Biofriendly Sol–Gel Processing for the Entrapment of Soluble and Membrane-Bound Proteins: Toward Novel Solid-Phase Assays for High-Throughput Screening

2007 ◽  
Vol 40 (9) ◽  
pp. 827-835 ◽  
Author(s):  
John D. Brennan
Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 1869 ◽  
Author(s):  
Stefano Dugheri ◽  
Alessandro Bonari ◽  
Matteo Gentili ◽  
Giovanni Cappelli ◽  
Ilenia Pompilio ◽  
...  

High-throughput screening of samples is the strategy of choice to detect occupational exposure biomarkers, yet it requires a user-friendly apparatus that gives relatively prompt results while ensuring high degrees of selectivity, precision, accuracy and automation, particularly in the preparation process. Miniaturization has attracted much attention in analytical chemistry and has driven solvent and sample savings as easier automation, the latter thanks to the introduction on the market of the three axis autosampler. In light of the above, this contribution describes a novel user-friendly solid-phase microextraction (SPME) off- and on-line platform coupled with gas chromatography and triple quadrupole-mass spectrometry to determine urinary metabolites of polycyclic aromatic hydrocarbons 1- and 2-hydroxy-naphthalene, 9-hydroxy-phenanthrene, 1-hydroxy-pyrene, 3- and 9-hydroxy-benzoantracene, and 3-hydroxy-benzo[a]pyrene. In this new procedure, chromatography’s sensitivity is combined with the user-friendliness of N-tert-butyldimethylsilyl-N-methyltrifluoroacetamide on-fiber SPME derivatization using direct immersion sampling; moreover, specific isotope-labelled internal standards provide quantitative accuracy. The detection limits for the seven OH-PAHs ranged from 0.25 to 4.52 ng/L. Intra-(from 2.5 to 3.0%) and inter-session (from 2.4 to 3.9%) repeatability was also evaluated. This method serves to identify suitable risk-control strategies for occupational hygiene conservation programs.


2000 ◽  
Vol 22 (5) ◽  
pp. 149-157 ◽  
Author(s):  
Ralf Thiericke

Secondary metabolites from plants, animals and microorganisms have been proven to be an outstanding source for new and innovative drugs and show a striking structural diversity that supplements chemically synthesized compounds or libraries in drug discovery programs. Unfortunately, extracts from natural sources are usually complex mixtures of compounds:: often generated in time consuming and for the most part manual processes. As quality and quantity of the provided samples play a pivotal role in the success of high-throughput screening programs this poses serious problems. In order to make samples of natural origin competitive with synthetic compound libraries, we devised a novel, automated sample preparation procedure based on solid-phase extraction (SPE). By making use of a modified Zymark RapidTrace®SPE workstation an easy-to-handle and effective fractionation method has been developed which allows the generation of highquality samples from natural origin, fulfilling the requirements of an integration into high-throughput screening programs.


Author(s):  
Kumiko Sakai-Kato ◽  
Masaru Kato ◽  
Naoko Utsunomiya-Tate ◽  
Toshimasa Toyo'oka

2000 ◽  
Vol 5 (1) ◽  
pp. 13-21 ◽  
Author(s):  
Marie-Helene Beydon ◽  
Alain Fournier ◽  
Lionel Drugeault ◽  
Jerome Becquart

Microbial HTS has been implemented at Rhone-Poulenc Rorer through the development of a dedicated robotic platform. This robot (Turbo) has been designed with the aim of fully integrating microbial HTS into the lead discovery processes. Innovative solutions have been found to reach high throughput as well as flexibility. This opens up new prospects for solid-phase microbial screening, taking advantage of the easy implementation and the very low costs of such screens. The different types of microbial screens done in our laboratory, as well as the throughputs and outputs obtained, are described. Some of the specific aspects of microbial HTS, as compared to biochemical and cell-based assays, are also discussed.


ChemInform ◽  
2016 ◽  
Vol 47 (15) ◽  
pp. no-no
Author(s):  
D. Baud ◽  
N. Ladkau ◽  
T. S. Moody ◽  
J. M. Ward ◽  
H. C. Hailes

2019 ◽  
Vol 23 (7) ◽  
pp. 768-808
Author(s):  
Virendra Prasad ◽  
Nidhi Mishra ◽  
Anand K. Agrahari ◽  
Sumit K. Singh ◽  
Prabhu P. Mohapatra ◽  
...  

Recent advances in high-throughput, automated techniques combined with the identification of new therapeutic targets in genome sequencing and molecular biology have generated a need for a large collection of diverse heterocyclic scaffolds. This inspires toward the development of novel reaction sequences and linking strategies to generate libraries of diverse simple to complex heterocyclic systems. In this regard, combinatorial chemistry has emerged as an excellent technology platform for the rapid assembly of building blocks to synthesize complex molecular structures with great ease in a few synthetic steps. By means of the implementation of high-throughput screening for the biological evaluation of hits and leads, combinatorial libraries have become important assets in drug discovery and development. In the last two decades, the cyclorelease strategy that minimizes the chemical and tethering implications by releasing the intact desired target molecule in the final step of reaction has attracted much attention. Recently, a particular interest is developing in linking strategies, where loading and cleavage steps contribute to the complexity of the target structure rather than only extraneous manipulations. This review summarises the practical and high-yielding approaches of solid phase combinatorial synthesis for diverse high-purity heterocyclic skeletons of pharmacological importance involving the cycloelimination strategy.


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