Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner.


Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
22 09 2022
Historique:
pubmed: 9 9 2022
medline: 24 9 2022
entrez: 8 9 2022
Statut: ppublish

Résumé

Venglustat is a known allosteric inhibitor for ceramide glycosyltransferase, investigated in diseases caused by lysosomal dysfunction. Here, we identified venglustat as a potent inhibitor (IC

Identifiants

pubmed: 36074125
doi: 10.1021/acs.jmedchem.2c01050
pmc: PMC9813856
mid: NIHMS1859204
doi:

Substances chimiques

Carbamates 0
Ceramides 0
Enzyme Inhibitors 0
Quinuclidines 0
venglustat BLP1XA3FZA
Methyltransferases EC 2.1.1.-
Glycosyltransferases EC 2.4.-

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, N.I.H., Intramural

Langues

eng

Sous-ensembles de citation

IM

Pagination

12334-12345

Subventions

Organisme : NCI NIH HHS
ID : P30 CA023168
Pays : United States
Organisme : NCI NIH HHS
ID : U01 CA214649
Pays : United States

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Auteurs

Guangping Dong (G)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, Indiana 47907, United States.

Youchao Deng (Y)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, Indiana 47907, United States.

Adam Yasgar (A)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Ravi Yadav (R)

Department of Biological Sciences, Markey Center for Structural Biology, and the Purdue Institute of Inflammation, Immunology and Infectious Disease, Purdue University, West Lafayette, Indiana 47907, United States.

Daniel Talley (D)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Alexey V Zakharov (AV)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Sankalp Jain (S)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Ganesha Rai (G)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Nicholas Noinaj (N)

Department of Biological Sciences, Markey Center for Structural Biology, and the Purdue Institute of Inflammation, Immunology and Infectious Disease, Purdue University, West Lafayette, Indiana 47907, United States.

Anton Simeonov (A)

National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland 20850, United States.

Rong Huang (R)

Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, Indiana 47907, United States.

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