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PENTENYL GLYCOSIDES--TRANSFORMATIONS AT ANOMERIC CENTER

PENTENYL GLYCOSIDES--TRANSFORMATIONS AT ANOMERIC CENTER
戊烯基糖苷——异头中心的转化
批准号:
2546017
负责人:
Bertram Oliver Fraser-Reid
金额:
$16.02万
依托单位国家:
美国
项目类别:
财政年份:
1996
资助国家:
美国
项目状态:
已结题
起止时间:
1996-09-30 至 1999-08-31

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项目成果

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中文摘要
翻译
描述:首席调查员表示, 该项目源于这样一个事实,即在生物聚合物的三大家族中, 蛋白质、寡核苷酸和寡糖,最后一种是最差的 理解是因为它们的隔离性、结构防护性,以及(最重要的) 实验室合成的难度和要求远远超过了 另外两个人的案子。他指出,然而,已经取得了长足的进步 在隔震和结构抗震技术中,这使得许多 这些低聚糖完好无损,现在很明显它们的 结构通常具有令人生畏的复杂性。他进一步表示, 对于另外两种生物聚合物,蛋白质和寡核苷酸,澄清 它们的生物调节作用随着 使它们和/或其类似物易于获得的合成方法 结构活性相关性。需要注意的是,低聚糖通常 作为细胞表面的主要识别剂,现在被广泛使用 理解,这一步骤是后续关键事件的前奏,例如 酶解、细胞穿透等,因此细菌、病毒、(许多) 荷尔蒙、其他细胞等必须参与这第一步,因此 可以想象,不良事件(如细菌感染) 通过使用模仿来否定识别步骤来防止。它是 进一步指出,另一方面,有益的互动,如在 在荷尔蒙的情况下,可以方便,从而提高认知度。 首席调查员表示,这些有远见的健康相关人员 好处最终依赖于随时可以获得合成低聚糖,或者 用于生化评估的片段及其修饰 构效关系研究。他指出,自从他们在 他的实验室六年前,正戊烯基苷已被证明是 多种寡糖和低聚糖的多功能合成前体 糖蛋白以及由此建立的可信度,他 设想极大地扩展他们的综合潜力来解决问题 与重大健康危害有关。据介绍,这些例子 包括与利什曼病有关的脂多糖和 A类脂类内毒素及其开发探索性研究 这些目标的方法是提案的一个重要部分。
英文摘要
DESCRIPTION: The principal investigator states that the importance of the project stems from the fact that of the three major families of biopolymers, proteins, oligonucleotides and oligosaccharides, the last is the least well understood because their isolation, structure-proof, and (above all) their laboratory syntheses have been far more difficult and demanding than in the case of the other two. He notes that however, great strides have been made in the techniques of isolation and structure-proof which has made many of these oligosaccharides available intact, and it is now clear that their structures are usually of daunting complexity. He further indicates that with the other two biopolymers, proteins and oligonucleotides, clarification of their biological regulatory roles accelerated markedly with the advent of synthetic methods that made them and/or their analogs, readily available for structure activity correlations. It is noted that oligosaccharides usually being the primary recognition agents on cell surfaces is now widely appreciated, this step being a prelude to subsequent critical events such as enzymolysis, cell penetration, etc and that thus bacteria, viruses, (many) hormones, other cells, etc. must engage in this first step, and hence undesirable events (such as bacterial infection) can conceivably be prevented by the use of mimics to negate the recognition step. It is further noted that on the other hand, beneficial interactions, as in the case of hormones, can be facilitated so as to enhance recognition. The principal investigator states that these visionary health-related benefits rely ultimately on ready access to synthetic oligosaccharides, or fragments and modifications thereof for biochemical evaluation and structure-activity investigations. He notes that since their discovery in his laboratory six years ago, n-pentenyl glycosides have proved to be versatile synthetic precursors for several oligosaccharides and glycoproteins and that with their credibility thereby established, he envisages greatly extending their synthetic potential to address problems associated with major health hazards. It is stated that examples of these include the lipopolysaccharides associated with Leishmaniasis and the endotoxin from lipid A and that exploratory studies aimed at developing methodology for these targets is an important segment of the proposal.
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Laboratory Syntheses of Mycobacterial tuberculosis LAM Prototypes
PENTENYL GLYCOSIDES--TRANSFORMATIONS AT ANOMERIC CENTER
PENTENYL GLYCOSIDES--TRANSFORMATIONS AT ANOMERIC CENTER
PENTENYL GLYCOSIDES--TRANSFORMATIONS AT ANOMERIC CENTER
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