Name: 1H-1,2,4-Triazol-5-amine. In 2019.0 J MED CHEM published article about LEUKEMIA MLL PROTEIN; STRUCTURAL BASIS; MYC/MAX DIMERIZATION; HIGH-AFFINITY; LINEAGE; BINDING; RECOGNITION; COMPLEX; ASSOCIATION; METHYLATION in [Macdonald, Jonathan D.; Simon, Selena Chacon; Han, Changho; Wang, Fen; Shaw, J. Grace; Howes, Jennifer E.; Sai, Jiqing; Yuh, Joannes P.; Camper, Demarco; Alicie, Bethany M.; Alvarado, Joseph; Nikhar, Sameer; Payne, William; Bauer, Joshua A.; Zhao, Bin; Phan, Jason; Rossanese, Olivia W.; Fesik, Stephen W.] Vanderbilt Univ, Dept Biochem, Sch Med, Nashville, TN 37232 USA; [Aho, Erin R.; Thomas, Lance R.; Tansey, William P.] Vanderbilt Univ, Dept Cell & Dev Biol, Sch Med, Nashville, TN 37232 USA; [Waterson, Alex G.; Stauffer, Shaun R.; Fesik, Stephen W.] Vanderbilt Univ, Dept Pharmacol, Sch Med, Nashville, TN 37232 USA; [Waterson, Alex G.; Stauffer, Shaun R.; Fesik, Stephen W.] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA; [Macdonald, Jonathan D.; Alvarado, Joseph; Stauffer, Shaun R.] Cleveland Clin, Ctr Therapeut Discovery, Cleveland, OH 44195 USA; [Han, Changho] Vanderbilt Ctr Neurosci Drug Discovery, Franklin, TN 37067 USA; [Wang, Fen] Novartis Inst Biomed Res, Emeryville, CA 94608 USA; [Howes, Jennifer E.] PhoreMost Ltd, Cambridge CB22 3AT, England; [Yuh, Joannes P.] Bluerock Therapeut, Toronto, ON M5G 1L7, Canada; [Camper, Demarco] Bristol Meyers Squibb, Cambridge, MA 02142 USA; [Rossanese, Olivia W.] Inst Canc Res, London SM2 5NG, England in 2019.0, Cited 56.0. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5.
The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC via the disruption of the protein-protein interaction between MYC and its chromatin cofactor WD Repeat-Containing Protein 5. Blocking the association of these proteins is hypothesized to disrupt the localization of MYC to chromatin, thus disrupting the ability of MYC to sustain tumorigenesis. Utilizing a high-throughput screening campaign and subsequent structure-guided design, we identify small-molecule inhibitors of this interaction with potent in vitro binding affinity and report structurally related negative controls that can be used to study the effect of this disruption. Our work suggests that disruption of this protein-protein interaction may provide a path toward an effective approach for the treatment of multiple tumors and anticipate that the molecules disclosed can be used as starting points for future efforts toward compounds with improved drug-like properties.
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,
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