Abstract
S100A1 is a member of the S100 family of Ca2+-binding proteins and regulates several cellular processes, including those involved in Ca2+ signaling and cardiac and skeletal muscle function. In Alzheimer's disease, brain S100A1 is overexpressed and gives rise to disease pathologies, making it a potential therapeutic target. The 2.25 Å resolution crystal structure of Ca2+-S100A1 is solved here and is compared with the structures of other S100 proteins, most notably S100B, which is a highly homologous S100-family member that is implicated in the progression of malignant melanoma. The observed structural differences in S100A1 versus S100B provide insights regarding target protein-binding specificity and for targeting these two S100 proteins in human diseases using structure-based drug-design approaches.
Keywords:
Alzheimer's disease; S100; S100A1; S100B; calcium-binding proteins; cardiomyopathy; crystal structure.
MeSH terms
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Amino Acid Sequence
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Binding Sites
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Calcium / chemistry*
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Calcium / metabolism
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Cations, Divalent
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Cloning, Molecular
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Crystallography, X-Ray
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Escherichia coli / genetics
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Escherichia coli / metabolism
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Gene Expression
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Genetic Vectors / chemistry
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Genetic Vectors / metabolism
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Humans
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Models, Molecular
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Protein Binding
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Protein Conformation, alpha-Helical
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Protein Interaction Domains and Motifs
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Protein Isoforms / chemistry
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Protein Isoforms / genetics
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Protein Isoforms / metabolism
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Protein Multimerization
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Recombinant Proteins / chemistry
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Recombinant Proteins / genetics
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Recombinant Proteins / metabolism
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S100 Calcium Binding Protein beta Subunit / chemistry*
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S100 Calcium Binding Protein beta Subunit / genetics
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S100 Calcium Binding Protein beta Subunit / metabolism
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S100 Proteins / chemistry*
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S100 Proteins / genetics
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S100 Proteins / metabolism
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Sequence Alignment
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Structural Homology, Protein
Substances
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Cations, Divalent
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Protein Isoforms
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Recombinant Proteins
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S100 Calcium Binding Protein beta Subunit
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S100 Proteins
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S100A1 protein
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S100B protein, human
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Calcium