نتایج جستجو برای: peptidomimetic
تعداد نتایج: 722 فیلتر نتایج به سال:
A concise synthetic route has been developed for the preparation of a constrained peptidomimetic pyrazinone building block. From hydroxy-L-lysine, the desired pyrazinone is obtained in 43% overall yield (6 steps) via an efficient deprotection-double cyclization sequence.
pepMMsMIMIC is a novel web-oriented peptidomimetic compound virtual screening tool based on a multi-conformers three-dimensional (3D)-similarity search strategy. Key to the development of pepMMsMIMIC has been the creation of a library of 17 million conformers calculated from 3.9 million commercially available chemicals collected in the MMsINC® database. Using as input the 3D structure of a pept...
Antibiotics with new mechanisms of action are urgently required to combat the growing health threat posed by resistant pathogenic microorganisms. We synthesized a family of peptidomimetic antibiotics based on the antimicrobial peptide protegrin I. Several rounds of optimization gave a lead compound that was active in the nanomolar range against Gram-negative Pseudomonas spp., but was largely in...
A solid-phase procedure is used to synthesize racemic peptidomimetics based on the fundamental peptide unit. The peptidomimetics are constructed around proline or proline homologues variably substituted at the amine and carbonyl sites. The procedure expands the diversity of substituted peptidomimetic molecules available to the Distributed Drug Discovery (D3) project. Using a BAL-based solid-pha...
• Modified peptides: these molecules contain relatively small modifications that do not modify the peptide bond, and thus they still possess a chemical structure of peptide nature. • Pseudopeptides: in these compounds partial modifications of either peptide bonds or side-chains are introduced, contributing to the generation of molecules possessing a chemical structure of only partial peptide na...
T he discovery of the cyclic nucleotides 3',5'cyclic monophosphate (cAMP, Prod. No. A 9501, A 4137) and guanosine 3',5'-cyclic monophosphate (cGMP, Prod. No. G 7504, G 6129) led to the first formulation of the second messenger concept. These cyclic nucleotides are now known to be ubiquitous intracellular second messengers that mediate the response of cells to a variety of extracellular stimuli ...
Development of therapy against infections caused by antibiotic-resistant pathogens is a major unmet need in contemporary medicine. In previous work, our group chemically modified an antimicrobial peptidomimetic motif for targeted applications against cancer and obesity. Here, we show that the modified motif per se is resistant to proteolytic degradation and is a candidate antiinfective agent. W...
Amidine-type peptide bond isosteres were designed based on the substitution of the peptide bond carbonyl (C=O) group with an imino (C=NH) group. The positively-charged property of the isosteric part resembles a reduced amide-type peptidomimetic. The peptidyl amidine units were synthesized by the reduction of a key amidoxime (N-hydroxyamidine) precursor, which was prepared from nitrile oxide com...
Ras CAAX (C = cysteine, A = aliphatic amino acid, and X = any amino acid) peptidomimetic inhibitors of farnesyl protein transferase suppress Ras-dependent cell transformation by preventing farnesylation of the Ras oncoprotein. These compounds are potential anticancer agents for tumors associated with Ras mutations. The peptidomimetic FTI-254 was tested for Ras1-inhibiting activity in whole anim...
A proteolytically stable small molecule beta-turn peptidomimetic, termed D3, was identified as an agonist of the TrkA neurotrophin receptor. D3 binds the Ig-like C2 region of the extracellular domain of TrkA, competes the binding of another TrkA agonist, affords selective trophic protection to TrkA-expressing cell lines and neuronal primary cultures, and induces the differentiation of primary n...
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