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相关概念视频

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...
Inhibitors of Gram-positive Cell Wall Synthesis01:23

Inhibitors of Gram-positive Cell Wall Synthesis

Bacterial cell walls are typically rigid structures composed mainly of peptidoglycan, a mesh-like polymer that provides mechanical strength and maintains cell shape. The synthesis of peptidoglycan is a crucial process in bacterial growth and serves as a primary target for many antibiotics.Mechanism of Action of Beta-Lactam AntibioticsBeta-lactam antibiotics, such as penicillin, inhibit peptidoglycan synthesis in actively growing cells. These antibiotics share a characteristic four-membered...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Peptidoglycan Synthesis01:28

Peptidoglycan Synthesis

Structure of PeptidoglycanPeptidoglycan is a vital structural component of the bacterial cell wall, providing mechanical strength and shape to the cell. It consists of repeating units of two sugars—N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM)—linked by β-1,4 glycosidic bonds. These sugar chains are cross-linked by short peptide chains, forming a mesh-like polymer that surrounds the bacterial plasma membrane.Cytoplasmic Phase – Precursor SynthesisPeptidoglycan biosynthesis begins in...

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相关实验视频

Updated: Jun 5, 2026

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
13:37

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library

Published on: June 20, 2014

全面的模仿药物 普遍的模仿药物

Eunhwa Ko1, Jing Liu, Lisa M Perez

  • 1Department of Chemistry and Laboratory for Molecular Simulation, Texas A&M University, Box 30012, College Station, Texas 77842, United States.

Journal of the American Chemical Society
|December 25, 2010
PubMed
概括
此摘要是机器生成的。

这项研究引入了极简主义的模仿,新的型模拟脚手架,旨在模仿蛋白质二级结构中的氨基酸侧链. 这些通用模仿剂对于高通量选图书馆设计非常有价值.

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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Solid-phase Submonomer Synthesis of Peptoid Polymers and their Self-Assembly into Highly-Ordered Nanosheets
13:42

Solid-phase Submonomer Synthesis of Peptoid Polymers and their Self-Assembly into Highly-Ordered Nanosheets

Published on: November 2, 2011

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Last Updated: Jun 5, 2026

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
13:37

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library

Published on: June 20, 2014

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Solid-phase Submonomer Synthesis of Peptoid Polymers and their Self-Assembly into Highly-Ordered Nanosheets
13:42

Solid-phase Submonomer Synthesis of Peptoid Polymers and their Self-Assembly into Highly-Ordered Nanosheets

Published on: November 2, 2011

科学领域:

  • 药用化学 医学化学
  • 有机化学 有机化学
  • 计算化学计算化学

背景情况:

  • 类仿制药旨在复制的结构和功能.
  • 在二次结构中模仿氨基酸侧链是具有挑战性的,因为有着形状上的惩罚.

研究的目的:

  • 设计能够在任何次要结构中模仿局部氨基酸对的通用peptidomimetic支架.
  • 开发极简主义的模仿,减少了热和热的惩罚.

主要方法:

  • 设计了四种新的型模拟脚手架.
  • 合成具有多种氨基酸侧链的化合物库.
  • 计算建模,以评估合规可访问性.

主要成果:

  • 基于四个支架的型模拟学可以采用模拟各种局部氨基酸侧链组合的构造.
  • 这些支架有效地呈现了与蛋白质二次结构相似的形状的侧链.
  • 对于高通量选图书馆设计的证明实用性.

结论:

  • 开发的极简主义模仿代表了一种普遍的型模仿策略.
  • 这些支架适合生成用于药物发现的各种图书馆.
  • 提交给NIH分子图书馆小分子存储库 (MLSMR) 的数据.