药用氨基酸的应用及其生物催化与生物转化法生产

目的对药用氨基酸的应用及其生物催化与生物转化法生产进展进行综述。方法查阅10余年来有关药用氨基酸的应用及其生物催化与生物转化法生产研究的国内外文献。结果药用氨基酸在疾病治疗和药物合成方面的应用广泛，生物催化和生物转化在药用氨基酸的生产中起的作用越来越重要。结论应加强生物催化和生物转化法制备药用氨基酸的研究。     

药用氨基酸的应用及其生物催化与生物转化法生产

OBJECTIVETo review the development of the applications, biocatalytic synthesis and biotransformation of pharmaceutical amino acids. METHODTo retrospect the domestic and foreign literature about the research on the applications, biocatalytic synthesis and     

生物催化技术在化学制药中的应用研究进展

生物催化技术在化学制药领域得到广泛的应用,部分生物催化技术在化学制药领域的应用已工业化生产。本文拟对生物催化进行简单阐述,并介绍生物催化技术在化学制药领域的应用研究进展。     

酶在有机溶剂中的生物催化性能及其固定化技术

在有机相中，酶具有与其在水相中相同的晶体结构，能够正确折叠和恢复活性，其活性严重依赖于干燥前水相的pH值，并受有机溶剂中水含量的影响。有机介质中水分子的存在对于保持天然蛋白质的活性构象和控制蛋白质表面基团的离子化状态具有重要作用。盐种类及有机介质对有机相中酶催化反应的对映体选择性有重要的影响。酶经固定化后，底物在酶分子间的传质阻力减少，酶活得以增大。固定化酶介质对固定化酶活具有较大的影响。文章还介绍了有机相中固定化酶的新方法。     

离子液体双相体系在生物催化中的应用

综述离子液体双相体系在生物催化中的应用研究进展,介绍其应用特点,并探讨现阶段研究中存在的问题。许多纯酶或全细胞中的酶均能在离子液体或由其与其他溶剂组成的两相体系中保持催化活性,离子液体也因此而成为生物催化反应研究的热点。     

D—氨基酸的生物转化与拆分技术研究的新进展

介绍了Ｄ－氨基酸的存在及其作用,着重综述了Ｄ－氨基酸的生物转化和拆分技术以及在生产制备中的应用。     

生物催化在手性药物制备中的应用

随着生物催化技术的不断发展,应用于手性药物制备过程中的生物催化也越来越广泛。该文仅就近5年来生物催化在手性药物制备中的应用情况进行了综述。     

第3届药用与芳香植物世界大会简介

第3届药用与芳香植物世界大会于2003年2月3～7日在泰国清迈市召开，此会每5年举行一次。来自50多个国家的500多名代表出席了本次大会。会议期间有130个报告、415份墙报和120个展览。大会主题是“生物多样性及药用与芳香植物在科学、技术、贸易和生产领域中的可持续应用”。本次大会由国际药用与芳香植物协会(ICMAP)、     

氨基酸药用现状

氨基酸在医药领域中的应用日益广泛。此文介绍了我国氨基酸药物的发展概况 ,以及有开发前景的几种氨基酸的特殊应用 ,并简述了氨基酸对基因表达的调节作用     

Design,synthesis, and antimalarial evaluation of thiazole-derived amino acids

A series of thiazole-derived N-Boc amino acids were synthesized and evaluated as targeted potential antimalarials against plasmepsins II enzyme of malaria parasite Plasmodium falciparum. All the compounds showed moderate to good activity. Compounds 3f and 3g were found to have highest the 50% inhibitory concentration (IC₅₀) values (3.45 μM and 4.89 μM, respectively) against Plasmodium falciparum. The compounds docked to the active site of plasmepsin II. Most of the compounds were found to interact with the catalytic amino acids ASP34 and ASP214 of plasmepsin II. A good correlation was observed between binding energy and antiparasitic activity of the thiazole derivatives.     

Methods for the synthesis of unnatural amino acids

A wide variety of methods have been used to prepare unnatural amino acids. This review covers methods reported between 2000 and the early part of 2001. Some of the approaches discussed are applications of established methods, but emphasis has been given to new approaches that could be generally applicable to large-scale syntheses, including catalytic reactions such as the Strecker reaction and biological approaches.     

