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Natural products have served as an important source of medicinal compounds and pharmaceutical leads over the last century. Within the last 10 years, significant interest has developed in applying combinatorial chemistry techniques to the study of natural products and their biological activities....
The development of soluble mixture‐based heterocyclic combinatorial libraries derived from amino acids and peptides is described. Starting with a “toolbox” of various chemical transformations, including alkylations, reductions, acylations, and the use of a variety of bifunctional reagents,...
This review focuses on the concept, methods, and strategies of orthogonal peptide ligation. It updates our previous review in 1999 on the same subject matter in Biopolymers (Peptide Science, 1999, Vol. 51, p. 311). Orthogonal peptide ligation is an amino terminal specific method to couple...
The genome sequencing effort has helped spawn the burgeoning field of proteomics. This review article examines state‐of‐the‐art proteomics methods that are helping change the discovery paradigm in a variety of biological disciplines and, in particular, protein biochemistry. The review...
Peptide recognition by G‐protein coupled receptors (GPCRs) is reviewed with an emphasis on the indirect approach used to determine the receptor‐bound conformation of peptide ligands. This approach was developed in response to the lack of detailed structural information available for these...
The problem of identifying downstream targets of kinase phosphorylation remains a challenge despite technological advances in genomics and proteomics. A recent approach involves the generation of kinase mutants that can uniquely use “orthogonal” ATP analogs to phosphorylate substrates in...
It has been a major focus in our laboratories to prepare novel reagents and peptidomimetic structures for drug design. We have designed and prepared novel guanidinylation reagents that can be employed in solution or as solid phase reagents. We and others have utilized the reagent...
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