About: Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases

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About: Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases
Creator	Florent, Isabelle Addlagatta, Anthony Alavi, Sarah Albrecht, Sébastien Revelant, Germain Salomon, Emmanuel Schmitt, Céline Schmitt, Marjorie Stamogiannos, Athanasios Stratikos, Efstratios Kumar Marapaka, Anil Tarnusa, Céline
Source	Medline; PMC
abstract	The synthesis of racemic substituted 7-amino-5,7,8,9-tetrahydrobenzocyclohepten-6-one hydrochlorides was optimized to enhance reproducibility and increase the overall yield. In order to investigate their specificity, series of enzyme inhibition assays were carried out against a diversity of proteases, covering representative members of aspartic, cysteine, metallo and serine endopeptidases and including eight members of the monometallic M1 family of aminopeptidases as well as two members of the bimetallic M17 and M28 aminopeptidase families. This aminobenzosuberone scaffold indeed demonstrated selective inhibition of M1 aminopeptidases to the exclusion of other tested protease families; it was particularly potent against mammalian APN and its bacterial/parasitic orthologues EcPepN and PfAM1.
has issue date	2018-10-11(xsd:dateTime)
bibo:doi	10.3390/molecules23102607
bibo:pmid	30314342
has license	cc-by
sha1sum (hex)	d33f858e29256297e9721a300f968f346aa81b0b
schema:url	https://doi.org/10.3390/molecules23102607
resource representing a document's title	Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases
has PubMed Central identifier	PMC6222927
has PubMed identifier	30314342
schema:publication	Molecules
resource representing a document's body	covid:d33f858e29256297e9721a300f968f346aa81b0b#body_text
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