Compound class:
Synthetic organic
Comment: TNG-462 (Tango Therapuetics) is a MTA-cooperative protein arginine methyltransferases 5 (PRMT5) inhibitor, that is proposed to treat methylthioadenosine phosphorylase (MTAP) deleted solid tumours. MTAP deficient cancer cells are unable to obtain adenine and methionine from the salvage pathway [1]. Adding inhibition of PRMT5 further decreases the viability of MTAP deficient cancer cells [2]. The chemical structure shown here was revealed during the First Time Disclosures session at the ACS meeting in September 2023, and we picked it up from Drug Hunter.
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References |
1. Bertino JR, Waud WR, Parker WB, Lubin M. (2011)
Targeting tumors that lack methylthioadenosine phosphorylase (MTAP) activity: current strategies. Cancer Biol Ther, 11 (7): 627-32. [PMID:21301207] |
2. Fu S, Zheng Q, Zhang D, Lin C, Ouyang L, Zhang J, Chen L. (2022)
Medicinal chemistry strategies targeting PRMT5 for cancer therapy. Eur J Med Chem, 244: 114842. [PMID:36274274] |