2 Hits in 9.2 sec

Inhibitors of Protein Methyltransferases and Demethylases

H. Ümit Kaniskan, Michael L. Martini, Jian Jin
2017 Chemical Reviews  
In this review, we cover the discovery, characterization, and biological application of inhibitors of PMTs and KDMs with emphasis on key advancements in the field.  ...  Consequently, discovering and developing inhibitors of these enzymes has become a very active and fast-growing research area over the past decade.  ...  Another report on the design and synthesis of reversible LSD1 inhibitors came from Zheng and co-workers in 2013. 543 This new class of triazole−dithiocarbamate-containing inhibitors was based on their  ... 
doi:10.1021/acs.chemrev.6b00801 pmid:28338320 pmcid:PMC5610952 fatcat:ifwczoutfndpljmpeqkyw2tsxm

SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases

Jing Zhang, Yujun George Zheng
2015 ACS Chemical Biology  
Meanwhile, new compounds built upon or derived from the SAM scaffold have been designed and tested as selective inhibitors for important MTase targets.  ...  In the past, many SAM/SAH analogs have been synthesized as MTase inhibitors. However, due to the restriction of protein expression and purification techniques, many of Zhang and Zheng  ...  Acknowledgments We are thankful to the National Institutes of Health, National Science Foundation, and American Heart Association for financial support.  ... 
doi:10.1021/acschembio.5b00812 pmid:26540123 pmcid:PMC5772741 fatcat:iri4iiarfffnbnxnmguceddw4u