Chemistry:YC8-02
From HandWiki
YC8-02 is a drug which acts as a potent inhibitor of the enzymes sirtuin 2 (SIRT2) and sirtuin 3 (SIRT3). It was developed from an older SIRT2 selective inhibitor thiomyristoyl, but substituted with a triphenylphosphine group which increases affinity to SIRT3 and selectively targets uptake into mitochondria. It is still relatively selective for SIRT2 with an IC50 of 62nM at SIRT2 vs 530nM at SIRT3, but this still makes it one of the most potent SIRT3 inhibitors currently available. In animal studies it is useful for the treatment of certain forms of blood cancer such as lymphoma and leukemia.[1][2][3]
See also
References
- ↑ "Non-oncogene Addiction to SIRT3 Plays a Critical Role in Lymphomagenesis". Cancer Cell 35 (6): 916–931.e9. June 2019. doi:10.1016/j.ccell.2019.05.002. PMID 31185214.
- ↑ "A Mitochondria-Targeting SIRT3 Inhibitor with Activity against Diffuse Large B Cell Lymphoma". Journal of Medicinal Chemistry 67 (17): 15428–15437. September 2024. doi:10.1021/acs.jmedchem.4c01053. PMID 39191393.
- ↑ "Simultaneous inhibition of Sirtuin 3 and cholesterol homeostasis targets acute myeloid leukemia stem cells by perturbing fatty acid β-oxidation and inducing lipotoxicity". Haematologica 108 (9): 2343–2357. September 2023. doi:10.3324/haematol.2022.281894. PMID 37021547.
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