Development of Selective RabGGTase Inhibitors and Crystal Structure of a RabGGTase–Inhibitor Complex (pages 3747–3750)
Zhong Guo, Yao-Wen Wu, Kui-Thong Tan, Robin S. Bon, Ester Guiu-Rozas, Christine Delon, Uyen T. Nguyen, Stefan Wetzel, Sabine Arndt, Roger S. Goody, Wulf Blankenfeldt, Kirill Alexandrov and Herbert Waldmann
Article first published online: 10 APR 2008 | DOI: 10.1002/anie.200705795
Stopping the transfer: Based on the structure of pepticinnamin E, specific inhibitors of Rab geranylgeranyl transferase (RabGGTase) with activity in cells were developed, and the first crystal structure of the enzyme in complex with an inhibitor is reported (see inhibitor structure and positioning in the active site of the enzyme). The findings may have implications for the chemical-biological study of Rab prenylation and vesicular transport and the involvement of RabGGTase in the establishment of disease.