The chemistry and biology of the bryostatins: potential PKC inhibitors in clinical development.

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.

journal_name

Curr Med Chem

authors

Ruan BF,Zhu HL

doi

10.2174/092986712800493020

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

2652-64

issue

16

eissn

0929-8673

issn

1875-533X

pii

CMC-EPUB-20120416-003

journal_volume

19

pub_type

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