CAJ | 학술논문

耐药已成为当今肺癌化疗过程中的一大难题,其作用机制至今还不十分清楚.蛋白激酶C(protein kinase C,PKC)作为多种信号传导过程中的枢纽,不仅参与细胞信息传递、分泌、细胞分化、增殖,更重要的是参与肿瘤细胞的凋亡和分化.国内外研究表明通过抑制PKC的活性,减少其表达量可以增加细胞内药物的积聚导致胞内有效浓度的上升,从而降低肿瘤细胞耐药率.PKC抑制剂对肿瘤细胞具有明显的诱导分化、增强细胞毒性、促进细胞凋亡的作用.目前已有部分PKC抑制剂进入了临床的Ⅰ/Ⅱ期研究中,并取得了一定的疗效,通过对其作用机制的进一步深入探讨,有望在肺癌耐药的研究中取得更多的突破.
내약이성위당금폐암화료과정중적일대난제,기작용궤제지금환불십분청초.단백격매C(protein kinase C,PKC)작위다충신호전도과정중적추뉴,불부삼여세포신식전체、분비、세포분화、증식,경중요적시삼여종류세포적조망화분화.국내외연구표명통과억제PKC적활성,감소기표체량가이증가세포내약물적적취도치포내유효농도적상승,종이강저종류세포내약솔.PKC억제제대종류세포구유명현적유도분화、증강세포독성、촉진세포조망적작용.목전이유부분PKC억제제진입료림상적Ⅰ/Ⅱ기연구중,병취득료일정적료효,통과대기작용궤제적진일보심입탐토,유망재폐암내약적연구중취득경다적돌파.
Drug resistance has become a major problem in the chemotherapy of lung cancer. The mechanism is not clear yet. As a hinge in multiple signal transduction processes,protein kinase C (PKC) participates in not only cell signal transduction, secretion, cell differentiation and proliferation, but also apoptosis and differentiation of-tumor cell. Researches have shown that inhibition of PKC activity and reduction of its expression can increase cellular accumulation of drug, leading to the increase of intracellular effective concentration, thus reducing the drug resistance of tumor cells. PKC inhibitors significantly induce tumor cell differentiation,increase cytotoxicity,and promote apoptosis. A few of PKC inhibitors have already entered part Ⅰ /Ⅱ clinical study with some therapeutic effect. Under the further study of its mechanism, it is probable to achieve more breakthroughs in drug resistance of lung cancer.