Novel activity-based probes for N-acylethanolamine acid amidase.

Petracca, Rita; Romeo, Elisa; Baggelaar, Marc P; Artola, Marta; Pontis, Silvia; Ponzano, Stefano; Overkleeft, Herman S; van der Stelt, Mario; Piomelli, Daniele

Petracca, Rita; Romeo, Elisa; Baggelaar, Marc P; Artola, Marta; Pontis, Silvia; Ponzano, Stefano; Overkleeft, Herman S; van der Stelt, Mario; Piomelli, Daniele.

Afiliação

Petracca R; School of Chemistry and Trinity Biomedical Sciences Institute (TBSI), Trinity College Dublin, The University of Dublin, Dublin 2, Ireland.

Chem Commun (Camb) ; 53(86): 11810-11813, 2017 Aug 22.

Article em En | MEDLINE | ID: mdl-29035406

ABSTRACT

ABSTRACT

The cysteine hydrolase, N-acylethanolamine acid amidase (NAAA) is a promising target for analgesic and anti-inflammatory drugs. Here, we describe the development of two unprecedented NAAA-reactive activity-based probes as research tools for application in the discovery of new inhibitors and for the in-depth characterization of NAAA in its cellular environment.

Assuntos

Amidoidrolases/metabolismo; Sondas Moleculares/química; Sondas Moleculares/metabolismo; Amidoidrolases/antagonistas & inibidores; Avaliação Pré-Clínica de Medicamentos; Inibidores Enzimáticos/farmacologia; Humanos; Sondas Moleculares/síntese química; Estrutura Molecular; Treonina/química; beta-Lactamas/química

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sondas Moleculares / Amidoidrolases Limite: Humans Idioma: En Ano de publicação: 2017 Tipo de documento: Article

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