NUAK

NUAK family SNF1-like kinase-1 [NUAK1, also known as ARK5 (AMPK-related kinase 5); EC 2.7.11.1] and the closely related NUAK2 [SNARK (SNF1/AMPK-related kinase)] are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor protein kinase[1]. They both contain a ubiquitin-associated domain located next to the C-terminal of their catalytic domains, which is required for LKB1 phosphorylation and activation. Studies on NUAK kinases hint at roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity and axon branching[2]. In the field of tumor biology, NUAK family members have been reported to promote tumor progression and metastatic capacity via the upregulation of cell proliferation, inhibition of p53-mediated tumor suppression, and increased matrix metalloproteinases (MMPs) in various cancer types. A key finding showing that NUAK1 operates as an essential survival factor in oncogenic Myc-driven tumours and may play a role in regulating tumor proliferation and survival through metabolic alteration in hepatocarcinoma. Therefore, targeting cellular energy homeostasis through inhibition of NUAK1 could be a valuable strategy to eliminate Myc-deregulated tumor cells[3].


[1] J.M. Lizcano et al. LKB1 is a master kinase that activates 13 kinases of the AMPK subfamily, including MARK/PAR-1. EMBO J. 2004 Feb 25;23(4):833-43.
[2] S. Banerjee et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.
[3] X. Sun et al. The regulation and function of the NUAK family. J Mol Endocrinol. 2013 Sep 10;51(2):R15-22. 

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Axon ID Name Description From price
2385 WZ 4003 Specific dual inhibitor of NUAK1 (ARK5) and NUAK2 (SNARK) €90.00

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