Babizhayev, Mark. A. Courbebaisse, Yann Nicolaÿ, Jean-François Semiletov, Yuri A.
Published in
Letters in Peptide Science
Histidine-containing natural dipeptides, such as L-carnosine, were reported to be effective against different oxygen-derived free radicals, and also lipoperoxyl radicals. However, L-carnosine appeared to be uneffective in vivo, due to the presence of ubiquitous specific or semi-specific hydrolytic enzymes. Therefore, a series of peptidomimetics wer...
Kasher, Ron Bitan, Gal Halloun, Christeen Gilon, Chaim
Published in
Letters in Peptide Science
The synthesis of a backbone bicyclic nonapeptide that mimics the binding site of bovine pancreatic trypsin inhibitor (BPTI) is described. The BPTI mimetic, which containscis-thioproline replacing Cys38 of the protein, inhibits trypsin with a Ki of 76 μM.
Babizhayev, Mark A. Courbebaisse, Yann Nicolay, Jean-François Semiletov, Yuri A.
Published in
Letters in Peptide Science
Histidine-containing natural dipeptides, such as L-carnosine, were reported to be effective against different oxygenderived free radicals, and also lipoperoxyl radicals. However, L-carnosine appeared to be uneffective in vivo, due to the presence of ubiquitous specific or semi-specific hydrolytic enzymes. Therefore, a series of peptidomimetics were...
Kasher, Ron Bitan, Gal Halloun, Christeen Gilon, Chaim
Published in
Letters in Peptide Science
The synthesis of a backbone bicyclic nonapeptide that mimics the binding site of bovine pancreatic trypsin inhibitor (BPTI) is described. The BPTI mimetic, which contains cis-thioproline replacing Cys38 of the protein, inhibits trypsin with a Ki of 76 μM.
Camenisch, Gian P. Wang, Wei Wang, Binghe Borchardt, Ronald T.
Published in
Pharmaceutical Research
Purpose. To compare the bioconversion rates in various biological media and the Caco-2 cell permeation characteristics of coumarin-based cyclic prodrugs (3a, 3b) and methylester-based linear prodrugs (1b, 2b) of two RGD peptidomimetics (la, 2a). Methods. Bioconversion rates of the prodrugs to the RGD peptidomimetics were determined in Hank balanced...
Nouvet, André Binard, Marc Lamaty, Frédéric Lazaro, René
Published in
Letters in Peptide Science
A direct synthesis of a series ofN-SES amino acids is described.N-SES Ala has been further utilized in the synthesis of a perhydro-1,4-diazepin-2-one.
Nouvet, André Binard, Marc Lamaty, Frédéric Lazaro, René
Published in
Letters in Peptide Science
A direct synthesis of a series of N-SES amino acids is described. N-SES Ala has been further utilized in the synthesis of a perhydro-1,4-diazepin-2-one.
Abell, Andrew D.
Published in
Letters in Peptide Science
Heterocyclic-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 co...
Abell, Andrew D.
Published in
Letters in Peptide Science
Heterocyclic-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 c...
Bultinck, Patrick Augustynen, S Hilbers, HW Moret, E Moret, JP
The program Generate, aimed at generating 3-D structures for peptides and peptidomimetics, is presented. The algorithm is based on a build-up procedure, using a library of conformations of amino acid residues. This library is built from conformational analysis of amino acids placed in a di- or tripeptide environment to mimic the surroundings of the...
