogenic.

Na Vitro

A na-akwalite Thalidomide na mbụ dị ka ihe na-eme ka ahụ sie ike, nwere immunomodulatory, mgbochi mkpali na mgbochi ọrịa cancer angiogenic, yana lekwasịrị anya cereblon (CRBN), akụkụ nke cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, na Kd nke∼250 nM[1]. Thalidomide (50μg / mL) na-eme ka ọrụ mgbochi tumor nke icotinib na-eme ka mmụba nke ma PC9 na A549 sel, na mmetụta a na-ejikọta na apoptosis na cell migration. Na mgbakwunye, Thalidomide na icotinib na-egbochi ụzọ EGFR na VEGF-R2 na sel PC9 [3].

Thalidomide (100 mg/kg, po) na-egbochi ntinye nke collagen, na-achịkwa ọkwa mRNA nke okwu.α-SMA na collagen I, ma na-ebelata nke ọma cytokines pro-inflammatory na ụmụ oke RILF. Thalidomide na-ebelata RILF site na nkwụsị nke ROS na nhazi ala nke TGF-β/ Ụzọ Smad dabere na ọnọdụ Nrf2 [2]. Thalidomide (200 mg / kg, po) jikọtara ya na icotinib na-egosi mmetụta mgbochi tumor synergistic na ụmụ oke ndị na-ebu sel PC9, na-egbochi uto tumor na ịkwalite ọnwụ tumor[3].