The p21 activated kinase (PAK) family of serine/threonine kinases are effector proteins for the Rho GTPases Cdc42 and Rac. They bind to Cdc42 and Rac through a GTPase Binding Domain (GBD), also sometimes known as a Cdc42 Rac Interactive Binding (CRIB) domain.

2021年10月25日 · The p21-Activated Kinases (PAKs) are a family of six serine/threonine kinases that were originally identified as downstream effectors of the Rho GTPases Cdc42 and Rac.

PAK（p21激活的激酶）是肌动蛋白动力学、细胞增殖和细胞存活的关键调节剂。 同时PAK还被认为是肌动蛋白细胞骨架和运动的主要调节因子。 由于它们在肌动蛋白重塑中的核心作用及其激活基质金属蛋白酶（MMPs）的能力，…

The p21 activated kinases (Paks) are well known effector proteins for the Rho GTPases Cdc42 and Rac. The Paks contain 6 members, which fall into 2 families of proteins. The first family consists of Paks 1, 2, and 3, and the second consists of Paks 4, 5, and 6.

The p21-activated kinases (PAKs) are central players in growth factor signaling networks and morphogenetic processes that control proliferation, cell polarity, invasion and actin cytoskeleton organization. This raises the possibility that interfering with PAK activity may produce significant anti-tumor activity.

2013年12月23日 · The amplification of p21-activated kinase (PAK) genes is the most well-described mechanism for increased PAK function in cancer; for example, amplification of chromosomal...

PAK 蛋白是丝氨酸/苏氨酸 p21 激活激酶家族，包括 PAK1、PAK2、PAK3 和 PAK4。 PAK 蛋白是将 Rho GTP 酶与细胞骨架重组和核信号联系起来的关键效应物。 它们作为小 GTP 结合蛋白 Cdc42 和 Rac 的靶标，并参与广泛的生物活动。 PAK4 与 GTP 结合形式的 Cdc42Hs 特异性相互作用，并弱激活 MAP 激酶的 JNK 家族。 PAK4 是丝状伪足形成的介质，可能在肌动蛋白细胞骨架的重组中发挥作用。 已经为该基因发现了编码不同亚型的多个选择性剪接的转录物变体。 …

2024年12月13日 · The PAK (p21-activated kinases) family is a class of intracellular signal transduction protein kinases that regulate various cellular functions, mainly through their interactions with small GTP enzymes. PAK1 and PAK2 in the PAK kinase family are key signal transduction molecules that play important …

PF-03758309 (PF-03758309) 是一种口服生物利用的，ATP竞争性的 p21-activated kinase (PAK) 抑制剂，其作用于PAK4的 Kd 为2.7 nM。 PF-3758309 具有抗增殖的作用，在HCT116肿瘤模型中可诱导凋亡。 FRAX486是有效的 PAK 抑制剂，抑制PAK1, PAK2, PAK3和PAK4的IC50分别为14, 33, 39和575 nM。 KPT 9274 ( ATG-019) 是一种具有口服活性的小分子化合物，是非竞争性的 PAK4 和 NAMPT 双重抑制剂。 在cell-free的酶活实验中，对NAMPT的IC50值约为120 nM。

The p21-Activated kinase 1 (PAK1), a member of serine-threonine kinases family, was initially identified as an interactor of the Rho GTPases RAC1 and CDC42, which affect a wide range of processes associated with cell motility, survival, metabolism, ...