Autelitano Dominic J, Rajic Antonio, Smith A Ian, Berndt Michael C, Ilag Leodevico L, Vadas Mathew
Cryptome Pharmaceuticals, PO Box 6492, St. Kilda Rd Central, Melbourne, Vic 8008, Australia.
Drug Discov Today. 2006 Apr;11(7-8):306-14. doi: 10.1016/j.drudis.2006.02.003.
There is increasing evidence that proteolytic cleavage gives rise to 'hidden' peptides with bioactivities that are often unpredicted and totally distinct to the parent protein. So far, the liberation of these cryptic peptides, or crypteins, has been shown to be prevalent in proteins associated with endocrine signalling, the extracellular matrix, the complement cascade and milk. A broad spectrum of proteases has been implicated in the generation of natural crypteins that appear to play a role in modulating diverse biological processes, such as angiogenesis, immune function and cell growth. The proteolytic liberation of crypteins with novel activities represents an important mechanism for increasing diversity of protein function and potentially offers new opportunities for protein-based therapeutics.
越来越多的证据表明，蛋白水解切割会产生具有生物活性的“隐藏”肽段，其生物活性往往是无法预测的，且与母体蛋白完全不同。到目前为止，这些隐蔽肽段（即隐肽）的释放已被证明在与内分泌信号传导、细胞外基质、补体级联反应和乳汁相关的蛋白质中普遍存在。多种蛋白酶与天然隐肽的产生有关，这些隐肽似乎在调节多种生物学过程中发挥作用，如血管生成、免疫功能和细胞生长。具有新活性的隐肽的蛋白水解释放是增加蛋白质功能多样性的重要机制，并且可能为基于蛋白质的治疗提供新的机会。
