Department of Biochemistry, Boston University School of Medicine, MA 02118, USA.
Future Oncol. 2010 Mar;6(3):457-70. doi: 10.2217/fon.09.174.
AMPK is an evolutionarily conserved fuel-sensing enzyme that is activated in shortage of energy and suppressed in its surfeit. AMPK activation stimulates fatty acid oxidation, enhances insulin sensitivity, alleviates hyperglycemia and hyperlipidemia, and inhibits proinflammatory changes. Thus, AMPK is a well-received therapeutic target for metabolic syndrome and Type 2 diabetes. Recent studies indicate that AMPK plays a role in linking metabolic syndrome and cancer. AMPK is an essential mediator of the tumor suppressor LKB1 and could be suppressed in cancer cells containing loss-of-function mutations of LKB1 or containing active mutations of B-Raf, or in cancers associated with metabolic syndrome. The activation of AMPK reprograms cellular metabolism and enforces metabolic checkpoints by acting on mTORC1, p53, fatty acid synthase and other molecules for regulating cell growth and metabolism. In keeping with in vitro studies, recent epidemiological studies indicate that the incidence of cancer is reduced in Type 2 diabetes treated with metformin, an AMPK activator. Thus, AMPK is emerging as an interesting metabolic tumor suppressor and a promising target for cancer prevention and therapy.
AMPK 是一种进化上保守的燃料感应酶,在能量短缺时被激活,在过剩时被抑制。AMPK 的激活刺激脂肪酸氧化,增强胰岛素敏感性,减轻高血糖和高血脂,并抑制促炎变化。因此,AMPK 是代谢综合征和 2 型糖尿病的一个备受欢迎的治疗靶点。最近的研究表明,AMPK 在代谢综合征和癌症之间起着联系作用。AMPK 是肿瘤抑制因子 LKB1 的重要介质,并且在含有 LKB1 功能丧失突变或含有 B-Raf 活性突变的癌细胞中,或者在与代谢综合征相关的癌症中,AMPK 可能被抑制。AMPK 的激活通过作用于 mTORC1、p53、脂肪酸合酶和其他调节细胞生长和代谢的分子,重新编程细胞代谢并强制代谢检查点。与体外研究一致,最近的流行病学研究表明,二甲双胍治疗 2 型糖尿病可降低癌症的发病率,二甲双胍是一种 AMPK 激活剂。因此,AMPK 作为一种有趣的代谢肿瘤抑制因子和癌症预防和治疗的有前途的靶点正在出现。