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The direct PAK1 inhibitor, TAT-PAK18, blocks preferentially the growth of human ovarian cancer cell lines in which PAK1 is abnormally activated by autophosphorylation at Thr 423.
Hashimoto H, Sudo T, Maruta H, Nishimura R. Hashimoto H, et al. Among authors: maruta h. Drug Discov Ther. 2010 Feb;4(1):1-4. Drug Discov Ther. 2010. PMID: 22491145
1,2,3-Triazolyl ester of ketorolac (15K): Boosting both heat-endurance and lifespan of C. elegans by down-regulating PAK1 at nM levels.
Nguyen BC, Kim SA, Won SM, Park SK, Uto Y, Maruta H. Nguyen BC, et al. Among authors: maruta h. Drug Discov Ther. 2018;12(2):92-96. doi: 10.5582/ddt.2018.01018. Drug Discov Ther. 2018. PMID: 29760342 Free article.
Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway.
Ahn MR, Bae JY, Jeong DH, Takahashi H, Uto Y, Maruta H. Ahn MR, et al. Among authors: maruta h. Drug Discov Ther. 2017;11(6):300-306. doi: 10.5582/ddt.2017.01058. Drug Discov Ther. 2017. PMID: 29332887 Free article.
The serum/PDGF-dependent "melanogenic" role of the minute level of the oncogenic kinase PAK1 in melanoma cells proven by the highly sensitive kinase assay.
Be Tu PT, Nguyen BC, Tawata S, Yun CY, Kim EG, Maruta H. Be Tu PT, et al. Among authors: maruta h. Drug Discov Ther. 2017 Jan 15;10(6):314-322. doi: 10.5582/ddt.2016.01062. Epub 2016 Oct 17. Drug Discov Ther. 2017. PMID: 27746419
1,2,3-Triazolyl ester of Ketorolac: A "Click Chemistry"-based highly potent PAK1-blocking cancer-killer.
Nguyen BCQ, Takahashi H, Uto Y, Shahinozzaman MD, Tawata S, Maruta H. Nguyen BCQ, et al. Among authors: maruta h. Eur J Med Chem. 2017 Jan 27;126:270-276. doi: 10.1016/j.ejmech.2016.11.038. Epub 2016 Nov 20. Eur J Med Chem. 2017. PMID: 27889630
Signal therapy of human pancreatic cancer and NF1-deficient breast cancer xenograft in mice by a combination of PP1 and GL-2003, anti-PAK1 drugs (Tyr-kinase inhibitors).
Hirokawa Y, Levitzki A, Lessene G, Baell J, Xiao Y, Zhu H, Maruta H. Hirokawa Y, et al. Among authors: maruta h. Cancer Lett. 2007 Jan 8;245(1-2):242-51. doi: 10.1016/j.canlet.2006.01.018. Epub 2006 Mar 15. Cancer Lett. 2007. PMID: 16540233
Sichuan pepper extracts block the PAK1/cyclin D1 pathway and the growth of NF1-deficient cancer xenograft in mice.
Hirokawa Y, Nheu T, Grimm K, Mautner V, Maeda S, Yoshida M, Komiyama K, Maruta H. Hirokawa Y, et al. Among authors: maruta h. Cancer Biol Ther. 2006 Mar;5(3):305-9. doi: 10.4161/cbt.5.3.2404. Epub 2006 Mar 12. Cancer Biol Ther. 2006. PMID: 16418572
Signal therapy of breast cancers by the HDAC inhibitor FK228 that blocks the activation of PAK1 and abrogates the tamoxifen-resistance.
Hirokawa Y, Arnold M, Nakajima H, Zalcberg J, Maruta H. Hirokawa Y, et al. Among authors: maruta h. Cancer Biol Ther. 2005 Sep;4(9):956-60. doi: 10.4161/cbt.4.9.1911. Epub 2005 Sep 13. Cancer Biol Ther. 2005. PMID: 16082189
Signal therapy of NF1-deficient tumor xenograft in mice by the anti-PAK1 drug FK228.
Hirokawa Y, Nakajima H, Hanemann CO, Kurtz A, Frahm S, Mautner V, Maruta H. Hirokawa Y, et al. Among authors: maruta h. Cancer Biol Ther. 2005 Apr;4(4):379-81. doi: 10.4161/cbt.4.4.1649. Epub 2005 Apr 4. Cancer Biol Ther. 2005. PMID: 15846074
A clue to the therapy of neurofibromatosis type 2: NF2/merlin is a PAK1 inhibitor.
Hirokawa Y, Tikoo A, Huynh J, Utermark T, Hanemann CO, Giovannini M, Xiao GH, Testa JR, Wood J, Maruta H. Hirokawa Y, et al. Among authors: maruta h. Cancer J. 2004 Jan-Feb;10(1):20-6. doi: 10.1097/00130404-200401000-00006. Cancer J. 2004. PMID: 15000491
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