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Development and Optimization of AlphaScreen Assay for Discovery of Galectin-1/-3 Inhibitors

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Date Issued:
2018
Abstract/Description:
Galectin-1 is a beta-galactoside-binding protein implicated in regulating apoptosis, cell proliferation and cell differentiation. The objective of our research was to develop and optimize an assay format for the discovery of new inhibitors of galectin-1 using AlphaScreen technology in a competitive binding configuration. Our efforts were hampered by the weak binding affinities of galectin-1 for its binding ligands (μM range). Consequently, the AlphaScreen assay could not have been developed at the level that would satisfy the guidelines from the National Chemical Genomics Center. Nevertheless, we have optimized the AlphaScreen assay for galectin-3, another member of galectin family, and screened an FDA approved oncology drug library (n = 101) from the NIH. We identified three possible inhibitors of galectin-3. These compounds showed a positive activity in dose response experiments: bleomycin (IC50 = 25.7 nM), cisplatin (IC50 = 127 nM), and mitoxantrone HCl (IC50 = 662 nM).
Title: Development and Optimization of AlphaScreen Assay for Discovery of Galectin-1/-3 Inhibitors.
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Name(s): Rivero, Yaima
Fitzgerald, Forrest
Cudic, Mare
Type of Resource: text
Genre: Poster
Date Created: 2018
Date Issued: 2018
Publisher: Florida Atlantic University
Place of Publication: Boca Raton, Florida
Physical Form: application/pdf
Extent: 1 p.
Language(s): English
Abstract/Description: Galectin-1 is a beta-galactoside-binding protein implicated in regulating apoptosis, cell proliferation and cell differentiation. The objective of our research was to develop and optimize an assay format for the discovery of new inhibitors of galectin-1 using AlphaScreen technology in a competitive binding configuration. Our efforts were hampered by the weak binding affinities of galectin-1 for its binding ligands (μM range). Consequently, the AlphaScreen assay could not have been developed at the level that would satisfy the guidelines from the National Chemical Genomics Center. Nevertheless, we have optimized the AlphaScreen assay for galectin-3, another member of galectin family, and screened an FDA approved oncology drug library (n = 101) from the NIH. We identified three possible inhibitors of galectin-3. These compounds showed a positive activity in dose response experiments: bleomycin (IC50 = 25.7 nM), cisplatin (IC50 = 127 nM), and mitoxantrone HCl (IC50 = 662 nM).
Identifier: FAU_SR00000050 (IID)
Collection: FAU Student Research Digital Collection
Subject(s): College students --Research --United States.
Held by: Florida Atlantic University Libraries
Sublocation: Digital Library
Persistent Link to This Record: http://purl.flvc.org/fau/fd/FAU_SR00000050
Restrictions on Access: Copyright © is held by the author, with permission granted to Florida Atlantic University to digitize, archive and distribute this item for non-profit research and educational purposes. Any reuse of this item in excess of fair use or other copyright exemptions requires permission of the copyright holder.
Host Institution: FAU
Is Part of Series: Florida Atlantic University Digital Library Collections.