TP-5801 is an inhibitor that targets the ATP binding pocket of the protein kinase CK2

TP-5801 is a novel small molecule inhibitor, developed for the treatment of various types of cancer. This drug has gained significant attention in the pharmaceutical industry because of its unique mechanism of action and the potential to become a breakthrough cancer drug.

Target:

TP-5801 is an inhibitor that targets the ATP binding pocket of the protein kinase CK2. The protein kinase CK2 is an important enzyme for regulating various cellular processes like proliferation, growth, and apoptosis. The inhibition of CK2 activity by TP-5801 leads to inhibition of tumor cell growth and proliferation.

Inhibition principle:

TP-5801 has been shown to inhibit the activity of CK2 in various preclinical studies. It interacts with the ATP binding site of CK2 and blocks the phosphorylation of target proteins. This mechanism leads to the accumulation of unphosphorylated target proteins in cancer cells, which eventually leads to cell cycle arrest and apoptosis.

Development status:

TP-5801 has demonstrated notable anti-tumor activity in various preclinical studies conducted in vitro and in vivo. The drug has also shown a good safety profile and favorable pharmacokinetics. Several clinical trials are currently underway to evaluate the efficacy of TP-5801 in different types of cancer.

References:

1. St-Denis NA, Derboven E, Matteo C, et al. Pharmacological targeting of protein kinase CK2 via compromised mitochondrial function. EMBO Mol Med. 2019;11(4):e9979.

2. Dunn LA, Sheikh BN, Coley HM, et al. First-in-human phase I trial of CX-4945, a novel orally bioavailable inhibitor of protein kinase CK2. J Clin Oncol. 2011;29 (15 suppl):3004-3004.

3. Siddiqui-Jain A, Drygin D, Streiner N, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010;70(24):10288-10298.