Structural Analysis of ATP Analogues Compatible with Kinase-Catalyzed Labeling
作者:Sujit Suwal、Chamara Senevirathne、Satish Garre、Mary Kay H. Pflum
DOI:10.1021/bc300404s
日期:2012.12.19
Kinase-catalyzed protein phosphorylation is an important biochemical process involved in cellular functions. We recently discovered that kinases promiscuously accept γ-modified ATPanalogues as cosubstrates and used several ATPanalogues as tools for studying protein phosphorylation. Herein, we explore the structural requirements of γ-modified ATPanalogues for kinase compatibility. To understand the
激酶催化的蛋白质磷酸化是涉及细胞功能的重要生化过程。我们最近发现激酶混杂地接受 γ 修饰的 ATP 类似物作为共底物,并使用几种 ATP 类似物作为研究蛋白质磷酸化的工具。在此,我们探索了 γ 修饰的 ATP 类似物对激酶相容性的结构要求。为了了解接头长度和组成的影响,合成了一系列 ATP 类似物,并通过定量质谱法确定激酶催化标记的效率。这项关于影响激酶共底物混杂的因素的研究将使设计用于各种激酶催化标记反应的 ATP 类似物成为可能。
Mono-acylation of symmetric diamines in the presence of water
作者:Wei Tang、Shiyue Fang
DOI:10.1016/j.tetlet.2008.07.174
日期:2008.10
Simply reacting equal equivalents of symmetricdiamines with esters or carbonates in the presence of a suitable amount of water gave mono-acylated products in good to quantitative yields.
在适量的水存在下,简单地将等当量的对称二胺与酯或碳酸酯反应,即可得到定量产率良好的单酰化产物。
Treatment for diabetes and obesity as well as method of screening compounds useful for such treatments
申请人:Chang Young-Tae
公开号:US20060293325A1
公开(公告)日:2006-12-28
The present invention relates to a compound having the formula
where Z is an amine, alcohol, or thiol-containing group, and Y is an alkyl-containing amine. Methods of producing such compounds and using them to treat patients with diabetes and obesity are also disclosed. The present invention also relates to treating such conditions with GADPH inhibitors and screening compounds useful for treating such conditions by using GADPH inhibitors. Compounds can also be screened for their effectiveness in modulating diabetes and obesity with a
C. elegans
strain.
METHODS OF LOWERING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
申请人:Catabasis Pharmacauticals, Iinc.
公开号:US20150344430A1
公开(公告)日:2015-12-03
The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
Synthesis and biological evaluation of novel 1,3,5-triazine derivatives as antimicrobial agents
作者:Chunhui Zhou、Jaeki Min、Zhigang Liu、Anne Young、Heather Deshazer、Tian Gao、Young-Tae Chang、Neville R. Kallenbach
DOI:10.1016/j.bmcl.2008.01.031
日期:2008.2
Numerous studies have contributed to the development of natural and synthetic antimicrobial peptides as a prospective source of antibiotic agents. Based on the concept that cationic charge, bulk, and lipophilicity are major factors determining antibacterial activity in these peptides, we designed and screened several combinatorial libraries based on 1,3,5-triazine as a template. A set of compounds were identified to show potent antimicrobial activity together with low hemolytic activity. (c) 2008 Elsevier Ltd. All rights reserved.