Capture compounds, collections thereof and methods for analyzing the proteome and complex compositions
申请人:Kõster Hubert
公开号:US20100248264A1
公开(公告)日:2010-09-30
Capture compounds and collections thereof and methods using the compounds for the analysis of biomolecules are provided. In particular, collections, compounds and methods are provided for analyzing complex protein mixtures, such as the proteome. The compounds are multifunctional reagents that provide for the separation and isolation of complex protein mixtures. Automated systems for performing the methods also are provided.
whether the observed in‐vivo effects can be traced back to their modulation. Furthermore, the metabolic fate of arylazoamidoximes 3 was addressed by investigation of a possible N‐reductive biotransformation. In summary, novel NO‐modulating compound classes are presented, among which arylazoamidoximes 3 are potent activators of NOS isoforms, and arylazoamidines 2 exert in‐vivo effects by unknown mechanisms
已经合成了三个脒基芳基肼 1、三个芳基偶氮脒 2 和九个芳基偶氮酰胺肟 3,并研究了它们作为一氧化氮 (NO) 调节剂的潜力。体外研究表明,2 和 3 抑制血小板聚集(2c,IC50 = 3 μM),这也可以通过抑制小动脉血栓形成在体内显示(3a,22%)。此外,所有化合物的抗高血压作用都在 SHR 大鼠身上进行了体内检测,其中 2a 是最有效的候选物,可将血压降低 19%。然而,没有显示出共同的潜在作用机制。其中一些化合物以非酶促方式释放 HNO。与 NO 合酶同种型 (NOS) 的孵育显示,化合物 1 至 3 是 NOS 的弱底物,但芳基偶氮酰胺肟 3 在 L-精氨酸存在下显着提高了 NOS 活性(3 小时,高达五倍)。此外,我们检查了对精氨酸酶和二甲基精氨酸二甲氨基水解酶(DDAH)的影响,这两种酶参与了 NO 生物合成的复杂调控,以阐明观察到的体内效应是否可以追溯到它们的调节。此外,芳基唑胺肟