靶向蛋白催化功能的小分子抑制剂具有特异性差和临床副作用多等缺点, 靶向蛋白的非催化功能
在药物开发中具有较大的潜力. 鉴于靶向蛋白非催化功能抑制剂的广阔的应用前景 …

The small molecule inhibitors targeting the conserved catalytic function of proteins face such
challenges as poor specificity and numerous side-effects, while targeting the non-catalytic …

蛋白酶广泛存在于生物体中, 参与分解蛋白质, 维持生物体正常的生命活动. 蛋白酶抑制剂通过与
蛋白酶活性位点结合调控靶蛋白酶活性, 从而影响蛋白质代谢. 蛋白酶及其抑制剂关键氨基酸的 …

The druggability of a target is defined by the likelihood of a certain target binding site to be
amendable to functional modulation by a small molecule in vivo. Thus, druggability depends …

Enzyme inhibition is a crucial mechanism for regulating biological processes and
developing therapeutic interventions. This pharmacological review summarizes recent …

Many of the highest priority targets in a wide range of disease states are difficult‐to‐drug
proteins. The development of reversible small molecule inhibitors for the active sites of these …

目的综述小分子抗肿瘤蛋白激酶抑制剂的研究进展. 方法以近5 年文献为主要依据,
对激酶靶点及小分子抑制剂的研究发展变化进行分析, 整理和总结. 结果呈现由单作用靶点抑制 …

Drugs that function as enzyme inhibitors constitute a significant portion of the orally
bioavailable therapeutic agents that are in clinical use today. Likewise, much of drug …

Cruzain, a cysteine protease in the cathepsin family, is pivotal to the life-cycle of
Trypanosoma cruzi, the etiological agent in Chagas disease. Current inhibitors of cruzain …

Activation-by-inhibition is a biochemical paradox seldom observed in exosite enzymes,
wherein active site-bound inhibitors unexpectedly lead to enzyme activation. This intriguing …