Contribution of poly(amino acids) to advances in pharmaceutical biotechnology

Recently, protein biotechnology generates tremendous impacts in therapeutic products. These products include enzymes, antibodies, hormones, blood factors, growth factors and regulatory factors. Protein, vaccine and gene therapy drugs could be formulated with suitable biomaterials to deliver active agents to their target sites at the right time and maintain therapeutic effects for proper durations. In this review article, we focus on poly(amino acids) or polymerized amino acids for their applications in drug delivery systems, vaccines, and gene therapy. The nomenclatures of poly(amino acids) are briefly introduced to systematically express synthetic polypeptides. In drug delivery systems, we introduce two applications of poly(amino acids) in pharmaceutical biotechnology, either as carriers to facilitate drug delivery, or as biomaterials to be formulated as suitable delivery systems for application in tissue engineering. Many short polypeptides are mapped from antigen motifs and used for vaccination. These poly(amino acids) provide protective effects in animal challenge tests and potential application in vaccine development to be briefly introduced. Finally, some reports related to new developed poly(amino acids) as DNA carriers for achieving gene delivery are also described in the text.     

Microbiological synthesis of L-tryptophan and its related amino acids.

Crystalline tryptophanase from Proteus rettgeri was shown to catalyze the synthesis of L-tryptophan from pyruvate, ammonia and indole, at maximum velocity approaching that of the degradative reaction. Based on the results obtained with the crystalline tryptophanase, an enzymatic method for preparation of L-tryptophan and its related amino acids was developed. The cells of Proteus rettgeri containing high enzymatic activity were used directly as the enzyme. This method is simple and is one of the most economical processes to date for preparing L-tryptophan related amino acids from starting materials: sodium pyruvate, indole and its derivatives.     

他汀类药物中间体的生物催化合成研究进展

他汀类药物是一类重要的降血脂药物,(3R,5S)-二羟基酯是他汀类药物发挥作用的关键结构,也是合成该类药物过程中的重要中间体,因其结构中具有两个手性碳原子,故含有(3R,5S)-二羟基酯结构中间体的制备在某种程度上已成为他汀类药物制备的限速步骤。该文对他汀类药物的类型、作用机制、化学结构和合成路线进行概述。着重对近几年采用生物催化方式制备具有 (3R,5S)-二羟基酯结构中间体的方法进行简述。     

Advances in the synthesis of bioactive unnatural amino acids and peptides

The key role of proteins and amino acids in the structure and function of living matter has stimulated extensive studies. Modified amino acids with enhanced biological activity, proteolitic stability and bioavailability are of increasing interest in protein design and engineering as drug candidates. In the last few years, several efforts have been devoted to the synthesis of amino acids having unusual side chains and unnatural chirality, commonly referred to as "nonproteinogenic" or "unnatural" amino acids, even though some of them can be isolated from natural sources. In this review we describe recent advances in the amino acid side-chain transformations and backbone modifications by oxidative and fluorination procedures.     

扩展氨基酸原料的应用领域,促进氨基酸产业的发展

自1980年我国自行开发的氨基酸输液投放市场以来，先后在中国医药工业公司及中国化学制药工业协会的组织、领导下，开发生产氨基酸原料，为输液配套。特别是从1989年明确提出以实现氨基酸原料国产化为目标，以彻底改变进口氨基酸原料垄断市场的被动局面后，国产氨基酸原料品种不断增加，质量迅速提高，成本大幅度下降，使广大的病患者能够用上质量好、价格低廉的氨基酸输液。     

Solid phase peptide synthesis utilizing 9-fluorenylmethoxycarbonyl amino acids

9-Fluorenylmethoxycarbonyl (Fmoc) amino acids were first used for solid phase peptide synthesis a little more than a decade ago. Since that time, Fmoc solid phase peptide synthesis methodology has been greatly enhanced by the introduction of a variety of solid supports, linkages, and side chain protecting groups, as well as by increased understanding of solvation conditions. These advances have led to many impressive syntheses, such as those of biologically active and isotopically labeled peptides and small proteins. The great variety of conditions under which Fmoc solid phase peptide synthesis may be carried out represents a truly “orthogonal” scheme, and thus offers many unique opportunities for bioorganic chemistry.