Chemistry:PF-3758309
From HandWiki
PF-3758309 is an experimental anticancer drug which acts as an inhibitor of p21-activated kinases with highest affinity for PAK4. It shows activity against a variety of different cancer types including colon, lung and pancreatic cancers, and is in early stage clinical trials.[1][2][3][4][5][6][7]
References
- ↑ "Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth". Proceedings of the National Academy of Sciences of the United States of America 107 (20): 9446–9451. May 2010. doi:10.1073/pnas.0911863107. PMID 20439741. Bibcode: 2010PNAS..107.9446M.
- ↑ "Therapeutic Potential of Targeting PAK Signaling". Anti-Cancer Agents in Medicinal Chemistry 16 (1): 75–88. 2016. doi:10.2174/1871520615666150617111414. PMID 26081410.
- ↑ "Inhibition of neuroblastoma proliferation by PF-3758309, a small-molecule inhibitor that targets p21-activated kinase 4". Oncology Reports 38 (5): 2705–2716. November 2017. doi:10.3892/or.2017.5989. PMID 29048629.
- ↑ "PAK inhibition by PF-3758309 enhanced the sensitivity of multiple chemotherapeutic reagents in patient-derived pancreatic cancer cell lines". American Journal of Translational Research 11 (6): 3353–3364. 2019. PMID 31312349.
- ↑ "Recent advances on development of p21-activated kinase 4 inhibitors as anti-tumor agents". Frontiers in Pharmacology 13. 2022. doi:10.3389/fphar.2022.956220. PMID 36105226.
- ↑ "Combined LIM kinase 1 and p21-Activated kinase 4 inhibitor treatment exhibits potent preclinical antitumor efficacy in breast cancer". Cancer Letters 493: 120–127. November 2020. doi:10.1016/j.canlet.2020.08.006. PMID 32829006.
- ↑ "Simultaneous inhibition of PI3K and PAK in preclinical models of neurofibromatosis type 2-related schwannomatosis". Oncogene 43 (13): 921–930. March 2024. doi:10.1038/s41388-024-02958-w. PMID 38336988.
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