Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Bryostatin-1

  • Bassel El-Rayes
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_745-2

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...

Keywords

Chronic Lymphocytic Leukemia Gastric Cancer Cell Line Weekly Paclitaxel Macrocyclic Lactone Single Agent Activity 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. 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 66:7261–7269CrossRefPubMedGoogle Scholar
  2. Deacon EM, Pongracz J, Griffiths G et al (1997) Isoenzymes of protein kinase C: differential involvement in apoptosis and pathogenesis. Mol Pathol 50:124–131CrossRefPubMedPubMedCentralGoogle Scholar
  3. Kortmansky J, Schwartz GK (2003) Bryostatin-1: a novel PKC inhibitor in clinical development. Cancer Invest 21:924–936CrossRefPubMedGoogle Scholar

See Also

  1. (2012) Kinase. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1943. doi: 10.1007/978-3-642-16483-5_3217Google Scholar
  2. (2012) Thrombocytopenia. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3678. doi: 10.1007/978-3-642-16483-5_5792Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Department of Hematology and Medical OncologyEmory University School of MedicineAtlantaUSA
  2. 2.Winship Cancer Institute of Emory UniversityAtlantaUSA