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ROCK-2-selective targeting and its therapeutic outcomes.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2019-12-12 , DOI: 10.1016/j.drudis.2019.11.017
Prasanti Sharma 1 , Kalyan Roy 1
Affiliation  

Despite the identification of distinct isoforms of Rho-kinase (ROCK-1 and ROCK-2), their isoform-specific roles in several disorders remain obscure. Recent studies have revealed a vital role of ROCK-2 in various vascular and neuronal disorders, where the potential for disease alleviation is wider with ROCK-2-selective targeting than with nonspecific ROCK inhibition. This approach is also crucial for resolving issues of safety and specificity associated with nonspecific ROCK inhibitors. In this review, we focus on the latest developments concerning ROCK-2 as a therapeutic target and justify the clinical use of ROCK-2-selective inhibitors.

中文翻译:

ROCK-2-选择性靶向及其治疗效果。

尽管已鉴定出Rho激酶的不同同工型(ROCK-1和ROCK-2),但它们在几种疾病中的同工型特异性作用仍然不清楚。最近的研究表明,ROCK-2在各种血管和神经元疾病中起着至关重要的作用,与非特异性ROCK抑制相比,ROCK-2选择性靶向可减轻疾病的可能性更大。这种方法对于解决与非特异性ROCK抑制剂相关的安全性和特异性问题也至关重要。在这篇综述中,我们集中于有关ROCK-2作为治疗靶标的最新进展,并证明ROCK-2选择性抑制剂的临床应用是合理的。
更新日期:2019-12-13
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