Results 71 to 80 of about 6,152 (116)
Some of the next articles are maybe not open access.
Steroid Receptor Coactivator Peptidomimetics
2003Publisher Summary This chapter focuses on the methods that are useful for designing and synthesizing a series of coactivator peptidomimetics (axXXbxcx) of the L1XXL2L3 sequence to identify specific inhibitors of particular hormone receptor (NR)–coactivator interactions.
Timothy R, Geistlinger, R Kiplin, Guy
openaire +2 more sources
Peptidomimetics derived from natural products
Medicinal Research Reviews, 1993Although much has been written in recent years about rational drug design, no drug has been designed de novo, that is, without using a natural substrate or inhibitor or screening lead as a starting point. Instead, as we have seen, medicinal chemists continue to depend upon serendipitous discovery of novel biological activities and novel chemical ...
R A, Wiley, D H, Rich
openaire +2 more sources
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
openaire +2 more sources
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
openaire +2 more sources
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 ...
openaire +2 more sources
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
openaire +2 more sources
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
openaire +1 more source
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
openaire +1 more source
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
openaire +1 more source