Bioorganic & Medicinal Chemistry 2018-04-04

Screening of ligands for redox-active europium using magnetic resonance imaging

Brooke A. Corbin, Lina A. Basal, Susan A. White, Yimin Shen, E. Mark Haacke, Kenneth W. Fishbein, Matthew J. Allen

Index: 10.1016/j.bmc.2018.04.001

Full Text: HTML

Abstract

We report a screening procedure to predict ligand coordination to EuII and EuIII using magnetic resonance imaging in which bright images indicate complexation and dark images indicate no complexation. Here, paramagnetic GdIII is used as a surrogate for EuIII in the screening procedure to enable detection with magnetic resonance imaging. The screening procedure was tested using a set of eight ligands with known coordination to EuII and EuIII, and results were found to be consistent with expected binding. Validation of the screening procedure with known coordination chemistry enables use with new ligands in the future.

Latest Articles:

Development of concise two-step catalytic approach towards lasofoxifene precursor nafoxidine

2018-04-10

[10.1016/j.bmc.2018.04.021]

Substituent effect of N-benzylated gramine derivatives that prevent the PP2A inhibition and dissipate the neuronal Ca2+ overload, as a multitarget strategy for the treatment of Alzheimer’s disease

2018-04-09

[10.1016/j.bmc.2018.04.019]

Rational Design and Screening of Peptide-Based Inhibitors of Heat Shock Factor 1 (HSF1)

2018-04-07

[10.1016/j.bmc.2018.04.018]

Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells

2018-04-06

[10.1016/j.bmc.2018.04.016]

Site-Specific Incorporation of Quadricyclane into a Protein and Photocleavage of the Quadricyclane Ligation Adduct

2018-04-04

[10.1016/j.bmc.2018.04.009]

More Articles...