Exploring S1 plasticity and probing S1 ' ...
Document type :
Article dans une revue scientifique
PMID :
Permalink :
Title :
Exploring S1 plasticity and probing S1 ' subsite of mammalian aminopeptidase N/CD13 with highly potent and selective aminobenzosuberone inhibitors
Author(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]
Journal title :
Bioorganic & medicinal chemistry
Abbreviated title :
Bioorg. Med. Chem.
Volume number :
23
Pages :
3192-3207
Publication date :
2015
HAL domain(s) :
Sciences du Vivant [q-bio]
French abstract :
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 ...
Show more >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.Show less >
Show more >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.Show less >
Language :
Anglais
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
Université de Lille
CHU Lille
CHU Lille
Collections :
Research team(s) :
Modélisation biopharmaceutique et pharmacocinétique
Submission date :
2019-02-26T17:11:49Z