Definition
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.
Characteristics
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...
References
Choi SH, Hyman T, Blumberg PM (2006) Differential effect of bryostatin 1 and phorbol 12-myristate 13-acetate on HOP-92 cell proliferation is mediated by down-regulation of protein kinase Cdelta. Cancer Res 66:7261–7269
Deacon EM, Pongracz J, Griffiths G et al (1997) Isoenzymes of protein kinase C: differential involvement in apoptosis and pathogenesis. Mol Pathol 50:124–131
Kortmansky J, Schwartz GK (2003) Bryostatin-1: a novel PKC inhibitor in clinical development. Cancer Invest 21:924–936
See Also
(2012) Kinase. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1943. doi: 10.1007/978-3-642-16483-5_3217
(2012) Thrombocytopenia. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3678. doi: 10.1007/978-3-642-16483-5_5792
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El-Rayes, B. (2015). Bryostatin-1. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27841-9_745-2
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DOI: https://doi.org/10.1007/978-3-642-27841-9_745-2
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Publisher Name: Springer, Berlin, Heidelberg
Online ISBN: 978-3-642-27841-9
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