Mini-Reviews in Organic Chemistry - Volume 8, Issue 2, 2011

Protein-protein and protein-nucleic acid interactions are of key importance in cellular biology and thus in the context of basic as well as applied life science. Roughly, five interaction partners for any given cellular protein have been predicted illustrating the complexity of the formed network. In this context, the parallel synthesis of oligopeptide arrays on cellulose membrane supports (SPOT method) fills the gap between applicati Read More

A detailed knowledge on how proteins interact with other proteins or nucleic acids is essential for basic research as well as for the development of drugs and therapeutic leads. In this context, peptide arrays represent a powerful tool to analyze individual interactions within complex protein networks. Moreover, peptide arrays allow for incorporation of artificial building blocks during synthesis and secondary modification of a Read More

The SPOT technique is one of the most frequently used methods for synthesis and screening of peptides on arrays. Materials such as polypropylene and glass are used for the preparation of peptide arrays, however the most commonly used material for SPOT membranes is cellulose. This paper focuses on materials and procedures used in the SPOT synthesis on cellulose membranes as a special type of solid phase peptide synthe Read More

Nowadays, lithographic methods facilitate the combinatorial synthesis of >50.000 oligonucleotides per cm2, an achievement that revolutionized the whole field of genomics. High-density peptide arrays might spark a similar development for the field of proteomics, but all lithographic methods have a peptide specific disadvantage that impairs their use for peptide synthesis: Each monomer must be coupled separately to the soli Read More

Peptide arrays are useful tools to characterize antibodies, to determine sequence specificities of enzymes, or to find interaction partners to given peptide sequences. One widely-used format for such arrays is a cellulose sheet with hundreds of synthetic peptides bound to it. These SPOT arrays have been used successfully in a broad range of applications since their invention at the beginning of the nineties. The simplicity and rob Read More

One of the first applications of peptide arrays in general and those prepared by SPOT synthesis in particular was the mapping of antibody epitopes. In this article the diverse applications in this field are described. Different types of peptide libraries such as peptide scans, substitution analyses, truncation and deletion libraries as well as combinatorial and randomly generated libraries are briefly covered. Furthermore, their applic Read More

Applications of peptide arrays in the field of enzyme profiling are described in detail. Focus is on assay principles for measuring activities of kinases, phosphatases or proteases and on substrate identification/optimization for kinases. Additionally, several examples for reliable identification of substrates for other enzymes like lysine methyl transferases and ATP-ribosyltransferases are given. Finally, use of high-density peptide Read More

Developing of new lead structures against multidrug-resistant bacteria is an urgent need and cationic antimicrobial peptides (AMPs) have the potential to become such a lead structure. Here we provide an overview of a method to screen peptides for antimicrobial activity based on the SPOT synthesis. Three different strategies to study and optimize antimicrobial activity of peptides have been reported, substitution analy Read More

Development of array technologies started in the late 1980s, and today this technique has become a powerful tool for high throughput approaches in biology and chemistry. Progress was mainly driven by the human genome project and associated with the development of several new technologies, leading to the birth of additional “omic” topics such as proteomics, glycomics, or antibodyomics. In this review we focus str Read More

Peptide arrays represent a powerful research tool, especially for the development of medical applications to screen peptides for the replacement of animal-derived proteins. This minireview focuses on the applicability of cellulose-bound peptide arrays to assay peptide- cell interactions. Moreover, the successful combination of peptide array and bioinformatics to overcome the limitation of library size in array-type screeni Read More

Ionic liquids (ILs) are attracting increasing interest as a potential ecosustainable alternative to traditional volatile organic solvents (VOCs), generally used in large amounts. About the “greenness” of ILs a certain controversy still exists because their toxicity and biodegradability need to be fully assessed. Moreover, the real advantages of using this novel class of solvents should be more deeply studied in comparison with tradition Read More

The preparation of oxime by nitrosation of active methyl and methylene groups of N-heteroaromatics is presented. The reaction of N-heteroaromatics with alkyl nitrite in the presence of a base in liq. NH3 or THF and the difference of reactivity based on E-Z geometrical isomers of oxime are discussed experimentally and theoretically.

3-Amino-2-hydroxy-4-phenylbutyric acids (AHPA or alternatively abbreviated AHPBA) serve as chiral building blocks for various bioactive compounds including aminopeptidase N (APN) inhibitors, HIV-l protease inhibitors, and renin inhibitors. The synthesis of α-hydroxy-β-amino acids has therefore attracted considerable interest in recent years and various synthetic approaches have been developed to complete their s Read More

Salicylanilides are a well-known family of pharmacological compounds, which are under renewed investigation because of the discovery of novel interesting biological activities and mechanisms of action over the last decade. This comprehensive mini-review describes the biological and pharmacological properties of salicylanilides, their activity against atypical and multi-drug resistant mycobacterial strains, and synthetic Read More