Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
Bioorg Med Chem Lett. 2012 Dec 15;22(24):7715-8. doi: 10.1016/j.bmcl.2012.09.086. Epub 2012 Oct 3.
Cysteine cathepsins play an important role in many (patho)physiological conditions. Among them, cathepsins L, S, K and B are subjects of several drug discovery programs. Besides their role as drug targets, cysteine cathepsins are additionally considered to be possible biomarkers for inflammation and cancer. Herein, we describe the design, synthesis, biological evaluation and spectral properties of fluorescently labeled dipeptide- and azadipeptide nitriles.
半胱氨酸组织蛋白酶在许多（病理）生理条件下发挥着重要作用。其中，组织蛋白酶 L、S、K 和 B 是几个药物发现计划的研究对象。除了作为药物靶点的作用外，半胱氨酸组织蛋白酶还被认为是炎症和癌症的潜在生物标志物。在此，我们描述了荧光标记的二肽和氮杂二肽腈的设计、合成、生物学评价和光谱特性。
