Bryostatins are a class of macrocyclic lactones. Bryostatins are potent modulators of Protein Kinase C (PKC). Bryostatin-1 was isolated from the marine invertebrate Bugula neritina. Bryostatin-1 is currently not available for commercial use.
Rationale for Targeting the PKC
PKC is a family of homologous serine/threonine protein Kinases that transduce signals linked to diverse cellular processes including proliferation, differentiation, angiogenesis, and apoptosis. The PKC family includes 12 isoforms subdivided into three major classes based on their cofactor requirements for activation. Aberrant regulation of the PKC enzymes activity has been demonstrated in a number of malignancies including: breast, colorectal, pancreatic, and non-small cell lung cancer.
Preclinical Activity of Bryostatin-1
Treatment of cancer cell lines with bryostatin-1 results in the activation of PKC. However, prolonged exposure to bryostatin-1 induces PKC inhibition most probably...
KeywordsChronic Lymphocytic Leukemia Gastric Cancer Cell Line Weekly Paclitaxel Macrocyclic Lactone Single Agent Activity
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