Conformation-activity relationships of polyketide natural products

Covering: up to the end of 2014 Polyketides represent an important class of secondary metabolites that interact with biological targets connected to a variety of disease-associated pathways. Remarkably, nature's assembly lines, polyketide synthases, manufacture these privileged structures throu...

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Bibliographic Details
Published in:Natural product reports 2015-08, Vol.32 (8), p.1183-126
Main Authors: Larsen, Erik M, Wilson, Matthew R, Taylor, Richard E
Format: Article
Language:English
Subjects:
Biological Products - chemistry
Biological Products - metabolism
Biological Products - pharmacology
Humans
Molecular Structure
Polyketide Synthases - metabolism
Polyketides - chemistry
Polyketides - metabolism
Polyketides - pharmacology
Stereoisomerism
Structure-Activity Relationship
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Summary:Covering: up to the end of 2014 Polyketides represent an important class of secondary metabolites that interact with biological targets connected to a variety of disease-associated pathways. Remarkably, nature's assembly lines, polyketide synthases, manufacture these privileged structures through a combinatorial mixture of just a few structural units. This review highlights the role of these structural elements in shaping a polyketide's conformational preferences, the use of computer-based molecular modeling and solution NMR studies in the identification of low-energy conformers, and the importance of conformational analogues in probing the bound conformation. In particular, this review covers several examples wherein conformational analysis complements classic structure-activity relationships in the design of biologically active natural product analogues. This review provides a comprehensive look into investigations that probe the conformational properties of polyketide natural products in order to exploit them in the design of bioactive analogues.
ISSN:0265-0568
1460-4752
DOI:10.1039/c5np00014a