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相关概念视频

Ligand Binding and Linkage00:49

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence the...
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...
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...
Allosteric Proteins-ATCase01:19

Allosteric Proteins-ATCase

Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to  N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
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...
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:

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Highly Enantioselective Oxidation Reactions Using a Tetradentate Mn(II) Catalyst Based on (<i>S</i>,<i>S</i>)-1,2-Diaminocyclohexane.

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Updated: Jul 5, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

乔治,阿博和其结构性亲属的酶选择性合成. 对分子层面的嗅觉理解的相关性.

Sungwoo Hong1, E J Corey

  • 1Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA.

Journal of the American Chemical Society
|January 26, 2006
PubMed
概括

乔治和阿博,木质的气味,是合成的enantioselectively. 研究揭示了木质气味感知和与嗅觉受体结合的结构要求,支持了组合模型.

科学领域:

  • 有机化学 有机化学
  • 嗅觉神经科学 嗅觉神经科学
  • 计算化学的计算化学

背景情况:

  • 像乔治和阿博龙这样的木质气味剂是香水和风味行业的关键组成部分.
  • 了解嗅觉的分子基础,特别是气味与嗅觉受体的相互作用,对于开发新的感官体验至关重要.
  • 酵素选择性在气味感知中起着重要作用,因为不同的酵素可以引起不同的嗅觉反应.

研究的目的:

  • 为了合成georgyone (1) 和arborone (2) 的enantioselectively,以及他们的enantiomers.
  • 为了合成1和2的结构亲属,以enantioselectively探测分子结合细节.
  • 阐明木质气味的结构要求,并了解这些气味剂与嗅觉G蛋白结合受体 (GPCRs) 的结合.

主要方法:

  • 乔治,阿博及其类型的酶选择性合成.
  • 对木质气味感知的结构-活动关系的研究.
  • 用小鼠嗅觉受体进行结合性研究,以确定激活的受体.

主要成果:

  • 成功地对乔治 (1) 和阿博 (2) 以及它们的反体进行了反选择性合成.
  • 鉴定木质气味的关键结构特征,包括绝对配置和甲基组方向.

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

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X-Ray Crystallography to Study the Oligomeric State Transition of the Thermotoga maritima M42 Aminopeptidase TmPep1050

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  • 证明气味剂1和2与至少10个小鼠嗅觉受体结合.

    • 结论:

    • 甲基组的绝对配置和空间排列对于木质气味至关重要.
    • 乔治和阿博与多个嗅觉受体的结合支持了嗅觉感知的组合模型.
    • 这项研究提供了对嗅觉GPCRs中的气味受体相互作用和潜在结合模式的洞察.