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1、Potent inhibition of human leukocyte elastase by 1,2,5-thiadiazolidin-3-one 1,1 dioxide-based sulfonamide derivative

摘要:The design, synthesis, and in vitro biochemical evaluation of a class of mechanism-based inhibitors of human leukocyte elastase (HLE) that incorporate in their structure a 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold with appropriate recognition and reactivity elements appended to it is described. The synthesized compounds were found to be efficient, time-dependent inhibitors of HLE. The interaction of the inhibitors with HLE is postulated to lead to the formation of a highly reactive N-sulfonyl imine (a Michael acceptor) that arises from an enzyme-induced sulfonamide fragmentation cascade. Subsequent reaction ultimately leads to the formation of a relatively stable acyl enzyme. The results cited herein demonstrate convincingly the superiority of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold over other scaffolds (e.g., saccharin) in the design of inhibitors of (chymo)trypsin-like serine proteases.Click on the DOI link below to access the article (may not be free). NHLBI NIH HHS
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2、Potential protease inhibitors based on a functionalized cyclic sulfamide scaffold

摘要:Exploratory studies related to the design and synthesis of functionalized cyclic sulfamides (I) as potential inhibitors of proteolytic enzymes were carried out. The structural motif and three diversity sites embodied in the scaffold render it amenable to combinatorial parallel synthesis and the facile generation of lead discovery prospecting libraries. The scaffold was readily assembled starting with (DL) serine methyl ester, and a series of compounds was generated and screened against human leukocyte elastase. Modification of the P(1) recognition element, believed to be accommodated at the primary specificity site (S(1) subsite) of the enzyme, yielded compounds that inhibited the enzyme by an apparent hyperbolic partial mixed-type inhibition.Click on the DOI link below to access the article (may not be free). NHLBI NIH HHS
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3、Toward High-Throughput Genotyping: Dynamic and Automatic Software for Manipulating Large-Scale Genotype Data Using Fluorescently Labeled Dinucleotide Marker

摘要:To efficiently manipulate large amounts of genotype data generated with fluorescently labeled dinucleotide markers, we developed a Microsoft Access database management system, named GenoDB. GenoDB offers several advantages. First, it accommodates the dynamic nature of the accumulations of genotype data during the genotyping process; some data need to be confirmed or replaced by repeat lab procedures. By using GenoDB, the raw genotype data can be imported easily and continuously and incorporated into the database during the genotyping process that may continue over an extended period of time in large projects. Second, almost all of the procedures are automatic, including autocomparison of the raw data read by different technicians from the same gel, autoadjustment among the allele fragment-size data from cross-runs or cross-platforms, autobinning of alleles, and autocompilation of genotype data for suitable programs to perform inheritance check in pedigrees. Third, GenoDB provides functions to track electrophoresis gel files to locate gel or sample sources for any resultant genotype data, which is extremely helpful for double-checking consistency of raw and final data and for directing repeat experiments. In addition, the user-friendly graphic interface of GenoDB renders processing of large amounts of data much less labor-intensive. Furthermore, GenoDB has built-in mechanisms to detect some genotyping errors and to assess the quality of genotype data that then are summarized in the statistic reports automatically generated by GenoDB. The GenoDB can easily handle >500,000 genotype data entries, a number more than sufficient for typical whole-genome linkage studies. The modules and programs we developed for the GenoDB can be extended to other database platforms, such as Microsoft SQL server, if the capability to handle still greater quantities of genotype data simultaneously is desired.
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4、Analysing China : commemorating EAI's 5th anniversary 2002

5、Behind China's World Trade Organization agreement with the USA 2001

6、The political economy of China's reforms : national and provincial policies toward non-state industry 2000

7、Special issue: Managing China energy sector between the market and the state 2015

8、藉由通話圖分割改善電信業批價系統的效能 = Improve performance of telecommunication billing system by call graph partitioning

9、The domestic sources of China's foreign policy : regimes, leadership, priorities and proce 2010

10、China's regional oil global (II) : reducing reliance on the Middle East and the Malacca Strait 2005

11、Managing China's energy sector : between the market and the state 2015

12、The Politics of Agricultural Cooperativization in China : Mao, Deng Zihui and the High Tide of 1955 1993

13、China's cultural rise in the context of its peaceful rise (I) 2006

14、Legislative activism and effectiveness of provincial delegates at the 1988 National People's Congress (NPC)/ Hongyi Lai 2001

摘要:從書:EAI working paper., East Asian Institute ;, 69 23, V Seiten
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15、Southeast Asian Studies in China 2006

摘要:1 online resource This book, a project of the ASEAN-China Study Programme of ISEAS, is designed to promote a better understanding between the people of the two regions as China continues to exert a dominant political and economic presence in Southeast Asia. Needless to say, scholars and academics from both sides have a significant role to play in terms of creating greater awareness of each other through research, workshops, and conferences. Whilst many universities and research institutes in the ASEAN region are conducting studies on various aspects of China, it is equally important for the Chinese counterparts to be fully engaged in Southeast Asian Studies in order to deepen their knowledge of the region for mutual benefit. The book traces the development of Southeast Asian Studies in China, discusses the current status of these studies, examines the problems encountered in the pursuit of these studies, and attempts to evaluate their prospects in the years ahead.
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16、Rule by virtue : Jiang Zemin's new moral order for the party 2001

17、Analysing China : East Asian Institute, Singapore 2002

18、China-ASEAN relations : economic and legal dimension 2006

19、Damage control : the Chinese Communist Party in the Jiang Zemin era 2003

20、Religious revival in China 2001

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