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A screening platform based on epitope editing for drug discovery

biorxiv. 2019; 
Biyue Zhu, Jing Yang, Richard Van, Kathleen Ran, Keyi Yin, Yingxia Liang, Xunuo Shen, Wei Yin, Se Hoon Choi, Ying Lu, Changning Wang, Yihan Shao, Rudolph E. Tanzi, Can Zhang, Yan Cheng, Zhirong Zhang,  Chongzhao Ran
Products/Services Used Details Operation
Gene Synthesis All reagents were commercial products and used without further purification. CRANAD-Xs compounds were synthesized according to our previously reported procedures and compounds with purities more than 95% determined by analytical HPLC, were used for further evaluation.17, 24 Synthetic Aβ1-40 peptide was purchased from rPeptide and different forms of Aβ1-40 including monomer, oligomer and aggregate were prepared by our previously reported methods.17 Acetylated-K16 Aβ1-40 was purchased from GenScript Get A Quote

摘要

The interaction between an antibody and its epitope has been daily utilized in various biological studies; however it has been rarely explored whether small molecules can alter the interaction. We discovered that small molecules could alter/edit surface properties of amyloid beta (Aβ) epitopes, and consequently inhibit or enhance corresponding antibody recognition. Remarkably, this editing effect could generate functional changes including protein aggregation behaviors, cell cytokine secreting and in vivo microglia activation. According to this discovery, we proposed a screen platform based on epitope editing for drug discovery (SPEED). With a small library of compounds, we validated that SPEED could be u... More

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