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Title:

Targeted Delivery of Proteasome Inhibitors to Somatostatin-Receptor-Expressing Cancer Cells by Octreotide Conjugation.

Document type:
Journal Article; Research Support, Non-U.S. Gov't
Author(s):
Beck, Philipp; Cui, Haissi; Hegemann, Julian D; Marahiel, Mohammed A; Krüger, Achim; Groll, Michael
Abstract:
Clinical application of proteasome inhibitors (PIs) is so far limited to peripheral blood cancers due to the pronounced cytotoxicity towards all cell types. Targeted delivery of PIs could permit the treatment of other cancers along with decreasing side effects. Herein we describe the first small-molecule proteasome inhibitor conjugate for targeted delivery, created by fusing PIs to a synthetic ligand of somatostatin receptors, which are highly expressed in a variety of tumors. X-ray crystallogra...     »
Journal title abbreviation:
ChemMedChem
Year:
2015
Journal volume:
10
Journal issue:
12
Pages contribution:
1969-73
Language:
eng
Fulltext / DOI:
doi:10.1002/cmdc.201500449
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/26471124
Print-ISSN:
1860-7179
TUM Institution:
Institut für Experimentelle Onkologie und Therapieforschung
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