组蛋白去乙酰化酶蛋白 8 的内腔功能：R37 是催化的关键残基。
On the function of the internal cavity of histone deacetylase protein 8: R37 is a crucial residue for catalysis.
机构信息
Centre for Cancer Research and Cell Biology, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2129-32. doi: 10.1016/j.bmcl.2011.01.128. Epub 2011 Feb 2.
Abstract
Biochemical studies reveal that a conserved arginine residue (R37) at the centre of the 14Å internal cavity of histone deacetylase (HDAC) 8 is important for catalysis and acetate affinity. Computational studies indicate that R37 forms multiple hydrogen bonding interactions with the backbone carbonyl oxygen atoms of two conserved glycine residues, G303 and G305, resulting in a 'closed' form of the channel. One possible rationale for these data is that water or product (acetate) transit through the catalytically crucial internal channel of HDAC8 is regulated by a gating interaction between G139 and G303 tethered in position by the conserved R37.
摘要
生化研究表明，组蛋白去乙酰化酶（HDAC）8 的 14Å 内部腔中心的保守精氨酸残基（R37）对于催化和乙酸亲和力很重要。计算研究表明，R37 与两个保守甘氨酸残基 G303 和 G305 的骨架羰基氧原子形成多个氢键相互作用，导致通道呈“关闭”形式。这些数据的一个可能的原理是，水或产物（乙酸）通过 HDAC8 的催化关键内部通道的转运是由通过保守的 R37 固定位置的 G139 和 G303 之间的门控相互作用来调节的。
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