在序列随机混合物的活性概况中,子单位标识,子单位比例,链长和立体化学之间的相互作用
Zvi Hayouka1, Saswata Chakraborty, Runhui Liu
1Department of Chemistry, University of Wisconsin, Madison, Wisconsin 53706, USA.
Journal of the American Chemical Society
|August 6, 2013
概括
研究人员创建了混合物来测试抗菌和溶血性质. 使用具有特定氨基酸残留的异体基质二元混合物,但不是同体基质混合物,可以实现选择性抗菌活性.
科学领域:
- 类化学和药物化学.
背景情况:
- 固相合成是创建库的一个关键方法.
- 了解抗微生物的结构-活性关系对于开发新疗法至关重要.
研究的目的:
- 通过基于Fmoc的固相方法合成的混合物的抗菌和溶血性质的研究.
- 为了确定序列随机性和奇拉性是否影响选择性抗微生物活性.
主要方法:
- 利用基于Fmoc的固体相合成生成长度受控的混合物,其中包含一个疏水性和一个阴离子残留物.
- 对合成的混合物分析了针对相关病原体的抗菌活性和针对红细胞的血液溶解活性.
主要成果:
- 混合物表现出不同程度的抗菌和溶血活性.
- 含有D-和L-氨基酸的异体二元混合物显示出选择性的抗菌活性.
- 仅由L-或D-氨基酸组成的同体二元混合物没有表现出选择性的抗菌作用.
结论:
- 选择性抗菌活性可以通过仔细选择氨基酸残留物和在混合物中采用异构体设计来实现.
- 性在合成的抗菌疗效和选择性中起着至关重要的作用.
相关概念视频
Cooperative Allosteric Transitions
Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
Protein Organization
Overview
Protein Organization
Proteins are polymers of amino acid residues. They are versatile and responsible for different cellular functions, including DNA replication, molecular transport, catalysis, and structural support. Proteins have a hierarchical structure comprising at least three levels of organization: primary, secondary, and tertiary structure. Some large proteins have a quaternary structure where individual protein subunits are linked together.
The primary structure of a protein is its amino acid sequence.
The primary structure of a protein is its amino acid sequence.
Protein Folding
Overview
Protein Folding
Proteins are chains of amino acids linked together by peptide bonds. Upon synthesis, a protein folds into a three-dimensional conformation, critical to its biological function. Interactions between its constituent amino acids guide protein folding, and hence the protein structure is primarily dependent on its amino acid sequence.
Protein Structure Is Critical to Its Biological Function
Proteins perform a wide range of biological functions such as catalyzing chemical reactions, providing...
Protein Structure Is Critical to Its Biological Function
Proteins perform a wide range of biological functions such as catalyzing chemical reactions, providing...
Protein-protein Interfaces
Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a polypeptide...


