从天然产物PHGDH抑制剂研究的见解

Zhaodan Wang, Xueqin Chen, Qingxiang Sun
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引用次数: 0

摘要

丝氨酸的合成活性在几种癌症中显著上调[1]。智人3-磷酸甘油酸脱氢酶(PHGDH)催化丝氨酸合成的限速步骤,将3-磷酸甘油酸(3PG)和NAD+转化为3-磷酸羟基丙酮酸和NADH[2,3]。最近,PHGDH抑制剂被广泛用于治疗受影响的癌症[4,5]。在所鉴定的抑制剂中,azacoccone E[6]、ixocarpalactone A[7]、withaferin A和oriidonin[8]三种天然产物均能有效抑制PHGDH酶活性和癌细胞生长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Insights from Natural Product PHGDH Inhibitor Studies
The synthetic activity of serine is significantly upregulated in several cancers [1]. Homo sapiens 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the rate-limiting step of serine synthesis, which converts 3-phosphoglycerate (3PG) and NAD+ to 3-phosphohydroxypyruvate and NADH [2,3]. PHGDH inhibitors were extensively pursued recently for their use in the treatment of affected cancers [4,5]. Among the inhibitors identified, three natural products including azacoccone E [6], ixocarpalactone A [7], withaferin A and oridonin [8] were shown to effectively inhibit PHGDH enzyme activity and cancer cell growth.
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