Molecular Braille: A Novel Technology for Identification and Characterization of Compounds that Modulate Receptor Function

11/3/1999

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Molecular Braille: A Novel Technology for Identification and Characterization of Compounds that Modulate Receptor Function

Molecular Braille

Example: The Estrogen Receptor

Step 1: Peptide Isolation

Step 2: Peptide Validation

Peptide Validation: Two-Hybrid Analysis of Peptides to Verify Intracellular Binding

Peptides interact the same in cells and in vitro

Peptide Validation: The peptides disrupt ER/ERE mediated transcription

The a II, a/b III, and a/b V peptides inhibit tamoxifen partial agonist activity

Step 3: High Throughput Screening

A novel ER modulator identified during a peptide competition screen

NPC-0300 effects peptide binding to ER a with other compounds present

NPC-0300 effects peptide binding to ER b with other compounds present

Step 4: Compound Characterization and Optimization

Determination of a quantitative braille pattern

Compound Fingerprints with ER-a

Compound Fingerprints with ER-b

Author: Dale J. Christensen

Email: [email protected]

Home Page: http://www.novalon.com

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