(Q48304342)

http://europepmc.org/abstract/PMC/5641481

9 July 2018

title

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474. (English)

1 reference

http://europepmc.org/abstract/PMC/5641481

9 July 2018

author

Marc P Baggelaar

8

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Thomas Hankemeier

23

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Annelot C M van Esbroeck

1

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Antonius P A Janssen

2

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Armand B Cognetta

3

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Daisuke Ogasawara

4

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Guy Shpak

5

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Mark van der Kroeg

6

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Vasudev Kantae

7

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Femke M de Vrij

9

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Hui Deng

10

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Marco Allarà

11

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Filomena Fezza

12

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Zhanmin Lin

13

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Tom van der Wel

14

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Marjolein Soethoudt

15

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Elliot D Mock

16

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Hans den Dulk

17

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Ilse L Baak

18

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Bogdan I Florea

19

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Giel Hendriks

20

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Luciano De Petrocellis

21

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Herman S Overkleeft

22

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Vincenzo Di Marzo

25

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Mauro Maccarrone

26

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Benjamin Cravatt

27

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Steven A Kushner

28

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

Mario van der Stelt

29

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

24

Chris I De Zeeuw

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

language of work or name

English

0 references

publication date

1 June 2017

1 reference

http://europepmc.org/abstract/PMC/5641481

9 July 2018

published in

Science

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

volume

356

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

issue

6342

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

page(s)

1084-1087

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

Acute Neurologic Disorder from an Inhibitor of Fatty Acid Amide Hydrolase

31 May 2020

cites work

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Implications of the BIA-102474-101 study for review of first-into-human clinical trials

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Selective N-Hydroxyhydantoin Carbamate Inhibitors of Mammalian Serine Hydrolases

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

A natural substrate-based fluorescence assay for inhibitor screening on diacylglycerol lipase α.

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Neuropathy target esterase impairments cause Oliver-McFarlane and Laurence-Moon syndromes.

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

The hereditary spastic paraplegia-related enzyme DDHD2 is a principal brain triglyceride lipase

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Loss-of-function mutations in PNPLA6 encoding neuropathy target esterase underlie pubertal failure and neurological deficits in Gordon Holmes syndrome

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Enzyme inhibitor discovery by activity-based protein profiling

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Prostamide F(2) α receptor antagonism combined with inhibition of FAAH may block the pro-inflammatory mediators formed following selective FAAH inhibition

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

The serine hydrolase ABHD6 Is a critical regulator of the metabolic syndrome

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Neuropathy target esterase (NTE): overview and future.

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

An efficient randomised, placebo-controlled clinical trial with the irreversible fatty acid amide hydrolase-1 inhibitor PF-04457845, which modulates endocannabinoids but fails to induce effective analgesia in patients with pain due to osteoarthritis

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Assessment of the pharmacology and tolerability of PF-04457845, an irreversible inhibitor of fatty acid amide hydrolase-1, in healthy subjects

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Mechanistic and Pharmacological Characterization of PF-04457845: A Highly Potent and Selective Fatty Acid Amide Hydrolase Inhibitor That Reduces Inflammatory and Noninflammatory Pain

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Molecular Characterization of Off-Target Activities of Telithromycin: a Potential Role for Nicotinic Acetylcholine Receptors

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2).

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Neuropathy target esterase: an essential enzyme for neural development and axonal maintenance

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo.

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Neuropathy target esterase is required for adult vertebrate axon maintenance

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Anandamide acts as an intracellular messenger amplifying Ca2+ influx via TRPV1 channels

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Modulation of anxiety through blockade of anandamide hydrolysis

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Cloning and expression of the murine sws/NTE gene

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Activity-based protein profiling: the serine hydrolases

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Isolation and structure of a brain constituent that binds to the cannabinoid receptor

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Scientists in the dark after French clinical trial proves fatal.

10 July 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6.

14 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain

14 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Enol carbamates as inhibitors of fatty acid amide hydrolase (FAAH) endowed with high selectivity for FAAH over the other targets of the endocannabinoid system

14 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

RPLC-ion-trap-FTMS method for lipid profiling of plasma: method validation and application to p53 mutant mouse model

14 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

Dual Effects of Anandamide on NMDA Receptor‐Mediated Responses and Neurotransmission

14 August 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=5641481

14 August 2018

Identifiers

DOI

10.1126/SCIENCE.AAF7497

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28596366%20AND%20SRC:MED&resulttype=core&format=json

31 May 2020

PubMed publication ID

28596366

1 reference