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Azido and Diazarinyl Analogues of Bis‐Tyrphostin as Asymmetrical Inhibitors of Dynamin GTPase |
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| Authors: | Luke R. Odell Dr. Ngoc Chau Anna Mariana Mark E. Graham Dr. Phillip J. Robinson Prof. Adam McCluskey Prof. |
| Affiliation: | 1. Chemistry, School of Environmental & Life Sciences, The University of Newcastle, University Drive, Callaghan, NSW 2308 (Australia), Fax: (+61)?249‐215472;2. Cell Signalling Unit, Children's Medical Research Institute, The University of Sydney, Locked Bag 23, Wentworthville, Sydney, NSW 2145 (Australia) |
| Abstract: | Probing the dynamin binding site : Bis‐tyrphostin ( 1 , Bis‐T), is a potent inhibitor of the phospholipid‐stimulated GTPase activity of dynamin I. Analogues of Bis‐T have significant potential as a biological probes for the dissection of endocytic pathways. Bis‐T‐derived compounds were synthesised and evaluated for their ability to inhibit the GTPase activity of dynamin I. Two analogues ( 23 and 24 ) represent the first asymmetrically substituted Bis‐T analogues to retain dynamin inhibition.  |
| Keywords: | bis‐tyrphostin dynamin GTPase I inhibitors photoaffinity synthesis |