Here we propose a novel universal assay strategy for monitoring small molecule-protein interactions in solution using strand displacement amplification (SDA) mediated by protein binding to small molecule with DNAzyme-based chemiluminescence detection. The DNA polymerase and nicking enzyme assisted SDA could...
An electro-optical single-molecule protein binding assay Molecular beacon-modified DNA carriers Full size image As an example, we incorporated a 15 mer thrombin-binding aptamer (TBA)38into the loop of the MB. TBA was selected due to its well-established structure, and high affinity towards throm...
Discovery of a small-molecule inhibitor of protein–microRNA interaction using binding assay with a site-specifically labeled Lin28. J. Am. Chem. Soc. 138, 13630–13638 (2016). Article CAS PubMed Google Scholar Lightfoot, H. L., Miska, E. A. & Balasubramanian, S. Identification of ...
assay at day 4 of EB-based differentiation to find factors which would promote the expression of red fluorescence protein (RFP) from the cardiac-specificMYH6(α-MHC gene) promoter[36]. They found onesmall molecule, Wnt inhibitor IWR1, was the most effective molecule at inducing MYH6-RFP ...
Photoaffinity and radiolabeled analogues of MPC-6827 were found to bind a 55-kDa protein, and this binding was competed by MPC-6827, paclitaxel, and colchicine, but not vinblastine. MPC-6827 effectively inhibited the polymerization of tubulin in vitro, competed with colchicine binding, and ...
1)PPI的最功利化的应用:Protein-protein interactions (PPIs) provide a rich source of drug targets for the development of new generation of clinical therapeutics 2)PPI inhibitor的先声:Bcl-2 inhibitor venetoclax 和LFA-1/ICAM-1 inhibitor lifitegrast ...
Through targeting G-quadruplexes, small-molecule ligands play pivotal roles in the regulation of c-Myc gene transcription. There are three basic binding modes of the ligands with G-quadruplexes (Fig. 8) [104, 119]: (1) external stacking: ligands with a π-delocalized system stack on the ...
A key histopathological hallmark of Alzheimer’s disease (AD) is the presence of neurofibrillary tangles of aggregated microtubule-associated protein tau in neurons. Anle138b is a small molecule which has previously shown efficacy in mice in reducing tau aggregates and rescuing AD disease phenotypes...
The biological rationale for targeting protein–protein interactions as a therapeutic strategy is strong, but identifying viable small-molecule drugs to achieve this has proved highly challenging. This article uses examples of successful discovery effort
A protein containing two or more topologically distinct binding sites that interact functionally with each other. SURFACE PLASMON RESONANCE A method for measuring binding interactions between a surface-immobilized molecule and a solution-phase analyte. The technology measures changes in refractive index caus...