What question did this study set out to answer?

To develop a nuclear magnetic resonance-based approach ("SAR by NMR") that identifies, optimizes, and links small organic molecules binding adjacent protein subsites to produce high-affinity ligands.

November 29, 1996Science

Discovering High-Affinity Ligands for Proteins: SAR by NMR

View Full Paper

Ask AI

Bookmark

Authors

SSSuzanne B. ShukerGeorgia Institute of Technology PHPhilip J. HajdukAbbVie (United States)RMRobert MeadowsUniversity of Surrey

Discussion

Member takes

Implication

Experimental study demonstrates rapid discovery of nanomolar FK506 binding protein ligands by tethering weak binders, indicating a streamlined approach for target-directed drug discovery.

Key Points

To develop a nuclear magnetic resonance-based approach ("SAR by NMR") that identifies, optimizes, and links small organic molecules binding adjacent protein subsites to produce high-affinity ligands.
Used NMR spectroscopy to identify and optimize small organic molecules that bind to proximal protein subsites.
Chemically linked two distinct ligands displaying micromolar binding affinities into a single molecule.
Rapidly produced linked compounds possessing nanomolar affinities for the target FK506 binding protein.
Decreased the extent of chemical synthesis and experimental time needed to generate high-affinity ligands for target-directed drug discovery.

Cite This Study

Shuker et al. (1996) studied this question.

synapsesocial.com/papers/69db18241e19c8ae088361b3 https://doi.org/10.1126/science.274.5292.1531

View Full Paper

Ask AI

Bookmark

Implication

Experimental study demonstrates rapid discovery of nanomolar FK506 binding protein ligands by tethering weak binders, indicating a streamlined approach for target-directed drug discovery.

Discovering High-Affinity Ligands for Proteins: SAR by NMR

Discussion

Member takes

Implication

Key Points

Cite This Study

Discovering High-Affinity Ligands for Proteins: SAR by NMR

Discussion

Member takes

Implication

Key Points

Cite This Study

Also Consider

Also Consider