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Oxidosqualene cyclase inhibitors as potential ipocholesterolemic, antifungal or antiprotozoaric drugs - CONCLUDED

Periodo
Fino al 01/04/2017
Coordinatore/trice
Prof. Gianni BALLIANO

Aree / Gruppi di ricerca

Partecipanti al progetto

Descrizione del progetto

upload_A2_oxidosqualene.jpg

Members of other units:

Dr. Henrietta Dehmlow, Gasch Hoffman-La Roche, Basilea-Swizerland
Prof. Armin Ruf, Gasch Hoffman-La Roche, Basilea-Swizerland
Dr. Tanja Schulz, Gasch Hoffman-La Roche, Basilea-Swizerland
Prof. Franz Bracher, Department Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität München, Germany

Partners:
Gasch Hoffman-La Roche, Basilea-Swizerland
Department Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität München, Germany 

Description

Objectives:
The study of structure activity relationship of inhibitors of:

  • human oxidosqualene cyclase (lanosterol synthase): a target for new inhibitors with hypocholestemic activity
  • yeast oxidosqualene cyclase: a target for new inhibitors with antifungal activity
  • oxidosqualene cyclases of patogen organisms (T. cruzi, P. carinii, C. albicans) expressed in non-patogen systems (yeasts) for preliminary inhibition studies.

The site-directed mutagenesis of the active site and of the access channel of oxidosqualene cyclase to find molecular targets for inhibition.

The study of subcellular distribution and direct or regulative interactions with the steroidogenesis enzymes: implication for membrane functions and regulation of cell proliferation.

Techiques and facilities:

  • in vitro enzyme activity tests
  • tracing of intermediate metabolites with radiolabelled precursor
  • protein electrophoresis and western blot
  • molecular biology laboratory for the production of recombinant proteins in bacterial and yeast cells
  • bacterial, yeast and human cell culture
  • fully equipped laboratory for radioactive molecules

Keywords:
oxidosqualene cyclase, lanosterol synthase, bacterial hopene cyclase, Cholesterol, Cholesterol biosynthesis, Inhibitors, Postsqualene sterol biosynthesis, Antitumoral activity, Receptor ligand, Antifungal activity, Cholesterol lowering drug, Hypocholesterolemic activity, Site-directed mutagenesis, Enzymatic activity

Links:
PDB molecule of the month: oxidosqualene cyclase

Ultimo aggiornamento: 03/07/2017 16:08
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