Jennings Lee D, Foreman Kenneth W, Rush Thomas S, Tsao Desiree H H, Mosyak Lidia, Kincaid Scott L, Sukhdeo Mohani N, Sutherland Alan G, Ding Weidong, Kenny Cynthia Hess, Sabus Chantel L, Liu Hanlan, Dushin Elizabeth G, Moghazeh Soraya L, Labthavikul Pornpen, Petersen Peter J, Tuckman Margareta, Haney Steven A, Ruzin Alexey V
Wyeth Research, Department of Medicinal Chemistry, 401 N. Middletown Road, Pearl River, NY 10965, USA.
Bioorg Med Chem. 2004 Oct 1;12(19):5115-31. doi: 10.1016/j.bmc.2004.07.031.
The ZipA-FtsZ protein-protein interaction is a potential target for antibacterial therapy. The design and parallel synthesis of a combinatorial library of small molecules, which target the FtsZ binding area on ZipA are described. Compounds were demonstrated to bind to the FtsZ binding domain of ZipA by HSQC NMR and to inhibit cell division in a cell elongation assay.
ZipA与FtsZ的蛋白质-蛋白质相互作用是抗菌治疗的一个潜在靶点。本文描述了针对ZipA上FtsZ结合区域的小分子组合文库的设计与平行合成。通过HSQC核磁共振证实化合物能与ZipA的FtsZ结合结构域结合,并在细胞伸长试验中抑制细胞分裂。