Abstract
Six bryostatins were isolated from Japanese bryozoan by evaluating their binding to the C1B domain of protein kinase Cδ (PKCδ). Structure-activity studies of bryostatins 4, 10, and 14 suggested that the ester group at C20 was not necessary for binding to and activating PKCδ. These bryostatins showed significant anti-tumor-promoting activity in induction tests with the Epstein-Barr virus early antigen.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antigens, Viral / metabolism
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / pharmacology
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B-Lymphocytes / drug effects*
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B-Lymphocytes / metabolism
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B-Lymphocytes / virology
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Bryostatins / isolation & purification*
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Bryostatins / pharmacology
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Bryozoa / chemistry*
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Enzyme Activation
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Herpesvirus 4, Human / physiology
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Humans
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Isoenzymes / chemistry
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Isoenzymes / metabolism
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Japan
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Protein Binding
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Protein Kinase C-delta / chemistry
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Protein Kinase C-delta / metabolism*
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Protein Structure, Tertiary
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Structure-Activity Relationship
Substances
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Antigens, Viral
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Antineoplastic Agents
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Bryostatins
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Epstein-Barr virus early antigen
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Isoenzymes
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Protein Kinase C-delta