Wang, S; Zhao, LJ; Shi, XJ; Ding, LN; Yang, LL; Wang, ZZ; Shen, DD; Tang, K; Li, XJ; Mamun, MAA; Li, HJ; Yu, B; Zheng, YC; Wang, SM; Liu, HM in [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Wang, Shaomeng; Liu, Hong-Min] Zhengzhou Univ, Inst Drug Discovery & Dev, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shaomeng] Univ Michigan, Dept Internal Med, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Pharmacol, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shaomeng] Univ Michigan, Dept Med Chem, 1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Liu, Hong-Min] Coinnovat Ctr Henan Prov New Drug R&D Preclin Saf, Zhengzhou 450001, Henan, Peoples R China; [Wang, Shuai; Zhao, Lijie; Shi, Xiao-Jing; Ding, Lina; Wang, Zhi-Zheng; Shen, Dandan; Tang, Kai; Li, Xiao-Jing; Mamun, M. A. A.; Li, Huiju; Yu, Bin; Zheng, Yi-Chao; Liu, Hong-Min] Zhengzhou Univ, Minist Educ China, Key Lab Adv Technol Drug Preparat Technol, Zhengzhou 450001, Henan, Peoples R China; [Yang, Linlin] Zhengzhou Univ, Sch Basic Med Sci, Dept Pharmacol, Zhengzhou 450001, Henan, Peoples R China; [Yu, Bin] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210023, Jiangsu, Peoples R China published Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5-a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction in 2019.0, Cited 53.0. Name: 1H-1,2,4-Triazol-5-amine. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
The cullin-RING ubiquitin ligases (CRLs) are responsible for about 20% of cellular protein degradation and regulate diverse cellular processes, and the dysfunction of CRLs is implicated in human diseases. Targeting the CRLs has become an emerging strategy for the treatment of human diseases. Herein, we describe the discovery of a hit compound from our in-house library and further structure-based optimizations, which have enabled the identification of new triazolo[1,5-a]pyrimidine-based inhibitors targeting the DCN1-UBC12 interaction. Compound WS-383 blocks the DCN1-UBC12 interaction (IC50 = 11 nM) reversibly and shows selectivity over selected kinases. WS-383 exhibits cellular target engagement to DCN1 in MGC-803 cells. WS-383 inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27, and NRF2. Collectively, targeting the DCN1-UBC12 interaction would be a viable strategy for selective neddylation inhibition of Cul3/1 and may be of therapeutic potential for disease treatment in which Cul3/1 is dysregulated.
Name: 1H-1,2,4-Triazol-5-amine. Bye, fridends, I hope you can learn more about C2H4N4, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics