Abstract
The screening of a small focused library of rhodanine derivatives as inhibitors of Bcl-2 proteins led to the discovery of two structurally related compounds with different binding profiles against the Bcl-XL and the Mcl-1 proteins. Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cyclin D1 / antagonists & inhibitors
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Cyclin D1 / genetics
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Cyclin D1 / metabolism*
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Fluorescence Polarization
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Inhibitory Concentration 50
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Mutagenesis, Site-Directed
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Spectrometry, Mass, Electrospray Ionization
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Structure-Activity Relationship
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Thiazolidines / chemical synthesis*
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Thiazolidines / chemistry
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Thiazolidines / pharmacology
Substances
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Antineoplastic Agents
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Thiazolidines
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Cyclin D1