Identification of a potential allosteric site of Golgi α-mannosidase II using computer-aided drug design.


Journal

PloS one
ISSN: 1932-6203
Titre abrégé: PLoS One
Pays: United States
ID NLM: 101285081

Informations de publication

Date de publication:
2019
Historique:
received: 29 11 2018
accepted: 15 04 2019
entrez: 9 5 2019
pubmed: 9 5 2019
medline: 22 1 2020
Statut: epublish

Résumé

Golgi α-mannosidase II (GMII) is a glycoside hydrolase playing a crucial role in the N-glycosylation pathway. In various tumour cell lines, the distribution of N-linked sugars on the cell surface is modified and correlates with the progression of tumour metastasis. GMII therefore is a possible molecular target for anticancer agents. Here, we describe the identification of a non-competitive GMII inhibitor using computer-aided drug design methods including identification of a possible allosteric binding site, pharmacophore search and virtual screening.

Identifiants

pubmed: 31067280
doi: 10.1371/journal.pone.0216132
pii: PONE-D-18-34266
pmc: PMC6505943
doi:

Substances chimiques

Recombinant Proteins 0
alpha-Mannosidase EC 3.2.1.24

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

e0216132

Déclaration de conflit d'intérêts

The authors have declared that no competing interests exist.

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Auteurs

Lina Irsheid (L)

Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany.

Thomas Wehler (T)

Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany.
Department of Biomedicine, University of Bergen, Bergen, Norway.

Christoph Borek (C)

Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany.

Werner Kiefer (W)

Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany.

Ruth Brenk (R)

Department of Biomedicine, University of Bergen, Bergen, Norway.

Maria Elena Ortiz-Soto (ME)

Institute of Organic Chemistry, University of Würzburg, Würzburg, Germany.

Jürgen Seibel (J)

Institute of Organic Chemistry, University of Würzburg, Würzburg, Germany.

Tanja Schirmeister (T)

Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany.

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Classifications MeSH