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Title:

Insights into the activity control of the kallikrein-related peptidase 6: small-molecule modulators and allosterism.

Document type:
Article; Journal Article; Research Support, Non-U.S. Gov't
Author(s):
Soualmia, Feryel; Bosc, Elodie; Amiri, Sabrina Aït; Stratmann, Dirk; Magdolen, Viktor; Darmoul, Dalila; Reboud-Ravaux, Michèle; El Amri, Chahrazade
Abstract:
The activity of kallikrein-related peptidase 6 (KLK6) is deregulated in various diseases such as cancer and neurodegenerative diseases. KLK6 is thus considered as an attractive therapeutical target. In this short report, we depict some novel findings on the regulation of the KLK6 activity. Namely, we identified mechanism-based inhibitors (suicide substrates) from an in-house library of 6-substituted coumarin-3-carboxylate derivatives. In addition, a molecular dynamics study evidenced the alloste...     »
Journal title abbreviation:
Biol Chem
Year:
2018
Journal volume:
399
Journal issue:
9
Pages contribution:
1073-1078
Fulltext / DOI:
doi:10.1515/hsz-2017-0336
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/29641412
Print-ISSN:
1431-6730
TUM Institution:
Frauenklinik und Poliklinik
 BibTeX