Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.


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:
14 Apr 2022
Historique:
received: 18 12 2021
accepted: 01 03 2022
entrez: 22 4 2022
pubmed: 23 4 2022
medline: 23 4 2022
Statut: epublish

Résumé

Phospholipase D (PLD) is a phospholipase enzyme responsible for hydrolyzing phosphatidylcholine into the lipid signaling molecule, phosphatidic acid, and choline. From a therapeutic perspective, PLD has been implicated in human cancer progression as well as a target for neurodegenerative diseases, including Alzheimer's. Moreover, knockdown of PLD rescues the ALS phenotype in multiple

Identifiants

pubmed: 35450377
doi: 10.1021/acsmedchemlett.1c00682
pmc: PMC9014516
doi:

Types de publication

Journal Article

Langues

eng

Pagination

665-673

Informations de copyright

© 2022 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Tricia L May-Dracka (TL)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Fang Gao (F)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Brian T Hopkins (BT)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Xiaoping Hronowski (X)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

TeYu Chen (T)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Jayanth V Chodaparambil (JV)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Claire M Metrick (CM)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Mike Cullivan (M)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Istvan Enyedy (I)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Maciej Kaliszczak (M)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Mark W Kankel (MW)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Isaac Marx (I)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Mackenzie A Michell-Robinson (MA)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Param Murugan (P)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

P Rajesh Kumar (PR)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Michael Rooney (M)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Eli Schuman (E)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Anindya Sen (A)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Ti Wang (T)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Tao Ye (T)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Emily A Peterson (EA)

Biotherapeutic and Medicinal Sciences, Neuromuscular & Movement Disorders Research Unit, Research and Early Development Biomarkers, Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.

Classifications MeSH