Bruno, Martin A Clarke, Paul B S Seltzer, Alicia Quirion, Rémi Burgess, Kevin Cuello, A Claudio Saragovi, H Uri
Published in
The Journal of neuroscience : the official journal of the Society for Neuroscience
Previously, we developed a proteolytically stable small molecule peptidomimetic termed D3 as a selective ligand of the extracellular domain of the TrkA receptor for the NGF. Ex vivo D3 was defined as a selective, partial TrkA agonist. Here, the in vivo efficacy of D3 as a potential therapeutic for cholinergic neurons was tested in cognitively impai...
Shannon, Kristen E. Keene, Jeffery L. Settle, Steven L. Duffin, Tiffany D. Nickols, Maureen A. Westlin, Marisa Schroeter, Sally Ruminski, Peter G. Griggs, David W.
Published in
Clinical & Experimental Metastasis
Integrins expressed on endothelial cells modulate cell migration and survival during angiogenesis. Integrins expressed on carcinoma cells potentiate metastasis by facilitating invasion and movement across blood vessels. We describe the activities of two synthetic low-molecular-weight peptidomimetics of the ligand amino acid sequence arg-gly-asp (RG...
Webb, Andrew I. Aguilar, Marie-isabel Purcell, Anthony W.
Published in
Letters in Peptide Science
In this brief review we describe the methods that our group and others have developed in incorporating non-natural amino acids into peptide antigens, principally to increase protease resistance, for potential use in peptide-based vaccines. Peptide-based vaccination has the potential to generate protective immunity without the need for in situ antig...
Webb, Andrew I. Aguilar, Marie-Isabel Purcell, Anthony W.
Published in
Letters in Peptide Science
In this brief review we describe the methods that our group and others have developed in incorporating non-natural amino acids into peptide antigens, principally to increase protease resistance, for potential use in peptide-based vaccines. Peptide-based vaccination has the potential to generate protective immunity without the need forin situ antige...
Trabocchi, Andrea Mancini, Francesco Menchi, Gloria Guarna, Antonio
Published in
Molecular Diversity
The development of new strategies for solid-phase synthesis of 3-aza-6,8-dioxabicyclo[3.2.1]octane scaffolds, named BTKa, is described. The preparation was made possible by the combination of three components: amines, α-halo-acetophenones, and sugar or tartaric acid derivatives. By anchoring each of the three components it was possible to synthesiz...
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...
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...
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.
