College of Chemistry and Molecular Sciences, Wuhan University, Wuhan, PR China.
Org Lett. 2011 Jun 3;13(11):2924-7. doi: 10.1021/ol2009544. Epub 2011 May 5.
2-Difluoromethylene-4-methylenepentanoic acid (DFMPA), a seemingly deviated analog of 2-oxoglutaric acid (2-OG), could surprisingly mimic its signaling function in cyanobacteria. Computer modeling revealed the favorable binding of DFMPA toward the 2-OG receptor, NtcA, via mutual conformational changes, suggesting that structural alteration of 2-OG is tolerated for it to exercise its signaling role. This extremely useful finding could be exploited for the design of affinity probes with which to study new 2-OG receptors in related signaling pathways.
2-二氟亚甲基-4-亚甲基戊二酸(DFMPA)是 2-氧代戊二酸(2-OG)的一种看似偏离的类似物,却能在蓝藻中出人意料地模拟其信号功能。计算机建模显示,DFMPA 通过相互构象变化,与 2-OG 受体 NtcA 具有良好的结合能力,表明 2-OG 的结构改变可以容忍其发挥信号作用。这一极其有用的发现可用于设计亲和探针,以研究相关信号通路中的新型 2-OG 受体。