Abstract
Transcription factors of the NFAT family regulate the production of effector proteins that coordinate the immune response. The immunosuppressive drugs FK506 and cyclosporin A (CsA) act by blocking a Ca2+-mediated signalling pathway leading to NFAT. Although FK506 and CsA have enabled human organs to be transplanted routinely, the toxic side-effects of these drugs limit their usage. This toxicity might be absent in antagonists that target NFAT directly. As a first step in the structure-based search for NFAT antagonists, we now report the identification and solution structure of a 20K domain of NFATc (NFATc-DBD) that is both necessary and sufficient to bind DNA and activate transcription cooperatively. Although the overall fold of the NFATc DNA-binding domain is related to that of NF-kappaB p50 (refs 2, 3), the two proteins use significantly different strategies for DNA recognition. On the basis of these results, we present a model for the cooperative complex formed between NFAT and the mitogenic transcription factor AP-1 on the interleukin-2 enhancer.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amino Acid Sequence
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Binding Sites
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Cloning, Molecular
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Crystallography, X-Ray
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DNA / metabolism
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DNA-Binding Proteins / chemistry*
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DNA-Binding Proteins / genetics
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DNA-Binding Proteins / metabolism
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Enhancer Elements, Genetic
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Escherichia coli
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Humans
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Interleukin-2 / genetics
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Sequence Data
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NF-kappa B / chemistry
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NFATC Transcription Factors
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Nuclear Proteins*
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Protein Conformation*
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Proto-Oncogene Proteins / chemistry*
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Proto-Oncogene Proteins c-rel
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Recombinant Proteins / chemistry
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Recombinant Proteins / metabolism
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Sequence Homology, Amino Acid
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Transcription Factor AP-1 / metabolism
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Transcription Factors / chemistry*
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Transcription Factors / genetics
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Transcription Factors / metabolism
Substances
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DNA-Binding Proteins
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Interleukin-2
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NF-kappa B
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NFATC Transcription Factors
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Nuclear Proteins
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Proto-Oncogene Proteins
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Proto-Oncogene Proteins c-rel
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Recombinant Proteins
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Transcription Factor AP-1
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Transcription Factors
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DNA