منابع مشابه
Ribosomal Synthesis of N-Methyl Peptides
N-methyl amino acids (N-Me AAs) are a common component of nonribosomal peptides (NRPs), a class of natural products from which many clinically important therapeutics are obtained. N-Me AAs confer peptides with increased conformational rigidity, membrane permeability, and protease resistance. Hence, these analogues are highly desirable building blocks in the ribosomal synthesis of unnatural pept...
متن کاملRibosomal synthesis of unnatural peptides.
Combinatorial libraries of non-biological polymers and drug-like peptides could in principle be synthesized from unnatural amino acids by exploiting the broad substrate specificity of the ribosome. The ribosomal synthesis of such libraries would allow rare functional molecules to be identified using technologies developed for the in vitro selection of peptides and proteins. Here, we use a recon...
متن کاملRibosomal Synthesis of Thioether-Bridged Bicyclic Peptides.
Many biologically active peptides found in nature exhibit a bicyclic structure wherein a head-to-tail cyclic backbone is further constrained by an intramolecular linkage connecting two side chains of the peptide. Accordingly, methods to access macrocyclic peptides sharing this overall topology could be of significant value toward the discovery of new functional entities and bioactive compounds....
متن کاملRibosomal synthesis of dehydroalanine-containing peptides.
Dehydroalanine is a nonproteinogenic amino acid, but it is a component of a wide variety of natural products with therapeutic activities. Indeed, this alpha,beta-unsaturated residue is a highly versatile building block due to its rigidifying effect on peptide backbones and its electrophilicity which allows site-specific thiol ligations of peptides with small molecules or proteins. To harness su...
متن کاملSYNTHESIS AND PHARMACOLOGICAL EVALUATION OF N-METHYL PIPERIDINE ANALGESICS
Pain is probably the immediate stimulus for more visits to the Physician's office than all other complaints combined. Since pain serves as an alert to injury, it is often the first harbinger of disease. Piperidine has been extensively utilized for the synthesis of a wide range of therapeutic agents in general and analgetics in particular for the mitigation of pain. In a similar attempt, th...
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ژورنال
عنوان ژورنال: Journal of the American Chemical Society
سال: 2008
ISSN: 0002-7863,1520-5126
DOI: 10.1021/ja710016v