Novel activity-based probes for N-acylethanolamine acid amidase

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

doi:10.1039/c7cc06838g

Novel activity-based probes for N-acylethanolamine acid amidase

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

Research output: Contribution to journal › Article › Academic › peer-review

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.

Original language	English
Pages (from-to)	11810-11813
Number of pages	4
Journal	Chemical communications (Cambridge, England)
Volume	53
Issue number	86
DOIs	https://doi.org/10.1039/c7cc06838g
Publication status	Published - 22 Aug 2017
Externally published	Yes

Keywords

Amidohydrolases/antagonists & inhibitors
Drug Evaluation, Preclinical
Enzyme Inhibitors/pharmacology
Humans
Molecular Probes/chemical synthesis
Molecular Structure
Threonine/chemistry
beta-Lactams/chemistry

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10.1039/c7cc06838g

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title = "Novel activity-based probes for N-acylethanolamine acid amidase",

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.",

keywords = "Amidohydrolases/antagonists \& inhibitors, Drug Evaluation, Preclinical, Enzyme Inhibitors/pharmacology, Humans, Molecular Probes/chemical synthesis, Molecular Structure, Threonine/chemistry, beta-Lactams/chemistry",

author = "Rita Petracca and Elisa Romeo and Baggelaar, \{Marc P\} and Marta Artola and Silvia Pontis and Stefano Ponzano and Overkleeft, \{Herman S\} and \{van der Stelt\}, Mario and Daniele Piomelli",

year = "2017",

month = aug,

day = "22",

doi = "10.1039/c7cc06838g",

language = "English",

volume = "53",

pages = "11810--11813",

journal = "Chemical communications (Cambridge, England)",

issn = "1359-7345",

publisher = "Royal Society of Chemistry",

number = "86",

}

TY - JOUR

T1 - Novel activity-based probes for N-acylethanolamine acid amidase

AU - Petracca, Rita

AU - Romeo, Elisa

AU - Baggelaar, Marc P

AU - Artola, Marta

AU - Pontis, Silvia

AU - Ponzano, Stefano

AU - Overkleeft, Herman S

AU - van der Stelt, Mario

AU - Piomelli, Daniele

PY - 2017/8/22

Y1 - 2017/8/22

N2 - 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.

AB - 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.

KW - Amidohydrolases/antagonists & inhibitors

KW - Drug Evaluation, Preclinical

KW - Enzyme Inhibitors/pharmacology

KW - Humans

KW - Molecular Probes/chemical synthesis

KW - Molecular Structure

KW - Threonine/chemistry

KW - beta-Lactams/chemistry

U2 - 10.1039/c7cc06838g

DO - 10.1039/c7cc06838g

M3 - Article

C2 - 29035406

SN - 1359-7345

VL - 53

SP - 11810

EP - 11813

JO - Chemical communications (Cambridge, England)

JF - Chemical communications (Cambridge, England)

IS - 86

ER -

Novel activity-based probes for N-acylethanolamine acid amidase

Abstract

Keywords

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