PDPK1 is a master kinase, which is crucial for the activation of AKT /PKB and many other AGC kinases including PKC, S6K, SGK. An important role for PDPK1 is in the signaling pathways activated by several growth factors and hormones including insulin signaling.

2024年12月25日 · PDK1 (Pyruvate Dehydrogenase Kinase 1) is a Protein Coding gene. Diseases associated with PDK1 include Pyruvate Dehydrogenase E3-Binding Protein Deficiency and Polycystic Kidney Disease 1 With Or Without Polycystic Liver Disease. Among its related pathways are Regulation of pyruvate metabolism and ESR-mediated signaling.

2022年4月6日 · PDK1 (3-phosphoinositide-dependent kinase 1) is a serine/threonine-protein kinase that plays a central role in regulating cell growth, survival, and proliferation. Knocking out PDK1 in...

Nucleus-located PDK1 regulates growth, invasion and migration of breast cancer cells. These findings highlight the potential use of PGK1 mRNA level, PGK1 promoter hypomethylation, and PGK1 pS203 and PDHK1 pT338 levels as biomarkers for cancer progression and prognosis, and the promising significance of PGK1 as a target in cancer treatment.

PDK1, as an important direct target for metabolism, inhibits pyruvate flux to mitochondrial respiration. A rescue of PDK1 expression in Wnt-inhibited cancer cells rescues glycolysis as well as vessel growth in the tumor microenvironment [79,80].

PDK-1 是 PI3K 通路中的关键节点，通过磷酸化和随后激活许多其他 AGC 激酶家族成员（如蛋白激酶 B），在胰岛素和生长因子信号传导中发挥关键作用。 PDK-1 负责调节细胞增殖和迁移，并且还被发现在不同癌症（包括胰腺癌和乳腺癌）中发挥关键作用。 许多癌症驱动突变会诱导 PDK-1 靶标的激活，包括 Akt、S6K（p70 核糖体 S6 激酶）和 SGK。 因此，PDK1 是多种促存活和致癌蛋白激酶的关键激活剂，因此它作为肿瘤药物靶点引起了人们的极大兴趣。

In humans, there have been four isozymes of Pyruvate Dehydrogenase Kinase that have been shown to phosphorylate these three sites: PDK1, PDK2, PDK3, and PDK4. PDK1 is the only enzyme capable of phosphorylating the 3rd serine site.

2018年2月1日 · This review analyzes the up-to-date knowledge supporting PDK1 involvement in altered signaling in cancer, what cancer types and subtypes would benefit from a PDK1 targeting and the molecular mechanisms by which PDK1 is involved in tumors.

2022年3月1日 · Here, we show that Pyruvate dehydrogenase kinase 1 (PDK1) acts as a targetable determinant of different metabolic states in acute myeloid leukemia (AML)....

An increasing amount of evidence hints at 3-phosphoinositide dependent protein kinase-1 (PDK1 or PDPK1) as an intriguing and underexplored target for cancer therapy. Several reports show that PDK1 expression is dysregulated in multiple cancer types.