Development and Therapeutic Potential of NUAKs Inhibitors,Journal of Medicinal Chemistry

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Development and Therapeutic Potential of NUAKs Inhibitors
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-12-24 , DOI: 10.1021/acs.jmedchem.0c00533
Muhammad Faisal ₁ , Jae Ho Kim ₂ , Kyung Ho Yoo ₂ , Eun Joo Roh _{1,

2} , Soon Sun Hong ₃ , So Ha Lee ₂

Affiliation

NUAK isoforms, NUAK1 (ARK5) and NUAK2 (SNARK), are important members of the AMPK family of protein kinases. They are involved in a broad spectrum of physiological and cellular events, and sometimes their biological roles overlap. NUAK isoform dysregulation is associated with numerous pathological disorders, including neurodegeneration, metastatic cancer, and diabetes. Therefore, they are promising therapeutic targets in metabolic diseases and cancers; consequently, various NUAK-targeted inhibitors have been disclosed. The first part of this review comprises a brief discussion of the homology, expression, structure, and characteristics of NUAK isoforms. The second part focuses on NUAK isoforms’ involvement in crucial biological operations, including mechanistic findings, highlighting how their abnormal functioning contributes to disease progression and quality of life. The third part summarizes the key findings and applications of targeting NUAK isoforms for treating multiple cancers and neurodegenerative disorders. The final part systematically presents a critical review and analysis of the literature on NUAK isoform inhibitions through small molecules.

中文翻译：

NUAKs抑制剂的开发和治疗潜力

NUAK亚型NUAK1（ARK5）和NUAK2（SNARK）是AMPK蛋白激酶家族的重要成员。它们参与广泛的生理和细胞事件，有时它们的生物学作用重叠。NUAK亚型失调与多种病理疾病有关，包括神经退行性疾病，转移性癌症和糖尿病。因此，它们是代谢疾病和癌症的有希望的治疗靶点。因此，已经公开了多种靶向NUAK的抑制剂。本文的第一部分简要讨论了NUAK亚型的同源性，表达，结构和特征。第二部分重点介绍NUAK亚型参与重要的生物学操作，包括机制发现，强调其异常功能如何促进疾病进展和生活质量。第三部分总结了靶向NUAK亚型治疗多种癌症和神经退行性疾病的关键发现和应用。最后一部分系统地介绍了有关通过小分子抑制NUAK同工型的文献的重要评论和分析。

更新日期：2021-01-14

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