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相关概念视频

In-vitro Mutagenesis01:16

In-vitro Mutagenesis

To learn more about the function of a gene, researchers can observe what happens when the gene is inactivated or “knocked out,” by creating genetically engineered knockout animals. Knockout mice have been particularly useful as models for human diseases such as cancer, Parkinson’s disease, and diabetes.
Cooperative Allosteric Transitions01:58

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...
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein.
Regulation of Metabolism01:19

Regulation of Metabolism

Cellular needs and conditions vary from cell to cell and change within individual cells over time. For example, the required enzymes and energetic demands of stomach cells are different from those of fat storage cells, skin cells, blood cells, and nerve cells. Furthermore, a digestive cell works much harder to process and break down nutrients during the time that closely follows a meal compared with many hours after a meal. As these cellular demands and conditions vary, so do the amounts and...
Cooperative Allosteric Transitions01:58

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...
Transduction01:16

Transduction

Among the three main modes of HGT—transformation, conjugation, and transduction—transduction is unique in that it is mediated by bacteriophages, or bacterial viruses.Transduction occurs in two ways. Generalized transduction occurs during the lytic cycle of a bacteriophage infection. In this process, bacteriophages infect bacterial cells, replicate within them, and ultimately cause cell lysis, releasing newly assembled virions. Occasionally, random fragments of the bacterial genome are...

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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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分子杂交策略用于调整生物活性的功能.

Cibele Nicolaski Pedron1,2, Marcelo Der Torossian Torres3,4,5, Cyntia Silva Oliveira2

  • 1Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Santo André, SP, 09210580, Brazil.

Communications biology
|October 19, 2023
PubMed
概括

杂化产生了具有毒性降低的新型抗微生物 (AMP). 这一战略增强了抗微生物和抗等离子体活性,为开发更安全的治疗方法提供了有前途的途径.

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科学领域:

  • 生物化学 生化学
  • 药用化学 医学化学
  • 分子生物学分子生物学

背景情况:

  • 抗微生物 (AMP) 对于天生的免疫力至关重要,但往往表现出毒性,限制了治疗应用.
  • 修改AMP的物理化学性质可能会降低毒性,同时提高抗微生物药物的有效性.
  • 开发更安全,更有效的抗微生物药物仍然是医学界的一个重大挑战.

研究的目的:

  • 通过结合不同天然的序列来设计和合成新型混合抗菌 (hAMPs).
  • 评估设计的hAMPs的抗微生物活性,抗等离子体效应和人类细胞毒性.
  • 证明杂化作为一种创建改进生物活性分子的策略的有效性.

主要方法:

  • 从有毒的VmCT1与其他四种自然存在的抗微生物混合化序.
  • 产生七种合成生物活性变体 (hAMPs).
  • 对抗红细胞的抗微生物活性 (3.1-128μmol L-1) 和抗血性活性 (0.8μmol L-1) 的评估.

主要成果:

  • 所有七个设计的hAMP都保持了结构完整性.
  • 合成变种表现出显著增加的抗菌活性.
  • 五种hAMP显示出强烈的抗等离子体活性,对红细胞的毒性最小.

结论:

  • 杂化是一种有效的策略,用于生成具有改进性质的新生物活性分子.
  • 这种方法成功地降低了毒性,同时增强了抗微生物和抗等离子体活动.
  • 开发的hAMP代表了未来针对微生物感染和疟疾的治疗开发的有希望的候选人.