نتایج جستجو برای: peptidomimetic
تعداد نتایج: 722 فیلتر نتایج به سال:
Two peptidomimetic macrocycles, regioisomeric in terms of the position of triazole/amide, have been synthesized. Both undergo self-assembly in a parallel manner but in solvents of opposite polarity, ascribed to (β, β) and (β-D, β-L) hydrogen bonding leading to formation of two different unique classes of organic nanostructures.
We report a first set of peptidomimetic ligands mimicking the adhesive interface identified by recent crystallographic structures of E- and N-cadherin. Compounds 2 and 3 inhibit adhesion of epithelial ovarian cancer (EOC) cells with improved efficacy compared to the ADH-1 peptide, a N-cadherin antagonist that is in early clinical trials in EOC patients.
The ligand-receptor interaction between some peptidomimetic inhibitors and a class II MHC peptide presenting molecule, the HLA-DR4 receptor, was modeled using some three-dimensional (3D) quantitative structure-activity relationship (QSAR) methods such as the Comparative Molecular Field Analysis (CoMFA), Comparative Molecular Similarity Indices Analysis (CoMSIA), and a pharmacophore building met...
The Front Cover shows a panorama from the so-called Path of Gods, hiking trail in Southern Italy. At end strenuous journey, trekker is rewarded with wonderful view Amalfi coast. path to developing (cyclic) peptoids as therapeutic agents still an uphill hike, but tremendous advances made last few decades terms both varied biological activity and structural diversity make them rather promising cl...
1 Lysine-enriched analogs of the cecropin-mellitin hybrid peptide, CA1-7 M2-9 (designated 2 CM15), designed with optimized amphipathicity retained antimicrobial activity similar to 3 wild type CM15 and had substantially reduced hemolytic activity and cytotoxicity 4 towards cultured macrophages, resulting in enhanced selectivity. These lysine-enriched 5 analogs provide templates for improved CM1...
Lysine-enriched analogs of the cecropin-mellitin hybrid peptide, CA(1-7) M(2-9) (designated CM15), designed with optimized amphipathicity, retained antimicrobial activities similar to that of wild-type CM15 and had substantially reduced levels of hemolytic activity and cytotoxicity toward cultured macrophages, resulting in enhanced selectivity. These lysine-enriched analogs provide templates fo...
β-Hairpin peptides were conformationally stabilized through a 1,4 disubstituted 1,2,3-triazole interstrand linkage. A NMR conformational analysis revealed that the β-hairpin content depends on the number and position of substituent methylene units of the 1,2,3-triazole ring. These results will allow the design of metabolically stable peptidomimetic analogs of bioactive β-hairpin peptides.
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