多肽噬菌体展示

噬菌体展示技术已被广泛地应用于生物学研究的各个方面.利用它可融合表达多肽、蛋白质结构域和蛋白质.尤其是多肽噬菌体展示,已被作为一种便利的研究工具去发现和研究那些与受体、酶、凝集素、抗体、核酸以及其他生物分子亲和的多肽配基和酶的底物专一性,该技术在药物的发现,疫苗的设计等医学领域也有着潜在的应用价值.     

Histamine H3 receptor antagonists: preclinical promise for treating obesity and cognitive disorders

The histamine H3 receptor is an attractive G protein-coupled receptor drug target that regulates neurotransmission in the central nervous system and plays a role in cognitive and homeostatic functions. Drug discovery efforts by numerous pharmaceutical companies have focused on the preclinical development of H3 receptor antagonists for the potential treatment of attention-deficit hyperactivity disorder, dementias, schizophrenia, as well as obesity and sleep disorders. This receptor exhibits molecular, pharmacological, and functional heterogeneity that informs the preclinical development of effective antagonists. Herein, we describe the biological and chemical implications for developing H3 receptor antagonists and their therapeutic potential as disclosed through animal models of cognition, sleep, and obesity.     

Application of QbD Principles for the Evaluation of Empty Hard Capsules as an Input Parameter in Formulation Development and Manufacturing

Understanding the product and process variable on the final product performance is an essential part of the quality-by-design (QbD) principles in pharmaceutical development. The hard capsule is an established pharmaceutical dosage form used worldwide in development and manufacturing. The empty hard capsules are supplied as an excipient that is filled by pharmaceutical manufacturers with a variety of different formulations and products. To understand the potential variations of the empty hard capsules as an input parameter and its potential impact on the finished product quality, a study was performed investigating the critical quality parameters within and in between different batches of empty hard gelatin capsules. The variability of the hard capsules showed high consistency within the specification of the critical quality parameters. This also accounts for the disintegration times, when automatic endpoint detection was used. Based on these data, hard capsules can be considered as a suitable excipient for product development using QbD principles.     

Saponins and their role in biological processes in plants

Saponins are steroid and triterpenoid glycosides that display diverse biological activities. The wide-spread occurrence in plants as well as the potential for pharmaceutical application has led to saponin extraction and identification in numerous species. Although these efforts are important to extend our knowledge of naturally occurring saponin structures, recent attention has been given to the biosynthesis and distribution in plants. In this review, we present recent advances on saponin production and distribution and highlight studies showing effects on the growth and development.     

Artificial microbial consortia for bioproduction processes

The application of artificial microbial consortia for biotechnological production processes is an emerging field in research as it offers great potential for the improvement of established as well as the development of novel processes. In this review, we summarize recent highlights in the usage of various microbial consortia for the production of, for example, platform chemicals, biofuels, or pharmaceutical compounds. It aims to demonstrate the great potential of co-cultures by employing different organisms and interaction mechanisms and exploiting their respective advantages. Bacteria and yeasts often offer a broad spectrum of possible products, fungi enable the utilization of complex lignocellulosic substrates via enzyme secretion and hydrolysis, and microalgae can feature their abilities to fixate CO₂ through photosynthesis for other organisms as well as to form lipids as potential fuelstocks. However, the complexity of interactions between microbes require methods for observing population dynamics within the process and modern approaches such as modeling or automation for process development. After shortly discussing these interaction mechanisms, we aim to present a broad variety of successfully established co-culture processes to display the potential of artificial microbial consortia for the production of biotechnological products.     

Strategies for biomarker discovery in fibrotic disease

The discovery and development of biomarkers for fibrotic diseases have potential utility in clinical decision-making as well as in pharmaceutical research and development. This review describes strategies for identifying diagnostic, prognostic and theranostic biomarkers. A range of technologies and platforms for biomarker discovery are highlighted, including several with specific relevance for fibrosis. Some challenges specific to fibrotic diseases are outlined including; benchmarking biomarkers against imperfect clinical measures of fibrosis, the complexity resulting from diverse aetiologies and target organs, and the availability of samples (including biopsy) from well-characterised patients with fibrotic disease. To overcome these challenges collaboration amongst clinical specialities as well as between academia and industry is essential. This article is part of a Special Issue entitled: Fibrosis: Translation of basic research to human disease.     

