蛋白激?對於多種細胞過程的調控扮演著重要的角色。因此，涉及與疾病相關的?常信號的激?被認為是發展藥物的重要目標。在過去的幾?中， IκB 激?（IKK）已成為藥廠發展新型抗風濕和消炎藥的首要目標。在此研究計畫中，我們?用最近期刊發表的IKKβ的蛋白結構，重新探討合成過的苯甲醯胺衍生物與蛋白質的作用。我們發現，這些苯甲醯胺衍生物與IKK β的鍵結位置很明顯地分成?組；而這?組的位置合併起?正好與一些已知的IKKβ抑製劑與蛋白鍵結位置相同。因此，我們設計?一系?新的化合物，?結?個於?同鍵結位置的苯甲醯胺衍生物，希望這新的化合物能夠?有效地抑制IKKβ。 Protein kinases are regulators of a broad range of cellular processes. Consequently, kinases involved in disease-associated abnormal signaling are considered attractive targets for drug discovery. Over the past few years, IκB kinase (IKK) emerged as a prime target for the development of novel anti-rheumatic and anti-inflammatory drugs. In this proposal, we revisited the benzamide analogs, in which some were found to inhibit IKKβ, to examine their binding with IKKβ using recently published IKKβ protein structure. Interestingly, benzamide analogs group into two binding positions which coincide with the binding position of active IKKβ inhibitors. We thus want to design a new series of compounds which join up benzamide analogues at different binding positions and hoping that they would exhibit better IKKβ inhibition.
