Exploring S1 plasticity and probing S1 ' ...
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
Exploring S1 plasticity and probing S1 ' subsite of mammalian aminopeptidase N/CD13 with highly potent and selective aminobenzosuberone inhibitors
Auteur(s) :
Revelant, Germain [Auteur]
Al-Lakkis-Wehbe, Mira [Auteur]
Schmitt, Marjorie [Auteur]
Alavi, Sarah [Auteur]
Schmitt, Celine [Auteur]
Roux, Lionel [Auteur]
Al-Masri, Mounir [Auteur]
Schifano, Nadege [Auteur]
Maiereanu, Carmen [Auteur]
Tarnus, Celine [Auteur]
Albrecht, Sebastien [Auteur]
Al-Lakkis-Wehbe, Mira [Auteur]
Schmitt, Marjorie [Auteur]
Alavi, Sarah [Auteur]
Schmitt, Celine [Auteur]
Roux, Lionel [Auteur]
Al-Masri, Mounir [Auteur]
Schifano, Nadege [Auteur]
Maiereanu, Carmen [Auteur]
Tarnus, Celine [Auteur]
Albrecht, Sebastien [Auteur]
Titre de la revue :
Bioorganic & medicinal chemistry
Nom court de la revue :
Bioorg. Med. Chem.
Numéro :
23
Pagination :
3192-3207
Date de publication :
2015
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé :
In order to probe the S1 and S1' mammalian aminopeptidase N subsites, racemic 1- or 4-substituted 7-aminobenzocyclohepten-6-one derivatives were synthesized and evaluated for their ability to inhibit mammalian aminopeptidase ...
Lire la suite >In order to probe the S1 and S1' mammalian aminopeptidase N subsites, racemic 1- or 4-substituted 7-aminobenzocyclohepten-6-one derivatives were synthesized and evaluated for their ability to inhibit mammalian aminopeptidase N. We focused on improving the physicochemical and ADME properties of this series by targeting lipophilicity and LELP score. Some 4-heteroaryl substituted analogues displayed reduced lipophilicity and enhanced inhibition potency with Ki values in the nanomolar range.Lire moins >
Lire la suite >In order to probe the S1 and S1' mammalian aminopeptidase N subsites, racemic 1- or 4-substituted 7-aminobenzocyclohepten-6-one derivatives were synthesized and evaluated for their ability to inhibit mammalian aminopeptidase N. We focused on improving the physicochemical and ADME properties of this series by targeting lipophilicity and LELP score. Some 4-heteroaryl substituted analogues displayed reduced lipophilicity and enhanced inhibition potency with Ki values in the nanomolar range.Lire moins >
Langue :
Anglais
Audience :
Internationale
Vulgarisation :
Non
Établissement(s) :
Université de Lille
CHU Lille
CHU Lille
Collections :
Équipe(s) de recherche :
Modélisation biopharmaceutique et pharmacocinétique
Date de dépôt :
2019-02-26T17:11:49Z