SART2 Inhibitors

Chemical inhibitors of SART2 can exert their inhibitory effects through various cellular pathways that are crucial for the protein's function. Bisindolylmaleimide I, a selective inhibitor of protein kinase C (PKC), impedes the phosphorylation events necessary for the regulation of proteins involved in cell cycle regulation and apoptosis, where SART2 plays a role. Similarly, Staurosporine broadly inhibits protein kinases that are integral to cell cycle control, potentially including those that regulate SART2, thus hindering the protein's function. LY294002 and Wortmannin are both specific inhibitors of PI3K, which is upstream in the AKT signaling pathway. This pathway's inhibition leads to reduced activity of downstream proteins, potentially including SART2 or its regulators. SP600125 and SB203580 target the stress response and inflammatory pathways by inhibiting c-Jun N-terminal kinase (JNK) and p38 MAP kinase, respectively. The inhibition of these kinases results in decreased phosphorylation of proteins that may interact with or regulate SART2, leading to a decrease in SART2 activity.

In addition to these, PD98059 and U0126 specifically inhibit MEK, which is upstream of ERK in the MAPK/ERK pathway, a pathway that SART2 may be involved in. By preventing MEK activity, these inhibitors decrease ERK activation and subsequent phosphorylation of proteins involved in cell division and differentiation, potentially including SART2. Leflunomide, through its inhibition of dihydroorotate dehydrogenase, impedes pyrimidine synthesis, which is essential for DNA synthesis and proliferation, and could, therefore, hinder SART2 activity in proliferating cells. Rapamycin suppresses the mTOR pathway, which is essential for cell growth and proliferation, potentially leading to the inhibition of downstream proteins that include SART2. Lastly, Roscovitine and Alsterpaullone are both potent inhibitors of cyclin-dependent kinases (CDKs). By impeding the activity of CDKs, these inhibitors can hamper cell cycle progression, leading to an inhibition of SART2.