谷氨酰胺酶新型抑制剂及其抗肿瘤活性研究进展

廖英; 冀林华; 崔森

doi:10.3969/j.issn.1000-8179.2019.07.273

谷氨酰胺酶新型抑制剂及其抗肿瘤活性研究进展

doi: 10.3969/j.issn.1000-8179.2019.07.273

青海大学附属医院血液内科（青海省西宁市810000）

基金项目:

国家人力资源社会保障部2017年度高层次留学人才回国项目 2017-200

详细信息

作者简介:
廖英专业方向为血液病诊断与治疗。E-mail：543396578@qq.com

通讯作者:
崔森 13897284366@163.com

计量
- 文章访问数: 73
- HTML全文浏览量: 167
- PDF下载量: 12
- 被引次数: 0
出版历程
- 收稿日期: 2019-03-18
- 修回日期: 2019-04-18
- 刊出日期: 2019-04-15

Research progress on the novel glutaminase inhibitor and its antitumor activity

Department of Hematology, Qinghai University Affiliated Hospital, Xilin 810000, China

Funds:

the Ministry of Human Resources and Social Security for High-level Overseas Talents to Return to China in 2017 2017-200

More Information

Corresponding author: Sen Cui; E-mail:13897284366@163.com

摘要

摘要: 肿瘤细胞利用各种代谢途径以满足增殖的能量和生物合成需求。除葡萄糖外，谷氨酰胺也是肿瘤细胞生长的重要前体物质及能量来源。谷氨酰胺酶（glutaminase，GSL）活性与Ras、c-Myc等癌基因以及Rho GTP酶相关。诸多临床前研究已证实谷氨酰胺酶抑制剂不仅具有抗肿瘤活性，还可以明显增强耐药肿瘤细胞对靶向药物的敏感性。目前新型GSL抑制剂CB-839已进入Ⅰ期临床试验，有望成为癌症治疗的新型药物。本文就谷氨酰胺代谢及其新型抑制剂抗肿瘤研究进展做一综述。
- 谷氨酰胺代谢 /
- 谷氨酰胺酶 /
- 肿瘤 /
- 谷氨酰胺酶抑制剂 /
- CB-839
Abstract: Tumor cells use several metabolic pathways to support bioenergetic and biosynthetic demands of proliferation. In addition to glucose, glutamine is an important source of precursor substances and energy for cancer cell growth. Glutaminase (GSL) activity is associated with Ras, c-Myc, and other oncogenes, as well as Rho GTP enzyme. Many preclinical studies have confirmed that glutaminase inhibitors not only exhibit anti-tumor activity, but can also remarkably enhance the sensitivity of resistant cancer cells to targeted drugs. At present, the novel GSL inhibitor CB-839 has entered phase Ⅰ clinical trials and is expected to become a new drug for cancer treatment. This paper reviews the research progress on this novel glutaminase inhibitor and its antitumor activity.
- glutamine metabolism /
- glutaminase /
- tumor /
- glutaminase inhibitor /
- CB-839

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参考文献(32)

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