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Small Molecule Control of Chromatin Remodeling
Aidan Finley, Robert A. Copeland Chemistry & Biology Volume 21, Issue 9, Pages (September 2014) DOI: /j.chembiol Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 1 Cartoon of the Conformational Transition of Chromatin from the More Open, Uncondensed Euchromatin State to the More Condensed Heterochromatin State Purple and red spheres represent individual histone proteins comprising the nucleosome core around which the DNA (turquoise) is wrapped. Small circles are meant to represent covalent modifications to the DNA and histones. Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 2 Reversible Methylation of Cytosine within CpG Islands of DNA
Methylation is catalyzed by the DNMT class of enzymes and reversed, in a multistep process, by the TET class of enzymes. See text for further details. SAM, S-adenosyl methionine; SAH, S-adenosyl homocysteine; α-KG, alpha-ketoglutarate. Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 3 The Chemistry of Histone Acetylation
(A) Reaction mechanism for the histone acetyltransferases (HATs). (B) Reaction mechanism for the metal-dependent histone deacetylases (HDACs). (C) Reaction mechanism for the Sirtuin histone deacetylases. Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 4 The Chemistry of Histone Methylation
(A) The common methyl group donor SAM is converted to SAH by all protein methyltransferases (PMTs). (B) Stepwise methylation of the ε-nitrogen of lysine side chains by the protein lysine methyltransferases (PKMTs) and of the side chain guanidino group of arginine by the protein arginine methyltransferases (PRMTs). (C) Reaction mechanism for the flavin-dependent lysine demethylases (LSDs). (D) Reaction mechanism for the iron-dependent lysine demethylases (JmjC). Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 5 Small Molecule Modulators of Histone Acetylation
(A) Histone acetyltransferase (HAT) inhibitors. (B) Metal-dependent histone deacetylase (HDAC) inhibitors. (C) BET domain protein antagonists. Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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Figure 6 Small Molecule Modulators of Histone Methylation
(A) Protein methyltransferase (PMT) inhibitors. (B) Lysine demethylase (KDM) inhibitors. (C) KMe reader domain protein antagonists. Chemistry & Biology , DOI: ( /j.chembiol ) Copyright © 2014 Elsevier Ltd Terms and Conditions
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