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- Title
The structure of a small GTPaseRhoA in complex with PDZRhoGEF and the inhibitor HL47.
- Authors
Yan, Zhaowei; Ma, Sheng; Zhang, Yan; Ma, La; Wang, Feng; Li, Jian; Miao, Liyan
- Abstract
Objectives: To study the structure of a small GTPaseRhoA in complex with PDZRhoGEF and the inhibitor HL47, and to provide an easier template for R&D of RhoA inhibitor. Results: Our initial attempts to obtain a binary complex of RhoA with the inhibitor HL47 were unsuccessful probably due to the presence of GDP. By targeting a ternary complex involving the RhoA-specific guanine nucleotide exchange factor PDZRhoGEF, we eliminated GDP and obtained a 2.3 Å structure of the RhoA-PDZRhoGEF-inhibitor HL47 ternary complex. Conclusion: This structure provides a new template for target-based pharmaceutical design against RhoA.
- Subjects
RHO GTPases; GUANOSINE triphosphatase; PDZ proteins; X-ray diffraction; GUANINE nucleotide exchange factors
- Publication
Biotechnology Letters, 2017, Vol 39, Issue 5, p745
- ISSN
0141-5492
- Publication type
Article
- DOI
10.1007/s10529-017-2292-7