An article Syntheses and evaluation of new Quinoline derivatives for inhibition of hnRNP K in regulating oncogene c-myc transcription WOS:000462472500001 published article about NUCLEAR RIBONUCLEOPROTEIN-K; CARBON NANOTUBES BINDING; I-MOTIF DNA; CELL-PROLIFERATION; STRANDED-DNA; G-QUADRUPLEX; PROMOTER; PROTEIN; METASTASIS; MECHANISM in [Shu, Bing; Zeng, Ping; Kang, Shuangshuang; Li, Peng-Hui; Hu, Dexuan; Kuang, Guotao; Cao, Jiaojiao; Li, Xiaoya; Zhang, Meiling; An, Lin-Kun; Huang, Zhi-Shu; Li, Ding] Sun Yat Sen Univ, Sch Pharmaceut Sci, 132 Waihuan East Rd, Guangzhou 510006, Guangdong, Peoples R China; [Shu, Bing] Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Guangdong, Peoples R China in 2019, Cited 54. Name: 1-(4-Nitrophenyl)ethanone. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6
Aberrant overexpression of heterogeneous nuclear ribonucleoprotein K (hnRNP K) is a key feature in oncogenesis and progression of many human cancers. hnRNP K has been found to be a transcriptional activator to up-regulate c-myc gene transcription, a critical proto-oncogene for regulation of cell growth and differentiation. Therefore, down-regulation of c-myc transcription by inhibiting hnRNP K through disrupting its binding to c-myc gene promoter is a potential approach for cancer therapy. In the present study, we synthesized and screened a series of Quinoline derivatives and evaluated their binding affinity for hnRNP K. Among these derivatives, (E)-1-(4-methoxyphenyl)-3-(4 morpholino-6-nitroquinolin-2-yl)prop-2-en-1-one (compound 25) was determined to be the first-reported hnRNP K binding ligand with its K-D values of 4.6 and 2.6 mu M measured with SPR and MST, respectively. Subsequent evaluation showed that the binding of compound 25 to hnRNP K could disrupt its unfolding of c-myc promoter i-motif, resulting in down-regulation of c-myc transcription. Compound 25 showed a selective anti-proliferative effect on human cancer cell lines with IC50, values ranged from 1.36 to 3.59 mu M. Compound 25 exhibited good tumor growth inhibition in a Hela xenograft tumor model, which might be related to its binding with hnRNP K. These findings illustrated that inhibition of DNA-binding protein hnRNP K by compound 25 could be a new and selective strategy of regulating oncogene transcription instead of targeting promoter DNA secondary structures such as G-quadruplexes or i-motifs.
Name: 1-(4-Nitrophenyl)ethanone. Welcome to talk about 100-19-6, If you have any questions, you can contact Shu, B; Zeng, P; Kang, SS; Li, PH; Hu, DX; Kuang, GT; Cao, JJ; Li, XY; Zhang, ML; An, LK; Huang, ZS; Li, D or send Email.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem