molecules of the month

compound 27 (CTPS1)

CTPS1/2 inhibitor

in vivo anti-inflammatory activity in mice

in-house HTS of 240K library + opt.

J. Med. Chem., 30 November 2022

Sygnature Discovery, UK and Step Pharma, FR

compound 27 chemical structure CTPS1/2 inhibitor- Sygnature Discovery, UK and Step Pharma, FR
3 mins read

Toward CTPS1 inhibitors as a safer alternative to nucleoside chemotherapeutics: Rapidly growing cancer cells are critically dependent on synthesis of nucleotides, the building blocks of RNA and DNA. Blocking the synthesis of nucleotides is a tried-and-true mechanism of action for widely used chemotherapeutics such as cytarabine (ara-C) and gemcitabine. However, such molecules are toxic due to their non-specific activity. Cytosine 5’-triphosphate synthase (CTPS) 1 and 2 are homologous enzymes that catalyze the final step in the de novo synthesis of the nucleotide CTP from UTP. Loss of CTPS1 function in humans leads to increased susceptibility to infections due to inhibited B and T cell proliferation, suggesting its critical role in lymphoid cells. The lack of significant effects in non-hematopoetic cell…

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