Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS.


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
11 Apr 2019
Historique:
received: 30 11 2018
accepted: 07 02 2019
entrez: 19 4 2019
pubmed: 19 4 2019
medline: 19 4 2019
Statut: epublish

Résumé

Acid-sensing ion channels (ASICs) are a family of ion channels permeable to cations and largely responsible for the onset of acid-evoked ion currents both in neurons and in different types of cancer cells, thus representing a potential target for drug discovery. Owing to the limited attention ASIC2 has received so far, an exploratory program was initiated to identify ASIC2 inhibitors using diminazene, a known 

Identifiants

pubmed: 30996808
doi: 10.1021/acsmedchemlett.8b00591
pmc: PMC6466820
doi:

Types de publication

Journal Article

Langues

eng

Pagination

627-632

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

Références

Physiol Rev. 2003 Oct;83(4):1183-221
pubmed: 14506304
Nat Biotechnol. 2006 Apr;24(4):439-46
pubmed: 16550174
J Biol Chem. 2006 Jul 14;281(28):19220-32
pubmed: 16704974
J Neurochem. 2008 Jul;106(1):429-41
pubmed: 18410516
Neuropharmacology. 2010 Jun;58(7):1045-53
pubmed: 20114056
Eur J Pharmacol. 2010 Dec 1;648(1-3):15-23
pubmed: 20854810
Am J Physiol Cell Physiol. 2012 Apr 1;302(7):C943-65
pubmed: 22277752
ACS Chem Neurosci. 2011 Jan 19;2(1):26-37
pubmed: 22778854
Nat Rev Neurosci. 2013 Jul;14(7):461-71
pubmed: 23783197
BMB Rep. 2013 Jun;46(6):295-304
pubmed: 23790972
Mol Biosyst. 2014 Oct;10(10):2724-34
pubmed: 25096593
Pharmacol Rev. 2015;67(1):1-35
pubmed: 25287517
Neuropharmacology. 2015 Jul;94:19-35
pubmed: 25613302
J Biomol Screen. 2016 Apr;21(4):372-80
pubmed: 26597957
Mol Brain. 2016 Jan 08;9:4
pubmed: 26746198
Br J Pharmacol. 2016 Sep;173(18):2671-701
pubmed: 27278329
J Cancer. 2016 Sep 13;7(13):1888-1891
pubmed: 27698929
Sci Rep. 2017 Mar 21;7:44843
pubmed: 28322303
J Exp Clin Cancer Res. 2017 Sep 19;36(1):130
pubmed: 28927426
Mol Pharmacol. 2017 Dec;92(6):665-675
pubmed: 29025967
Sci Rep. 2018 May 8;8(1):7179
pubmed: 29739981
PLoS One. 2018 May 21;13(5):e0196894
pubmed: 29782492

Auteurs

Leda Ivanova Bencheva (LI)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Marilenia De Matteo (M)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Luca Ferrante (L)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Marco Ferrara (M)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Adolfo Prandi (A)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Pietro Randazzo (P)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Silvano Ronzoni (S)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Roberta Sinisi (R)

Promidis, Via Olgettina 60, 20132 Milan, Italy.

Pierfausto Seneci (P)

Promidis, Via Olgettina 60, 20132 Milan, Italy.
Chemistry Department, Università degli Studi di Milano, Via Golgi 19, I-20133 Milan, Italy.

Vincenzo Summa (V)

IRBM Science Park, Via Pontina Km 30.600, 00070 Pomezia, Rome, Italy.

Mariana Gallo (M)

IRBM Science Park, Via Pontina Km 30.600, 00070 Pomezia, Rome, Italy.

Maria Veneziano (M)

IRBM Science Park, Via Pontina Km 30.600, 00070 Pomezia, Rome, Italy.

Antonella Cellucci (A)

IRBM Science Park, Via Pontina Km 30.600, 00070 Pomezia, Rome, Italy.

Nausicaa Mazzocchi (N)

San Raffaele Scientific Institute, Experimental Imaging Center, ALEMBIC, Advanced Light and Electron Microscopy BioImaging Center, Via Olgettina 60, 20132 Milan, Italy.

Andrea Menegon (A)

San Raffaele Scientific Institute, Experimental Imaging Center, ALEMBIC, Advanced Light and Electron Microscopy BioImaging Center, Via Olgettina 60, 20132 Milan, Italy.

Romano Di Fabio (R)

Promidis, Via Olgettina 60, 20132 Milan, Italy.
IRBM Science Park, Via Pontina Km 30.600, 00070 Pomezia, Rome, Italy.

Classifications MeSH