Monovich Lauren, Mugrage Benjamin, Quadros Elizabeth, Toscano Karen, Tommasi Ruben, LaVoie Stacey, Liu Eugene, Du Zhengming, LaSala Daniel, Boyar William, Steed Paul
Novartis Institutes for BioMedical Research, 100 Technology Square, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett. 2007 Apr 15;17(8):2310-1. doi: 10.1016/j.bmcl.2007.01.059. Epub 2007 Jan 25.
Halopemide, which was identified by HTS to inhibit phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-carboxylic acids with superior potency versus PLD2.
通过高通量筛选（HTS）鉴定出的卤培米德可抑制磷脂酶D2（PLD2），这为探索性研究提供了基础，旨在鉴定用作炎症介质的PLD2强效抑制剂。利用平行合成和纯化技术快速鉴定出源自吲哚-2-羧酸的口服可用酰胺类似物，其对PLD2的效力更强。
