Conformation-activity relationships of polyketide natural products.
Nat Prod Rep
; 32(8): 1183-206, 2015 Aug.
Article
em En
| MEDLINE
| ID: mdl-25974024
ABSTRACT
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Produtos Biológicos
/
Policetídeo Sintases
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Policetídeos
Limite:
Humans
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article