Combinatorial Chemistry & High Throughput Screening - Volume 5, Issue 6, 2002

Molecular recognition between molecules is one of the most fundamental processes in biology and chemistry. The recognition process is largely driven by non-covalent forces such as hydrogen bonding, electrostatics, van der Waals forces, π-π interactions, and conformational energy. The complementarity between the receptor and substrate is very similar to the “lock and key” function, first described by Emil Fischer over 1 Read More

New approaches for manufacturing and application of peptide arrays on planar surfaces are emerging, thereby opening advanced opportunities to probe the expression and function of the proteome. In complementing DNA and protein array analyses, peptide fragment screening directly addresses functional protein interaction sites, leading to a detailed insight into the discovered molecular recognition events, placing the Read More

It was in the 1980's that the first papers in which the use of either combinatorial methods or microwave heating in organic chemistry were published. Unlike combinatorial chemistry, which quite readily became an accepted method, particularly in the pharmaceutical industry, it is only now that microwave heating is truly gaining acceptance. Our aim in this review is to attempt to rationalize this slow acceptance and to s Read More

Development of predictive in vitro surrogate methods for traditional approaches assessing bioavailability and pharmacokinetics of lead compounds must be made to both keep pace with highthroughput (HT) lead identification and to mitigate the high costs associated with progression of compounds with poor chances of developmental success. Indeed opportunities for improvement still exist in the lead optimization phase Read More

We have demonstrated that mRNA, ribosome and resulting protein form complexes (ternary complexes) in wheat germ cell-free translation system and these complexes are stable for at least several hours. The protein folds into a proper conformation capable of specific binding with the inhibitor of its enzymatic activity. The removal of the stop codon from mRNA does not affect translation and mRNA-ribosome-protein complex sta Read More

Combinatorial chemistry has become a dramatically useful tool for the development of new medicinal agents. In the search to discover a novel and effective lead for the treatment of giardiasis, solutionphase synthesis of a library of isoflavone derivatives has been accomplished. Of the products screened, several compounds such as P(A1,B1) and P(A1,B11) exhibited potent antigiardial activity. The details of synthesis, in vitro antig Read More

A combinatorial Fab phage display library was generated from the antibody variable region genes of each of 2 BALB / c mice immunized with the human colorectal cancer cell lines SW480, SW948, and SW837. These libraries were shown to be diverse by nucleotide sequencing and diagnostic restriction enzyme digestion (fingerprinting) of individual members. The two libraries were combined and selected for binding to a suspe Read More

This paper reports a new solid support reagent that showed high degrees of selective molecular reactivity and molecular recognition in homo-functional reactions (reactions having similar reactive functionality in reactants and products).