Enhancing Repair of Oxidative DNA Damage with Small-Molecule Activators of MTH1 was written by Lee, Yujeong;Onishi, Yoshiyuki;McPherson, Lisa;Kietrys, Anna M.;Hebenbrock, Marian;Jun, Yong Woong;Das, Ishani;Adimoolam, Shanthi;Ji, Debin;Mohsen, Michael G.;Ford, James M.;Kool, Eric T.. And the article was included in ACS Chemical Biology in 2022.Category: iodides-buliding-blocks This article mentions the following:
Here, it is reported that selected tyrosine kinase (TK) inhibitors including nilotinib, employed clin. in the treatment of chronic myeloid leukemia, are activators of the repair enzyme Human MutT Homolog 1 (MTH1). MTH1 cleanses the oxidatively damaged cellular nucleotide pool by hydrolyzing the oxidized nucleotide 8-oxo-2′-deoxyguanosine (8-oxo-dG)TP, which is a highly mutagenic lesion when incorporated into DNA. Structural optimization of analogs of TK inhibitors resulted in compounds such as SU0448, which induces 1000 +/- 100% activation of MTH1 at 10μM and 410 +/- 60% at 5μM. The compounds are found to increase the activity of the endogenous enzyme, and at least one (SU0448) decreases levels of 8-oxo-dG in cellular DNA. The results suggest the possibility of using MTH1 activators to decrease the frequency of mutagenic nucleotides entering DNA, which may be a promising strategy to suppress tumorigenesis in individuals with elevated cancer risks. In the experiment, the researchers used many compounds, for example, 5-Iodonicotinic acid (cas: 15366-65-1Category: iodides-buliding-blocks).
5-Iodonicotinic acid (cas: 15366-65-1) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. Polyiodoorganic compounds are sometimes employed as X-ray contrast agents, in fluoroscopy, a type of medical imaging. This application exploits the X-ray absorbing ability of the heavy iodine nucleus.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com