2015 年江苏省医药产业发展报告

江苏省作为传统医药大省,是全国医药产业发展的重要组成部分。通过资料查询,从产业规模与体系、研发创新、产业潜能、人 才队伍、科研机构和专利发明等多方位,分析江苏省医药产业发展现状,并与其他医药产业重点省份进行比较,揭示目前全省医药产业 发展中的主要问题所在,为全省医药产业健康发展建言献策。     

医药 CRO 专题报告——蓝海市场，强者恒强

随着全球制药企业研发投资成本加大、研发周期变长、研发成功率降低,作为社会分工专业化的产物,CRO 企业凭借其低成本、高效率、 多服务的特点,快速发展,且服务范畴已涵盖药物研发的整个过程,成为医药研发产业链中不可缺少的环节。报告采用文献调研、数据库检索、 数据统计与分析等定性定量研究方法,从发展概况、发展策略、竞争格局、企业布局等角度对国内外医药 CRO 领域进行多角度、多层次的 分析,旨在为相关企业确定产品研发思路、制定市场策略提供线索和参考。     

Zipper interacting protein kinase (ZIPK): function and signaling

Zipper interacting protein kinase (ZIPK), also known as death associated protein kinase 3, is a serine/threonine kinase that mediates variety of cell functions. The major biologic function of ZIPK is considered to be the regulation of apoptosis and smooth muscle contraction. Recently, several other functions of ZIPK have been gradually clarified. In this review article, we summarized the recent findings on ZIPK function and ZIPK-related cell signaling. We propose that ZIPK is a potential future target for the development of pharmaceutical therapy for cancer as well as cardiovascular diseases.     

Enantiomeric separation and determination of absolute stereochemistry of asymmetric molecules in drug discovery: building chiral technology toolboxes

The application of Chiral Technology, or the (extensive) use of techniques or tools for the determination of absolute stereochemistry and the enantiomeric or chiral separation of racemic small molecule potential lead compounds, has been critical to successfully discovering and developing chiral drugs in the pharmaceutical industry. This has been due to the rapid increase over the past 10-15 years in potential drug candidates containing one or more asymmetric centers. Based on the experiences of one pharmaceutical company, a summary of the establishment of a Chiral Technology toolbox, including the implementation of known tools as well as the design, development, and implementation of new Chiral Technology tools, is provided.     

Bioactive phenolic compounds: production and extraction by solid-state fermentation. A review

Interest in the development of bioprocesses for the production or extraction of bioactive compounds from natural sources has increased in recent years due to the potential applications of these compounds in food, chemical, and pharmaceutical industries. In this context, solid-state fermentation (SSF) has received great attention because this bioprocess has potential to successfully convert inexpensive agro-industrial residues, as well as plants, in a great variety of valuable compounds, including bioactive phenolic compounds. The aim of this review, after presenting general aspects about bioactive compounds and SSF systems, is to focus on the production and extraction of bioactive phenolic compounds from natural sources by SSF. The characteristics of SSF systems and variables that affect the product formation by this process, as well as the variety of substrates and microorganisms that can be used in SSF for the production of bioactive phenolic compounds are reviewed and discussed.     

2015年度中国医药市场发展蓝皮书——产业经济部分 （ Ⅰ ）

从产业经济角度,包括医药工业总产值、医药工业销售收入、医药工业盈利水平、医药流通行业销售规模、医药商业效益水平、     

Polypharmacology and supercomputer-based docking: opportunities and challenges

Polypharmacology, the ability of drugs to interact with multiple targets, is a fundamental concept of interest to the pharmaceutical industry in its efforts to solve the current issues of the rise in the cost of drug development and decline in productivity. Polypharmacology has the potential to greatly benefit drug repurposing, bringing existing pharmaceuticals on the market to treat different ailments quicker and more affordably than developing new drugs, and may also facilitate the development of new, potent pharmaceuticals with reduced negative off-target effects and adverse side effects. Present day computational power, when combined with applications such as supercomputer-based virtual high-throughput screening (docking) will enable these advances on a massive chemogenomic level, potentially transforming the pharmaceutical industry. However, while the potential of supercomputing-based drug discovery is unequivocal, the technical and fundamental challenges are considerable.     

