Literature DB >> 33488964

The Bicyclic Form of galacto-Noeurostegine Is a Potent Inhibitor of β-Galactocerebrosidase.

Agnete Viuff1, Stéphane Salamone1, Joseph McLoughlin2, Janet E Deane2, Henrik H Jensen1.   

Abstract

Competitive inhibitors of galactocerebrosidase (GALC) could be candidates for pharmacological chaperone therapy of patients with Krabbe disease. The known and selective nortropane-type iminosugar galacto-noeurostegine has been found to competitively inhibit GALC with K i = 7 μM at pH 4.6, which is 330-fold more potent than the analogous deoxynoeurostegine. It was shown through X-ray protein crystallography that galacto-noeurostegine binds to the active site of GALC in its bicyclic form.
© 2020 American Chemical Society.

Entities:  

Year:  2020        PMID： 33488964      PMCID： PMC7812600          DOI： 10.1021/acsmedchemlett.0c00377

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  16 in total

1.  Synthesis of uronic-noeurostegine--a potent bacterial β-glucuronidase inhibitor.

Authors:  Tina S Rasmussen; Heidi Koldsø; Shinpei Nakagawa; Atsushi Kato; Birgit Schiøtt; Henrik H Jensen
Journal:  Org Biomol Chem       Date:  2011-09-27       Impact factor: 3.876

Review 2.  Clinical management of Krabbe disease.

Authors:  Maria L Escolar; Tara West; Alessandra Dallavecchia; Michele D Poe; Kathleen LaPoint
Journal:  J Neurosci Res       Date:  2016-11       Impact factor: 4.164

Review 3.  Chaperones as potential therapeutics for Krabbe disease.

Authors:  Adriana Carol Eleonora Graziano; Giovanna Pannuzzo; Rosanna Avola; Venera Cardile
Journal:  J Neurosci Res       Date:  2016-11       Impact factor: 4.164

Review 4.  Krabbe disease: One Hundred years from the bedside to the bench to the bedside.

Authors:  David A Wenger; Mohammad A Rafi; Paola Luzi
Journal:  J Neurosci Res       Date:  2016-11       Impact factor: 4.164

5.  Insights into Krabbe disease from structures of galactocerebrosidase.

Authors:  Janet E Deane; Stephen C Graham; Nee Na Kim; Penelope E Stein; Rosamund McNair; M Begoña Cachón-González; Timothy M Cox; Randy J Read
Journal:  Proc Natl Acad Sci U S A       Date:  2011-08-29       Impact factor: 11.205

6.  Synthesis and evaluation of galacto-noeurostegine and its 2-deoxy analogue as glycosidase inhibitors.

Authors:  Stéphane Salamone; Lise L Clement; Agnete H Viuff; Ole Juul Andersen; Frank Jensen; Henrik H Jensen
Journal:  Org Biomol Chem       Date:  2015-06-26       Impact factor: 3.876

7.  Synthesis and evaluation of N-alkylated analogues of aza-galacto-fagomine - potential pharmacological chaperones for Krabbe disease.

Authors:  Agnete H Viuff; Henrik H Jensen
Journal:  Org Biomol Chem       Date:  2016-08-22       Impact factor: 3.876

8.  Azasugar inhibitors as pharmacological chaperones for Krabbe disease.

Authors:  Chris H Hill; Agnete H Viuff; Samantha J Spratley; Stéphane Salamone; Stig H Christensen; Randy J Read; Nigel W Moriarty; Henrik H Jensen; Janet E Deane
Journal:  Chem Sci       Date:  2015-03-30       Impact factor: 9.825

Review 9.  New therapeutic approaches for Krabbe disease: The potential of pharmacological chaperones.

Authors:  Samantha J Spratley; Janet E Deane
Journal:  J Neurosci Res       Date:  2016-11       Impact factor: 4.164

10.  Molecular Mechanisms of Disease Pathogenesis Differ in Krabbe Disease Variants.

Authors:  Samantha J Spratley; Chris H Hill; Agnete H Viuff; James R Edgar; Karsten Skjødt; Janet E Deane
Journal:  Traffic       Date:  2016-05-30       Impact factor: 6.215
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