相关实验视频
Updated: Jul 16, 2026

09:26
Synthesis and Characterization of Supramolecular Colloids
Published on: April 22, 2016
使用 stilbene 模拟物测试 HTI-286 与素的相互作用
Mei-Chu Lo1, Ann Aulabaugh, Girija Krishnamurthy
1Biophysics/Enzymology-Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA. lom@wyeth.com
Journal of the American Chemical Society
|August 12, 2004
概括
这项研究显示,一种抗瘤剂HTI-286以1:1的比例结合素单体,形成环状结构. 这种结合不会与菌素部位重叠,为新的癌症疗法提供了洞察力.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 药理学 药理学是指药理学的学科.
背景情况:
- HTI-286是一种具有强烈抗瘤活性的合成hemiasterlin模拟物.
- HTI-286通过诱导氨酸寡合化而起作用.
研究的目的:
- 为了研究HTI-286与管氨酸的结合史泰基测量.
- 为了确定HTI-286在突结合期间的结合部位.
主要方法:
- 合成一种含有stilbene的HTI-286类似物.
- 分析超离心,以量化抑制剂与素寡合体的结合.
主要成果:
- 在抑制剂:蛋白质比 ≥ 1 的情况下,HTI-286 模拟物会以 1:1 的结合史泰基几何学 (抑制剂:图林单体) 诱导图林环形成.
- 在抑制剂:蛋白质比率 < 1 时,氨酸形成具有 < 1:1 结合史泰基度的中间体.
- 没有检测到抑制剂和图林单体之间的稳定复合物.
- HTI-286类型的结合部位与菌素结合部位不重叠.
结论:
- 在较高度下,HTI-286以1:1的固态度结合素单体,形成环状结构.
- 与素相比,这种独特的结合部位表明了协同或替代治疗策略的潜力.
相关概念视频
Stability of Substituted Cyclohexanes
This lesson discusses the stability of substituted cyclohexanes with a focus on energies of various conformers and the effect of 1,3-diaxial interactions.
The two chair conformations of cyclohexanes undergo rapid interconversion at room temperature. Both forms have identical energies and stabilities, each comprising equal amounts of the equilibrium mixture. Replacing a hydrogen atom with a functional group makes the two conformations energetically non-equivalent.
For example, in...
The two chair conformations of cyclohexanes undergo rapid interconversion at room temperature. Both forms have identical energies and stabilities, each comprising equal amounts of the equilibrium mixture. Replacing a hydrogen atom with a functional group makes the two conformations energetically non-equivalent.
For example, in...
Stereoisomerism of Cyclic Compounds
In this lesson, we delve into the role of ring conformation and its stability, which determines the spatial arrangement and, consequently, the molecular symmetry and stereoisomerism of cyclic compounds. 1,2-Dimethylcyclohexane is used as a case study to evaluate the possible number of stereoisomers. Here, given the multiple (n = 2) chiral centers, there are 2n = 4 possible configurations that lack a plane of symmetry, as the ring skeleton exists in a non-planar chair conformation. In addition,...
Directing and Steric Effects in Disubstituted Benzene Derivatives
When disubstituted benzenes undergo electrophilic substitution, the product distribution depends on the directing effect of both substituents. When the directing effects of both substituents reinforce each other, a single product is obtained. For example, bromination of p-nitrotoluene occurs ortho to the methyl group and meta to the nitro group, which is the same position, resulting in a single product. However, if the directing effects of the two groups oppose each other, the more strongly...
Stability of Conjugated Dienes
Introduction
A comparison of the enthalpies of hydrogenation of dienes reveals that conjugated dienes release less heat on hydrogenation, rendering them more stable than their nonconjugated analogs.
A comparison of the enthalpies of hydrogenation of dienes reveals that conjugated dienes release less heat on hydrogenation, rendering them more stable than their nonconjugated analogs.
Radical Reactivity: Steric Effects
The presence of electron-donating, electron-withdrawing, or conjugating groups adjacent to a radical center, imparts electronic stabilization to the radicals. Examples of such electronically-stabilized radicals are triphenylmethyl, tetramethylpiperidine‐N‐oxide, and 2,2‐diphenyl‐1‐picrylhydrazyl. These radicals are remarkably stable and are known as persistent radicals. Some of the persistent radicals can even be isolated and purified.
Along with electronic factors, steric factors also account...
Along with electronic factors, steric factors also account...
Radical Substitution: Hydrogenolysis of Alkyl Halides with Tributyltin Hydride
Radical substitution reactions can be used to remove functional groups from molecules. The hydrogenolysis of alkyl halides is one such reaction, where the weak Sn–H bond in tributyltin hydride reacts with alkyl halides to form alkanes. Here, the reagent Bu3SnH yields tributyltin halide as a byproduct.
The bonds formed in this reaction are stronger than the bonds broken, making it energetically favorable. The reaction follows a radical chain mechanism similar to radical halogenation reactions,...
The bonds formed in this reaction are stronger than the bonds broken, making it energetically favorable. The reaction follows a radical chain mechanism similar to radical halogenation reactions,...