Biological activities and potential health benefits of bioactive peptides derived from marine organisms

Marine organisms have been recognized as rich sources of bioactive compounds with valuable nutraceutical and pharmaceutical potentials. Recently, marine bioactive peptides have gained much attention because of their numerous health beneficial effects. Notably, these peptides exhibit various biological activities such as antioxidant, anti-hypertensive, anti-human immunodeficiency virus, anti-proliferative, anticoagulant, calcium-binding, anti-obesity and anti-diabetic activities. This review mainly presents biological activities of peptides from marine organisms and emphasizing their potential applications in foods as well as pharmaceutical areas.     

单抗药物专题报告——走过孕育期，收获正当时（Ⅱ）

单抗药物以靶向性强、特异性高、副反应小等优势在癌症、自身免疫性疾病等治疗领域取得了快速发展，成为医药行业增速最快的 细分领域。报告采用文献调研、数据库检索、数据统计与分析等定性定量研究方法，从竞争优势、应用领域、给药剂型、产业现状、成长 路径等角度对国内外单抗药物领域进行多角度、多层次的分析，旨在为相关医药企业明确发展方向、确定产品研发思路及制定市场策略提 供参考。     

单抗药物专题报告——走过孕育期，收获正当时（Ⅰ）

单抗药物以靶向性强、特异性高、副反应小等优势在癌症、自身免疫性疾病等治疗领域取得了快速发展,成为医药行业增速最快的 细分领域。报告采用文献调研、数据库检索、数据统计与分析等定性定量研究方法,从竞争优势、应用领域、给药剂型、产业现状、成长 路径等角度对国内外单抗药物领域进行多角度、多层次的分析,旨在为相关医药企业明确发展方向、确定产品研发思路及制定市场策略提 供参考。     

2014年江苏省医药产业发展报告

江苏省作为传统医药大省,是全国医药产业发展的重要组成部分,但仍存在诸多不足,极大地影响了其可持续发展。通过资料查询, 将江苏省与山东、河南、广东、吉林、浙江、湖北等医药产业重点省份进行比较,多方位分析江苏省医药产业发展现状,揭示眼下全省 医药产业发展中的主要问题所在,为全省医药产业健康发展建言献策     

Recent Updates on Corals from Nephtheidae

Marine natural products display a wide range of biological activities, which play a vital role in the innovation of lead compounds for the drug development. Soft corals have been ranked at the top in regard to the discovery of bioactive metabolites with potential pharmaceutical applications. Many of the isolated cembranoids revealed diverse biological activities, such as anticancer, antidiabetic and anti‐osteoporosis. Likewise, sterols from soft corals exhibited interesting biological potential as anti‐inflammatory, antituberculosis and anticancer. Consequently, investigating marine soft corals will definitely lead to the discovery of a large number of chemically varied secondary metabolites with countless bioactivities for possible applications in medicine and pharmaceutical industry. This review provides a complete survey of all metabolites isolated from the family Nephtheidae, from 2011 until November 2018, along with their natural sources and biological potential whenever possible.     

Recent applications of machine learning in medicinal chemistry

In recent decades, artificial intelligence and machine learning have played a significant role in increasing the efficiency of processes across a wide spectrum of industries. When it comes to the pharmaceutical and biotechnology sectors, numerous tools enabled by advancement of computer science have been developed and are now routinely utilized. However, there are many aspects of the drug discovery process, which can further benefit from refinement of computational methods and tools, as well as improvement of accessibility of these new technologies. In this review, examples of recent developments in machine learning application are described, which have the potential to impact different parts of the drug discovery and development flow scheme. Notably, new deep learning-based approaches across compound design and synthesis, prediction of binding, activity and ADMET properties, as well as applications of genetic algorithms are highlighted.