The Chemistry and Biology of the Bryostatins: Potential PKC Inhibitors in Clinical Development

Title:The Chemistry and Biology of the Bryostatins: Potential PKC Inhibitors in Clinical Development

Volume: 19 Issue: 16

Author(s): B.-F. Ruan and H.-L. Zhu

Affiliation:

Keywords: Anti-cancer, bryostatin, PKC, alzheimer's disease, immunity, analogue, structure-activity relationship, learning and memory, clinical, natural products

Abstract: The bryostatins, powerful protein kinase C (PKC) agonists, are a family of complex macrolactone natural products. They are originally isolated from the marine bryozoan Bugula neritina. So far tweenty bryostatins have been obtained naturally and exhibit a remarkable range of biological activities, including antineoplastic activity, synergistic chemotheoreputic activity, cognition and memory enhancement, etc. Of the 20 known members, the most extensively studied is bryostatin 1. The effects of bryostatin 1 are mainly linked to its ability of selectively modulating the function of various individual protein kinase C (PKC) isozymes. Moreover, bryostatin 1, or in combination with other agents, has been proposed for phase I and phase II clinical trials. The bryostatins have excellent biological properties, but are scarce in nature. Therefore, it has attracted considerable interests in structural modification over the past two decades. In this review, we will attempt to summarize the main developments that have occurred in the structure-activity relationship and biology of bryostatins over the period 1982–2011.

Cite this article as:

Ruan B.-F. and Zhu H.-L., The Chemistry and Biology of the Bryostatins: Potential PKC Inhibitors in Clinical Development, Current Medicinal Chemistry 2012; 19 (16) . https://dx.doi.org/10.2174/092986712800493020