Amide-Derived Lysine Analogues as Substrates and Inhibitors of Histone Lysine Methyltransferases and Acetyltransferases

2021 ◽  
Author(s):  
Jordi Hintzen ◽  
Jona Merx ◽  
Marijn Maas ◽  
Sabine Langens ◽  
Paul White ◽  
...  
Keyword(s):  
Gene Regulation ◽  
Human Gene ◽  
Histone Lysine ◽  
Lysine Residues ◽  
Lysine Methyltransferases ◽  
Histone Lysine Methyltransferases

Histone lysine methyltransferases and acetyltransferases are two classes of epigenetic enzymes that play pivotal roles in human gene regulation. Although they both recognise and posttranslationally modify lysine residues in histone...

scholarly journals Allosteric regulation of histone lysine methyltransferases: from context-specific regulation to selective drugs

2021 ◽  
Author(s):  
Chen Davidovich ◽  
Qi Zhang
Keyword(s):  
Molecular Mechanisms ◽  
Allosteric Regulation ◽  
Precise Control ◽  
Histone Lysine ◽  
Allosteric Sites ◽  
Lysine Residues ◽  
Lysine Methyltransferases ◽  
Specific Regulation ◽  
Context Specific ◽  
Histone Lysine Methyltransferases

Histone lysine methyltransferases (HKMTs) are key regulators of many cellular processes. By definition, HKMTs catalyse the methylation of lysine residues in histone proteins. The enzymatic activities of HKMTs are under precise control, with their allosteric regulation emerging as a prevalent paradigm. We review the molecular mechanisms of allosteric regulation of HKMTs using well-studied histone H3 (K4, K9, K27 and K36) methyltransferases as examples. We discuss the current advances and future potential in targeting allosteric sites of HKMTs for drug development.

scholarly journals Methylation of geometrically constrained lysine analogues by histone lysine methyltransferases

2020 ◽  
Vol 56 (20) ◽  
pp. 3039-3042 ◽  
Author(s):  
Abbas H. K. Al Temimi ◽  
Paul B. White ◽  
Marcus J. M. Mulders ◽  
Nicole G. A. van der Linden ◽  
Richard H. Blaauw ◽  
...  
Keyword(s):  
Substrate Specificity ◽  
Histone Lysine ◽  
Lysine Methyltransferases ◽  
Geometrically Constrained ◽  
Histone Lysine Methyltransferases

Histone lysine methyltransferases (KMTs) exhibit substrate specificity for lysine and its geometrically constrained mimics.

Role of Histone Lysine Methyltransferases SUV39H1 and SETDB1 in Gliomagenesis: Modulation of Cell Proliferation, Migration, and Colony Formation

2013 ◽  
Vol 16 (1) ◽  
pp. 70-82 ◽  
Author(s):  
Anastasia Spyropoulou ◽  
Antonios Gargalionis ◽  
Georgia Dalagiorgou ◽  
Christos Adamopoulos ◽  
Kostas A. Papavassiliou ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Colony Formation ◽  
Histone Lysine ◽  
Lysine Methyltransferases ◽  
Histone Lysine Methyltransferases

scholarly journals Role of several histone lysine methyltransferases in tumor development

2016 ◽  
Vol 4 (3) ◽  
pp. 293-299 ◽  
Author(s):  
JIFU LI ◽  
SHUNQIN ZHU ◽  
XIAO-XUE KE ◽  
HONGJUAN CUI
Keyword(s):  
Tumor Development ◽  
Histone Lysine ◽  
Lysine Methyltransferases ◽  
Histone Lysine Methyltransferases

scholarly journals Lysine Ethylation by Histone Lysine Methyltransferases

ChemBioChem ◽  
2019 ◽  
Vol 21 (3) ◽  
pp. 392-400 ◽  
Author(s):  
Abbas H. K. Al Temimi ◽  
Michael Martin ◽  
Qingxi Meng ◽  
Danny C. Lenstra ◽  
Ping Qian ◽  
...  
Keyword(s):  
Histone Lysine ◽  
Lysine Methyltransferases ◽  
Histone Lysine Methyltransferases
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