构建一个可测序的蛋白质模拟库,具有真正的3D多元化化学空间
Zhonghan Li1, Shiqun Shao1, Xiaodong Ren1
1Department of Chemistry , University of California, Riverside , Riverside , California 92521 , United States.
Journal of the American Chemical Society
|October 27, 2018
概括
我们开发了新的双循环,模仿蛋白质. 一个类向c-Myccoprotein,通过干扰转录来抑制癌细胞的增殖.
科学领域:
- 药用化学 医学化学
- 分子生物学分子生物学
- 生物技术是生物技术.
背景情况:
- 像c-Myc这样的内在无序蛋白质是具有挑战性的治疗点.
- 蛋白质模拟剂为传统药物提供了一个有希望的替代品.
研究的目的:
- 创建一个具有多样化化学空间的新型双循环的库.
- 为了识别和表征一种抑制c-Myc活动的.
主要方法:
- 通过点击化学和环闭转化合成双循环.
- 通过Edman降解和线性化后的质谱测量来测序.
- 与c-Myc E363-R378表位组对抗的高通量选.
- 在体内测试在质母细胞瘤细胞系中的有效性.
主要成果:
- 一个纳米大小的图书馆,刚性双循环与空间多样化的侧链被合成.
- 鉴定了一种特定的,它与c-Myccoprotein结合.
- 这种表明了细胞内传递,干扰了c-Myc介导的转录,并抑制了质母细胞瘤细胞增殖.
结论:
- 双循环代表了开发新疗法的多功能支架.
- 用特定的抑制剂向c-Myc显示出质母细胞瘤治疗的潜力.
相关概念视频
True Stress and True Strain
848
Engineering stress is calculated as the load divided by the original, undeformed cross-sectional area. It approximates a material under load. This approximation is especially relevant post-yield in ductile materials. Though engineering stress-strain diagrams are often used for their convenience and accessibility, they can sometimes fall short in accuracy, particularly when dealing with large strain values.
In contrast, true stress offers a more precise portrayal. It is computed by dividing the...
In contrast, true stress offers a more precise portrayal. It is computed by dividing the...
848
Peptide Bonds
83.0K
A peptide bond covalently attaches amino acids through a dehydration reaction. One amino acid's carboxyl group and another amino acid's amino group combine, releasing a water molecule. The resulting bond is the peptide bond. The products that such linkages form are peptides. As more amino acids join this growing chain, the resulting chain is a polypeptide. Each polypeptide has a free amino group at one end. This end has the N-terminal, or the amino-terminal, and the other end has a free...
83.0K
Protein Organization
157.7K
Overview
157.7K
Chemical Formulas
61.2K
A chemical formula presents information about the proportions of atoms constituting a particular chemical compound or molecule, mainly using symbols of elements and numbers. At times other symbols, such as dashes, parentheses, brackets, commas, plus, and minus signs, are also used. A chemical formula can be one of three types – molecular, empirical, and structural.
61.2K
Protein and Protein Structure
87.6K
Proteins are one of the most abundant organic molecules in living systems and have the most diverse range of functions of all macromolecules. Proteins may be structural, regulatory, contractile, or protective. They may serve in transport, storage, or membranes; or they may be toxins or enzymes. Their structures, like their functions, vary greatly. They are all, however, amino acid polymers arranged in a linear sequence.
A protein's shape is critical to its function. For example, an enzyme...
A protein's shape is critical to its function. For example, an enzyme...
87.6K
Space Trusses
1.3K
A space truss is a three-dimensional counterpart of a planar truss. These structures consist of members connected at their ends, often utilizing ball-and-socket joints to create a stable and versatile framework. The space truss is widely used in various construction projects due to its adaptability and capacity to withstand complex loads.
At the core of a space truss lies the fundamental unit known as the tetrahedron. This structure is composed of six members that form a three-dimensional shape...
At the core of a space truss lies the fundamental unit known as the tetrahedron. This structure is composed of six members that form a three-dimensional shape...
1.3K


