Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
Cells. 2021 Dec 17;10(12):3565. doi: 10.3390/cells10123565.
P21-activated kinases (PAKs) are serine/threonine kinases involved in the regulation of cell survival, proliferation, inhibition of apoptosis, and the regulation of cell morphology. Some members of the PAK family are highly expressed in several types of cancer, and they have also been implicated in several other medical disorders. They are thus considered to be good targets for treatment of cancer and other diseases. Although there are several inhibitors of the PAKs, the utility of some of these inhibitors is reduced for several reasons, including limited metabolic stability. One way to overcome this problem is the use of nanoparticles, which have the potential to increase drug delivery. The overall goals of this review are to describe the roles for PAK kinases in cell signaling and disease, and to describe how the use of nanomedicine is a promising new method for administering PAK inhibitors for the purpose of disease treatment and research. We discuss some of the basic mechanisms behind nanomedicine technology, and we then describe how these techniques are being used to package and deliver PAK inhibitors.
P21 激活激酶（PAKs）是丝氨酸/苏氨酸激酶，参与细胞存活、增殖、抑制细胞凋亡和细胞形态调节的调控。PAK 家族的一些成员在多种类型的癌症中高度表达，它们也与其他几种医学疾病有关。因此，它们被认为是治疗癌症和其他疾病的良好靶点。尽管有几种 PAK 的抑制剂，但由于多种原因，其中一些抑制剂的实用性降低，包括代谢稳定性有限。克服这个问题的一种方法是使用纳米粒子，它具有增加药物递送的潜力。本综述的总体目标是描述 PAK 激酶在细胞信号转导和疾病中的作用，并描述纳米医学的使用如何成为一种有前途的新方法，用于管理 PAK 抑制剂，以达到疾病治疗和研究的目的。我们讨论了纳米医学技术背后的一些基本机制，然后描述了如何使用这些技术来包装和输送 PAK 抑制剂。
