首页> 美国卫生研究院文献>Journal of Enzyme Inhibition and Medicinal Chemistry >The first activation study of a δ-carbonic anhydrase: TweCAδ from the diatom Thalassiosira weissflogii is effectively activated by amines and amino acids
【2h】

The first activation study of a δ-carbonic anhydrase: TweCAδ from the diatom Thalassiosira weissflogii is effectively activated by amines and amino acids

机译:δ-碳酸酐酶的首次激活研究:来自硅藻Thalassiosira weissflogii的TweCAδ被胺和氨基酸有效激活

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务,本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文,但由于OA文献来源多样且变更频繁,仍可能出现获取不到、文献不完整或与标题不符等情况,如果获取不到我们将提供退款服务。请知悉。

摘要

The activation of the δ-class carbonic anhydrase (CAs, EC 4.2.1.1) from the diatom Thalassiosira weissflogii (TweCAδ) was investigated using a panel of natural and non-natural amino acids and amines. The most effective activator of TweCAδ was d-Tyr (KA of 51 nM), whereas several other amino acids and amines, such as L-His, L-Trp, d-Trp, dopamine and serotonin were submicromolar activators (KAs from 0.51 to 0.93 µM). The most ineffective activator of TweCAδ was 4-amino-l-Phe (18.9 µM), whereas d-His, l-/d-Phe, l-/d-DOPA, l-Tyr, histamine, some pyridyl-alkylamines, l-adrenaline and aminoethyl-piperazine/morpholine were moderately potent activators (KAs from 1.34 to 8.16 µM). For any δ-CA, there are no data on the crystal structure, homology modelling and the amino acid residues that are responsible for proton transfer to the active site are currently unknown making it challenging to provide a detailed rational for these findings. However, these data provide further evidence that this class of underexplored CA deserves more attention.
机译:使用一组天然和非天然氨基酸和胺,研究了硅藻Thalasiosira weissflogii(TweCAδ)中δ类碳酸酐酶(CAs,EC 4.2.1.1)的活化。 TweCAδ最有效的活化剂是d-Tyr(KA为51 nM),而其他几种氨基酸和胺,例如L-His,L-Trp,d-Trp,多巴胺和5-羟色胺则是亚微摩尔活化剂(KA的范围从0.51至0.93 µM)。 TweCAδ最无效的活化剂是4-氨基-1-苯丙氨酸(18.9μm),而d-His,l- / d-Phe,l // d-DOPA,l-Tyr,组胺,一些吡啶基烷基胺,l -肾上腺素和氨乙基-哌嗪/吗啉是中等有效的激活剂(KAs在1.34至8.16µM之间)。对于任何δ-CA,都没有关于晶体结构的数据,同源性建模以及负责质子转移至活性位点的氨基酸残基目前尚不清楚,因此很难为这些发现提供详细的合理性。但是,这些数据提供了进一步的证据,表明此类未充分开发的CA值得更多关注。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号