New classes of potent heparanase inhibitors from ligand-based virtual screening.


Journal

Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203

Informations de publication

Date de publication:
Dec 2020
Historique:
entrez: 10 9 2020
pubmed: 11 9 2020
medline: 1 5 2021
Statut: ppublish

Résumé

Heparanase is a validated target in cancer therapy and a potential target for several inflammatory pathologies. A ligand-based virtual screening of commercial libraries was performed to expand the chemical space of small-molecule inhibitors. The screening was based on similarity with known inhibitors and was performed in several runs, starting from literature compounds and progressing through newly discovered inhibitors. Among the fifty-five tested compounds, nineteen had IC

Identifiants

pubmed: 32907434
doi: 10.1080/14756366.2020.1811701
pmc: PMC7534336
doi:

Substances chimiques

Amides 0
Enzyme Inhibitors 0
Ligands 0
heparanase EC 3.2.1.-
Glucuronidase EC 3.2.1.31

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1685-1696

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Auteurs

Daniele Pala (D)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Laura Scalvini (L)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Gian Marco Elisi (GM)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Alessio Lodola (A)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Marco Mor (M)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Gilberto Spadoni (G)

Dipartimento di Scienze Biomolecolari, Università degli Studi di Urbino "Carlo Bo", Urbino, Italy.

Fabiana F Ferrara (FF)

Takis s.r.l., Roma, Italy.

Emiliano Pavoni (E)

Takis s.r.l., Roma, Italy.

Giuseppe Roscilli (G)

Takis s.r.l., Roma, Italy.

Ferdinando M Milazzo (FM)

R&D Alfasigma S.p.A., Roma, Italy.

Gianfranco Battistuzzi (G)

R&D Alfasigma S.p.A., Roma, Italy.

Silvia Rivara (S)

Dipartimento di Scienze degli Alimenti e del Farmaco, Università degli Studi di Parma, Parma, Italy.

Giuseppe Giannini (G)

R&D Alfasigma S.p.A., Roma, Italy.

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Classifications MeSH