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Incorporating Target Protein Structure Flexibility and Dynamics in Computational Drug Discovery Using Ensemble-Based Docking Analysis

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Targeting FKBP isoforms with small-molecule ligands.

Elizabeth A Blackburn¹, Malcolm D Walkinshaw

¹The Centre for Translational and Chemical Biology, ISMB, University of Edinburgh, Edinburgh EH9 3JR, UK.

Current Opinion in Pharmacology

|August 2, 2011

Summary

FK506 binding protein (FKBP) drug targets offer therapeutic potential for cancer and neurological disorders. Comparing FKBP structures reveals conserved binding sites, enabling the design of specific inhibitors.

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Area of Science:

Biochemistry
Structural Biology
Pharmacology

Background:

The FK506 binding protein (FKBP) family comprises diverse protein isoforms modulating various cellular pathways.
FKBP proteins represent promising drug targets for treating cancer, neurodegenerative diseases, and psychiatric disorders.

Purpose of the Study:

To conduct a detailed sequence and structural comparison of human FKBP domains.
To identify conserved regions within FKBP binding sites for targeted drug design.

Main Methods:

Comparative analysis of available X-ray crystallographic and NMR structural data for human FKBP proteins.
Sequence and structural comparison of human FKBP domains.

Main Results:

Eight of fourteen human FKBP proteins, covering ten distinct FKBP domains, have available structural data.
The chemical scaffolds of immunosuppressive inhibitors FK506 and rapamycin bind to the most conserved region across FKBP binding sites.

Conclusions:

The conserved binding site region offers a strategic target for developing novel FKBP inhibitors.
This structural insight facilitates the design of isoform-specific FKBP inhibitors for targeted therapies.