Sigalov Alexander B
SignaBlok, Inc.; Shrewsbury, MA USA.
Self Nonself. 2010 Jul;1(3):192-224. doi: 10.4161/self.1.3.12794. Epub 2010 Jun 11.
Protein-protein interactions play a central role in biological processes and thus represent an appealing target for innovative drug design and development. They can be targeted by small molecule inhibitors, modulatory peptides and peptidomimetics, which represent a superior alternative to protein therapeutics that carry many disadvantages. Considering that transmembrane signal transduction is an attractive process to therapeutically control multiple diseases, it is fundamentally and clinically important to mechanistically understand how signal transduction occurs. Uncovering specific protein-protein interactions critical for signal transduction, a general platform for receptor-mediated signaling, the signaling chain homooligomerization (SCHOOL) platform, suggests these interactions as universal therapeutic targets. Within the platform, the general principles of signaling are similar for a variety of functionally unrelated receptors. This suggests that global therapeutic strategies targeting key protein-protein interactions involved in receptor triggering and transmembrane signal transduction may be used to treat a diverse set of diseases. This also assumes that clinical knowledge and therapeutic strategies can be transferred between seemingly disparate disorders, such as T cell-mediated skin diseases and platelet disorders or combined to develop novel pharmacological approaches. Intriguingly, human viruses use the SCHOOL-like strategies to modulate and/or escape the host immune response. These viral mechanisms are highly optimized over the millennia, and the lessons learned from viral pathogenesis can be used practically for rational drug design. Proof of the SCHOOL concept in the development of novel therapies for atopic dermatitis, rheumatoid arthritis, cancer, platelet disorders and other multiple indications with unmet needs opens new horizons in therapeutics.
蛋白质-蛋白质相互作用在生物过程中起着核心作用,因此是创新药物设计与开发的一个有吸引力的靶点。它们可以被小分子抑制剂、调节性肽和拟肽靶向,这些代表了携带许多缺点的蛋白质疗法的一种优越替代方案。鉴于跨膜信号转导是一个在治疗上控制多种疾病的有吸引力的过程,从机制上理解信号转导如何发生在基础和临床上都很重要。揭示对于信号转导至关重要的特定蛋白质-蛋白质相互作用,一个受体介导信号传导的通用平台,即信号链同型寡聚化(SCHOOL)平台,表明这些相互作用是通用的治疗靶点。在该平台内,各种功能不相关的受体的信号传导一般原则是相似的。这表明针对受体触发和跨膜信号转导中涉及的关键蛋白质-蛋白质相互作用的全局治疗策略可用于治疗多种疾病。这也假定临床知识和治疗策略可以在看似不同的疾病之间转移,例如T细胞介导的皮肤病和血小板疾病,或者结合起来开发新的药理学方法。有趣的是,人类病毒利用类似SCHOOL的策略来调节和/或逃避宿主免疫反应。这些病毒机制在数千年中高度优化,从病毒发病机制中学到的经验教训可实际用于合理的药物设计。SCHOOL概念在特应性皮炎、类风湿性关节炎、癌症、血小板疾病和其他多种未满足需求的适应症的新型疗法开发中的验证为治疗学开辟了新的视野。