Structure-guided development of selective RabGGTase inhibitors

Bon, Robin S., Guo, Zhong, Stigter, E. Anouk, Wetzel, Stefan, Menninger, Sacha, Wolf, Alexander, Choidas, Axel, Alexandrov, Kirill, Blankenfeldt, Wulf, Goody, Roger S. and Waldmann, Herbert (2011) Structure-guided development of selective RabGGTase inhibitors. Angewandte Chemie (International Edition), 50 21: 4957-4961. doi:10.1002/anie.201101210


Author Bon, Robin S.
Guo, Zhong
Stigter, E. Anouk
Wetzel, Stefan
Menninger, Sacha
Wolf, Alexander
Choidas, Axel
Alexandrov, Kirill
Blankenfeldt, Wulf
Goody, Roger S.
Waldmann, Herbert
Title Structure-guided development of selective RabGGTase inhibitors
Journal name Angewandte Chemie (International Edition)   Check publisher's open access policy
ISSN 1433-7851
1521-3773
Publication date 2011-05
Sub-type Article (original research)
DOI 10.1002/anie.201101210
Volume 50
Issue 21
Start page 4957
End page 4961
Total pages 5
Place of publication Weinheim, Germany
Publisher Wiley - V C H Verlag GmbH & Co. KGaA
Collection year 2012
Language eng
Formatted abstract
Designing for selectivity: A combination of protein crystal-structure analysis, virtual screening, and synthetic chemistry has been used to develop noncytotoxic inhibitors of RabGGTase (IC 50: 42nM for the example shown; red O, blue N, yellow S) that are selective over FTase and GGTaseI. Furthermore, the inhibitors display cellular activity and inhibit cancer cell proliferation.
Keyword Antitumor Agents
Drug Design
Inhibitors
Protein modification
Transferases
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

 
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Created: Wed, 07 Mar 2012, 14:38:31 EST by Susan Allen on behalf of Institute for Molecular Bioscience