Improved Surface Display of Human Hyal1 and Identification of Testosterone Propionate and Chicoric Acid as New Inhibitors.

autodisplay hyal1 hyaluronic acid hyaluronidase inhibitors

Journal

Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453

Informations de publication

Date de publication:
26 Mar 2020
Historique:
received: 03 02 2020
revised: 18 03 2020
accepted: 24 03 2020
entrez: 1 4 2020
pubmed: 1 4 2020
medline: 1 4 2020
Statut: epublish

Résumé

Degradation of high molecular weight hyaluronic acid (HA) in humans is mainly catalyzed by hyaluronidase Hyal1. This enzyme is involved in many pathophysiological processes and therefore appears an interesting target for drug discovery. Until now, only a few inhibitors of human Hyal1 are known due to obstacles in obtaining active enzymes for inhibitor screening. The aim of the present work was to provide a convenient enzyme activity assay and show its feasibility by the identification of new inhibitors. By autodisplay,

Identifiants

pubmed: 32224932
pii: ph13040054
doi: 10.3390/ph13040054
pmc: PMC7243119
pii:
doi:

Types de publication

Journal Article

Langues

eng

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Auteurs

Isabelle Lengers (I)

Institute of Pharmaceutical and Medicinal Chemistry, PharmaCampus, Westfälische WilhelmsUniverstität Münster, 48149 Münster, Germany.

Fabian Herrmann (F)

Institute of Pharmaceutical Biology and Phytochemistry, PharmaCampus, Westfälische WilhelmsUniverstität Münster, 48149 Münster, Germany.

Marc Le Borgne (M)

Université de Lyon, Université Claude Bernard Lyon 1, Faculté de Pharmacie-ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453-INSERM US7, 8 Avenue Rockefeller, F-69373 Lyon CEDEX 8, France.

Joachim Jose (J)

Institute of Pharmaceutical and Medicinal Chemistry, PharmaCampus, Westfälische WilhelmsUniverstität Münster, 48149 Münster, Germany.

Classifications MeSH