蛋白酪胺酸激脢(protein tyrosine kinase)，簡稱為PTKs，是催化受質(substrate)和ATP之間的反應，亦即在PTKs的催化下，ATPγ位置上的磷酸根會轉移至受質的tyrosine上。如此的機制，便造成細胞間訊號的傅遞，進而造成分裂、增殖以及生長。如果能有一種抑制劑能與PTKs結合，且其與PTKs結合能力較其它受質強，如此便可以中斷細胞間訊號的傅遞，進而減緩或中止細胞分裂、增殖以及生長。如此便可以作為對抗細菌、病毒、惡性腫瘤等等的藥劑。本實驗室以Solution-Phase以及Solid-Phase的方式，成功合成多種摸擬PTKs的抑制劑，希望這些藥劑能如模擬中的一樣，具有生物活性。也期望自己的努力能為人類盡一些綿帛之力 Protein tyrosine kinases (PTKs) catalyze reaction between substrate and ATP. In the presence of PTKs, the phosphate from theγposition of ATP will transfer to the tyrosine of the substrate. Which will be a message that induces the cell division, multiplication, or growth. Here, we successfully synthesized a series of potential PTKs inhibitors, which mimic the substrate, in nine steps by applying combinatorial solid phase method. At the same time, the evaluation biological activity is in process.
