|
|||||
|
|
A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase,YopH |
|
| Authors: | Fa Liu Ramin Mollaaghababa Hakami Beverly Dyas Medhanit Bahta George T Lountos David S Waugh Robert G Ulrich Terrence R Burke |
| Institution: | 1. Chemical Biology Laboratory, Molecular Discovery Program, Center for Cancer Research, National Cancer Institute, National Institutes of Health, NCI-Frederick, Frederick, MD 21702, USA;2. Faculty Research Participation Program, Oak Ridge Associated Universities, Belcamp, MD 21017, USA;3. Laboratory of Molecular Immunology, United States Army Medical Research Institute of Infectious Diseases, Frederick, MD 21702, USA;4. Macromolecular Crystallography Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, NCI-Frederick, Frederick, MD 21702, USA |
| Abstract: | A bivalent tethered approach toward YopH inhibitor development is presented that joins aldehydes with mixtures of bis-aminooxy-containing linkers using oxime coupling. The methodology is characterized by its facility and ease of use and its ability to rapidly identify low micromolar affinity inhibitors. The generality of the approach may potentially make it amenable to the development of bivalent inhibitors directed against other phosphatases. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |