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Benzodiazepine peptidomimetic inhibitors of farnesyltransferase
Bioorganic & Medicinal Chemistry, 1994A structural survey of protein Zn2+ binding geometries was instigated based upon the functional requirement of Ras farnesyltransferase for Zn2+. The Cys-X-X-Cys motif found in Zn(2+)-binding proteins such as aspartate transcarbamylase was used as a template to devise a bidentate-coordination model for Cys-A1-A2-X peptide inhibitors.
James C. Marsters +15 more
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Oxetanyl Amino Acids for Peptidomimetics
Organic Letters, 2017Peptides are important in the drug discovery process. In analogy to nonpeptidic small-molecule counterparts, they can sometimes suffer from disadvantages such as their low bioavailability and poor metabolic stability. Herein, we report the synthesis of new oxetanyl dipeptides and their incorporation into Leu-enkephalin analogues as proof-of-principle ...
Guido P. Möller +6 more
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Heterocyclic-based peptidomimetics
Letters in Peptide Science, 2001Heterocyclic-based peptidomimetics possess properties that are dictated by the chemical and physical properties of the constituent heterocycle. Here we review two general classes of peptidomimetic, one in which the conformation of a peptide is confined into a particular geometry, and a second, where chemical reactivity is masked and released in a ...
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Multivalent peptidomimetics for tumor targeting
2009Introduction Multivalency is a common phenomenon in nature to increase affinity and specifity of receptor-ligand interactions, especially on the cell surface. Chemists have tried to make use of multivalent interactions in different context and have synthesized a lot of scaffolds for the assembly of multivalent receptor ligands [1]. We designed suitable
Nadine, Pannier +4 more
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2019
The peptidomimetics are peptide or non-peptide molecules with a potential for enhanced conformational stability and activity compared with natural peptides. One of the numerous design approaches utilizes a small molecular scaffold aimed to induce the formation of turn structures upon insertion into the peptide backbone.
Kovačević, Monika +2 more
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The peptidomimetics are peptide or non-peptide molecules with a potential for enhanced conformational stability and activity compared with natural peptides. One of the numerous design approaches utilizes a small molecular scaffold aimed to induce the formation of turn structures upon insertion into the peptide backbone.
Kovačević, Monika +2 more
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Beta-peptidic peptidomimetics.
Accounts of chemical research, 2008For more than a decade now, a search for answers to the following two questions has taken us on a new and exciting journey into the world of beta- and gamma-peptides: What happens if the oxygen atoms in a 3i-helix of a polymeric chain composed of (R)-3-hydroxybutanoic acid are replaced by NH units?
Dieter, Seebach, James, Gardiner
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Conformationally restricted peptidomimetics
2000Peptidomimetic compounds are becoming increasing important as medicinal agents. This thesis describes the design and synthesis of a novel class of non-hydrolysable peptidomimetic isosteres, the tetrazole-based amide bond isosteres. These new structural mimics have been developed for incorporation into enzyme inhibitors and biological probes where a non-
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Hydrazino-based peptidomimetics
2015Peptide-inspired drug scaffolds having designable molecular shape and surface chemistry pattern are of particular interest. Biological function of biomolecules ; enzyme- substrate specificity, binding to receptors, protein-protein or protein-nucleic acid interactions, is determined by their specific secondary structure (helices, turns, sheets ...
Vlahoviček-Kahlina, Kristina +2 more
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