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相关概念视频

Amino Acid Catabolism01:18

Amino Acid Catabolism

1
Microorganisms rely on proteins as an essential carbon and energy source, particularly in environments with limited polysaccharides or lipids. However, proteins are too large to cross the plasma membrane unaided, necessitating enzymatic degradation. Microbes secrete extracellular proteases and peptidases that hydrolyze proteins into peptides, which can then be transported across the membrane. Once inside the cell, intracellular proteases degrade these peptides into free amino acids, which...
1
Amino Acid Biosynthetic Pathways01:29

Amino Acid Biosynthetic Pathways

3
Amino acid biosynthesis is essential for cell growth, protein synthesis, and metabolic regulation. Cells generate essential and non-essential amino acids from metabolic intermediates to sustain vital biological functions. These intermediates originate from key metabolic pathways: glycolysis, the tricarboxylic acid (TCA) cycle, and the pentose phosphate pathway. Important precursors include α-ketoglutarate, pyruvate, oxaloacetate, phosphoenolpyruvate, and erythrose-4-phosphate, which...
3
Amines to Amides: Acylation of Amines01:19

Amines to Amides: Acylation of Amines

2.4K
Various carboxylic acid derivatives (such as acid chlorides, esters, and anhydrides) can be used for the acylation of amines to yield amides. The reaction requires two equivalents of amines. The first amine molecule functions as a nucleophile and attacks the carbonyl carbon to produce a tetrahedral intermediate. This is followed by the loss of the leaving group and restoration of the C=O bond.
Next, the second equivalent of amine serves as a Brønsted base and deprotonates the quaternary...
2.4K
Phase II Reactions: Acetylation Reactions01:24

Phase II Reactions: Acetylation Reactions

188
Acetylation, a phase II biotransformation reaction, introduces an acetyl group to drugs or their metabolites. Acetyltransferase enzymes facilitate this reaction, which resembles α-amino acid conjugation due to the addition of a functional group to the drug molecule.
The substrates for acetylation are typically drugs or their metabolites with an amino, sulfonamide, or hydrazine functional group. Acetylation can occur at several points in the drug molecule, including primary, secondary, and...
188
Phase II Reactions: Sulfation and Conjugation with α-Amino Acids01:19

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

178
Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
178
Amides to Carboxylic Acids: Hydrolysis01:28

Amides to Carboxylic Acids: Hydrolysis

3.1K
Amides can undergo either acid-catalyzed hydrolysis or base-promoted hydrolysis through a typical nucleophilic acyl substitution. Each hydrolysis requires severe conditions.
Acid-catalyzed hydrolysis:
Hydrolysis of amides under acidic conditions yields carboxylic acids. Since the reaction occurs slowly, hydrolysis requires the conditions of heat.
The mechanism begins with the protonation of the carbonyl oxygen by the acid catalyst. The protonation makes the amide carbonyl carbon more...
3.1K

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Updated: Jun 7, 2025

Solid Phase Synthesis of a Functionalized Bis-Peptide Using "Safety Catch" Methodology
11:42

Solid Phase Synthesis of a Functionalized Bis-Peptide Using "Safety Catch" Methodology

Published on: May 15, 2012

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生物催化性氨基酸功能化

Mark R Petchey1, Pascal Schneider1, Lucy A Harwood1

  • 1Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.

ChemMedChem
|November 14, 2024
PubMed
概括

酶合成为新型非正规氨基酸 (ncAA) 提供了一条强大的途径. 本综述强调了酶功能化的进步,以产生各种ncAAs,这对于药物发现至关重要.

科学领域:

  • 合成化学 合成化学
  • 生物技术是生物技术.
  • 药品化学 药品化学 是一个

背景情况:

  • 合成化学的进步对于开发新的治疗方式至关重要.
  • 非规范性氨基酸 (ncAAs) 提供了一种超出标准氨基酸的方法来优化类药物特性.
  • 目前ncAAs的合成方法包括定制化学合成或使用化学试剂或酶直接修改母化合物.

研究的目的:

  • 审查最近在氨基酸的酶功能化的进展.
  • 以突出使用酶方法生产各种非正规氨基酸 (ncAAs).
  • 为了强调这些进展对药物发现管道的重要性.

主要方法:

  • 关于氨基酸酶功能化的文献综述.
  • 专注于利用酶直接修改氨基酸的方法.
  • 探索各种合成途径以获得非正规氨基酸 (ncAAs).

主要成果:

  • 在合成非正规氨基酸 (ncAAs) 的酶方法方面取得了重大进展.
  • 酶方法提供了高效和特定的途径,以广泛的修改氨基酸.
  • 这些方法补充了传统的化学合成,扩大了药物化学家的工具包.
关键词:
这是一个C-C合器.在C−H激活过程中.氨基酸是氨基酸中的一种.生物催化剂的生物催化剂酸是一种酸.

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Enzymatic Cascade Reactions for the Synthesis of Chiral Amino Alcohols from L-lysine
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Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function
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Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function

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结论:

  • 酶功能化代表了生产非正规氨基酸 (ncAAs) 的关键创新.
  • 这些合成策略的开发对于基于的治疗方法的进步至关重要.
  • 酶合成的持续研究将通过提供新的分子构建块来加速药物发现过程.