Chemistry:SirReal2
From HandWiki
SirReal2 is a drug which acts as a potent and selective sirtuin 2 (SIRT2) inhibitor. It inhibits SIRT2 with an IC50 of 140nM, and is selective over SIRT1, SIRT3 and SIRT5. It is used in research into cancer, inflammation and neurodegenerative disorders such as Parkinson's disease, and has led to the discovery of a number of related derivatives.[1][2][3][4][5][6][7]
References
- ↑ "Selective Sirt2 inhibition by ligand-induced rearrangement of the active site". Nature Communications 6. February 2015. doi:10.1038/ncomms7263. PMID 25672491. Bibcode: 2015NatCo...6.6263R.
- ↑ "SIRT2 Promotes the Migration and Invasion of Gastric Cancer through RAS/ERK/JNK/MMP-9 Pathway by Increasing PEPCK1-Related Metabolism". Neoplasia 20 (7): 745–756. July 2018. doi:10.1016/j.neo.2018.03.008. PMID 29925042.
- ↑ "Direct Comparison of SIRT2 Inhibitors: Potency, Specificity, Activity-Dependent Inhibition, and On-Target Anticancer Activities". ChemMedChem 13 (18): 1890–1894. September 2018. doi:10.1002/cmdc.201800391. PMID 30058233.
- ↑ "SIRT2 inhibits oxidative stress and inflammatory response in diabetic osteoarthritis". European Review for Medical and Pharmacological Sciences 24 (6): 2855–2864. March 2020. doi:10.26355/eurrev_202003_20649. PMID 32271403.
- ↑ "Virtual Screening Combined with Enzymatic Assays to Guide the Discovery of Novel SIRT2 Inhibitors". International Journal of Molecular Sciences 24 (11): 9363. May 2023. doi:10.3390/ijms24119363. PMID 37298312.
- ↑ "SIRT2 inhibitor SirReal2 enhances anti-tumor effects of PI3K/mTOR inhibitor VS-5584 on acute myeloid leukemia cells". Cancer Medicine 12 (18): 18901–18917. September 2023. doi:10.1002/cam4.6480. PMID 37658623.
- ↑ "Hunting potential SIRT2 inhibitors towards cancer treatment: Drug repurposing, molecular dynamics, and binding energy computations". Biochemical and Biophysical Research Communications 760. May 2025. doi:10.1016/j.bbrc.2025.151701. PMID 40158406. Bibcode: 2025BBRC..76051701I.
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