Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the syk SH2 domains with equally high affinity as the natural ligand.

Dekker FJ; de Mol NJ; Fischer MJ; Liskamp RM

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Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the syk SH2 domains with equally high affinity as the natural ligand.

机译：二价配体的刚性间隔基中的氨基丙炔基苯甲酸结构单元以与天然配体同样高的亲和力与syk SH2结构域结合。

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摘要

The construction of rigid spacers composed of amino propynyl benzoic acid building blocks is described. These spacers were used to link two phosphopeptide ligand sites towards obtaining divalent ligands with a high affinity for Syk tandem SH2 domains, which are important in signal transduction. The spacer containing two of those rigid building blocks led to a ligand which was as active as the natural ligand, indicating that this building block can be used in the design and synthesis of high affinity divalent constructs that can successfully interfere with crucial protein-protein interactions.

机译：描述了由氨基丙炔基苯甲酸结构单元组成的刚性间隔基的结构。这些间隔子用于连接两个磷酸肽配体位点，以获得对Syk串联SH2结构域具有高亲和力的二价配体，这在信号转导中很重要。包含其中两个刚性结构单元的间隔基产生了一个与天然配体一样有活性的配体，表明该结构单元可用于设计和合成可以成功干扰关键蛋白-蛋白相互作用的高亲和力二价结构。

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《Bioorganic and Medicinal Chemistry Letters》 |2003年第7期|共4页
作者
Dekker FJ; de Mol NJ; Fischer MJ; Liskamp RM;
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正文语种 eng
中图分类药学;生物化学;
关键词
Ligands; Benzoic Acid; binding; Proteins; Signal Transduction; 配体; 苯甲酸; 蛋白质类; 信号传递;

机译：Ligands;Benzoic Acid;binding;Proteins;Signal Transduction;配体;苯甲酸;蛋白质类;信号传递;

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1. Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the syk SH2 domains with equally high affinity as the natural ligand. [J] . Dekker FJ, de Mol NJ, Fischer MJ, Bioorganic and Medicinal Chemistry Letters . 2003,第7期

机译：二价配体的刚性间隔基中的氨基丙炔基苯甲酸结构单元以与天然配体同样高的亲和力与syk SH2结构域结合。
2. Synthesis of the Novel Amino Acid 4-Amino-3-(aminomethyl)benzoic Acid (AmAbz) and Its Protected Derivatives as Building Blocks for Pseudopeptide Synthesis [J] . Robert Pascal, Regine Sola, Frederic Labeguere, European journal of organic chemistry . 2000,第22期

机译：新型氨基酸4-氨基-3-（氨基甲基）苯甲酸（AmAbz）的合成及其作为伪肽合成基础的受保护衍生物
3. Identification of the ligand-binding domains of CD22, a member of the immunoglobulin superfamily that uniquely binds a sialic acid-dependent ligand. [J] . P Engel, N Wagner, A S Miller, The Journal of Experomental Medicine . 1995,第4期

机译：CD22的配体结合域的鉴定，CD22是唯一与唾液酸依赖性配体结合的免疫球蛋白超家族成员。
4. Molecularly imprinted nano-cavities capable of size, shape and ligand binding domain recognition for proteins bearing high homologous amino acid sequences and sizes [C] . Yuri Kamon, Toshifumi Takeuchi 日本化学会春季年会講演予稿集 . 2018

机译：具有含有高同源氨基酸序列和尺寸的蛋白质的尺寸，形状和配体结合域识别的分子印迹纳米腔
5. Influence of length and flexibility of spacers on the binding affinity of divalent ligands [O] . Susanne Liese, Roland R Netz 2015

机译：间隔基的长度和柔韧性对二价配体结合亲和力的影响
6. Novel nonphosphorylated peptides with conserved sequences selectively bind to Grb7 SH2 domain with affinity comparable to its phosphorylated ligand. [O] . Dan Zhang, Chen Shao, Siqi Hu, 2012

机译：具有保守序列的新型非磷酸化肽选择性结合Grb7 sH2结构域，其亲和力与其磷酸化配体相当。

Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the syk SH2 domains with equally high affinity as the natural ligand.

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