The non-canonical target PARP16 contributes to polypharmacology of the PARP inhibitor talazoparib and its synergy with WEE1 inhibitors was written by Palve, Vinayak;Knezevic, Claire E.;Bejan, Daniel S.;Luo, Yunting;Li, Xueli;Novakova, Silvia;Welsh, Eric A.;Fang, Bin;Kinose, Fumi;Haura, Eric B.;Monteiro, Alvaro N.;Koomen, John M.;Cohen, Michael S.;Lawrence, Harshani R.;Rix, Uwe. And the article was included in Cell Chemical Biology in 2022.SDS of cas: 850462-65-6 This article mentions the following:
PARP inhibitors (PARPis) display single-agent anticancer activity in small cell lung cancer (SCLC) and other neuroendocrine tumors independent of BRCA1/2 mutations. Here, we determine the differential efficacy of multiple clin. PARPis in SCLC cells. Compared with the other PARPis rucaparib, olaparib, and niraparib, talazoparib displays the highest potency across SCLC, including SLFN11-neg. cells. Chem. proteomics identifies PARP16 as a unique talazoparib target in addition to PARP1. Silencing PARP16 significantly reduces cell survival, particularly in combination with PARP1 inhibition. Drug combination screening reveals talazoparib synergy with the WEE1/PLK1 inhibitor adavosertib. Global phosphoproteomics identifies disparate effects on cell-cycle and DNA damage signaling thereby illustrating underlying mechanisms of synergy, which is more pronounced for talazoparib than olaparib. Notably, silencing PARP16 further reduces cell survival in combination with olaparib and adavosertib. Together, these data suggest that PARP16 contributes to talazoparib′s overall mechanism of action and constitutes an actionable target in SCLC. In the experiment, the researchers used many compounds, for example, Methyl 2-(bromomethyl)-5-fluoro-3-nitrobenzoate (cas: 850462-65-6SDS of cas: 850462-65-6).
Methyl 2-(bromomethyl)-5-fluoro-3-nitrobenzoate (cas: 850462-65-6) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.SDS of cas: 850462-65-6
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary