Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR, PR China.
Expert Opin Ther Pat. 2022 Apr;32(4):441-453. doi: 10.1080/13543776.2022.2027912. Epub 2022 Jan 20.
One of the most distinctive hallmarks of cancer cells is increased glucose consumption for aerobic glycolysis, which is called the Warburg effect. In recent decades, extensive research has been carried out to exploit this famous phenomenon, trying to detect promising targetable vulnerabilities in altered metabolism to fight cancer. Targeting aberrant glucose metabolism can perturb cancer malignant proliferation and even induce programmed cell death.
This review covered the recent patents which focused on targeting key glycolytic enzymes, including hexokinase, pyruvate dehydrogenase kinases, and lactate dehydrogenase for cancer treatment.
Compared with the conventional cancer treatment, specifically targeting the well-known Achilles heel, the Warburg effect has attracted considerable attention. Although there is still no single glycolytic agent for clinical cancer treatment, the combination of glycolytic inhibitor with conventional anticancer drugs or the combined use of multiple glycolytic inhibitors are being investigated extensively in recent years, which could emerge as attractive anticancer strategies.
癌细胞的一个最显著特征是有氧糖酵解过程中葡萄糖摄取量增加,即瓦博格效应。近几十年来,人们开展了广泛的研究来利用这一著名现象,试图在改变的代谢中寻找有前途的可靶向的脆弱性来对抗癌症。靶向异常葡萄糖代谢可以扰乱癌症的恶性增殖,甚至诱导程序性细胞死亡。
本文综述了最近的专利,这些专利主要集中在靶向关键糖酵解酶,包括己糖激酶、丙酮酸脱氢酶激酶和乳酸脱氢酶,用于癌症治疗。
与传统的癌症治疗相比,专门针对众所周知的阿喀琉斯之踵——瓦博格效应,引起了相当大的关注。尽管目前还没有单一的糖酵解抑制剂用于临床癌症治疗,但近年来,人们广泛研究了糖酵解抑制剂与传统抗癌药物的联合应用,或联合使用多种糖酵解抑制剂,这可能成为有吸引力的抗癌策略。