Small-molecule inhibitors of IL-2/IL-2R: lessons learned and applied.
Curr Top Microbiol Immunol
; 348: 25-59, 2011.
Article
em En
| MEDLINE
| ID: mdl-20703966
ABSTRACT
The IL-2IL-2R protein-protein interaction is of central importance to both healthy and diseased immune responses, and is one of the earliest examples of successful small-molecule inhibitor discovery against this target class. Drug-like inhibitors of IL-2 have been identified through a combination of fragment discovery, structure-based design, and medicinal chemistry; this discovery approach illustrates the importance of using a diverse range of complementary screening methods and analytical tools to achieve a comprehensive understanding of molecular recognition. The IL-2 story also provides insight into the dynamic nature of protein-protein interaction surfaces, their potential druggability, and the physical and chemical properties of effective small-molecule ligands. These lessons, from IL-2 and similar discovery programs, underscore an increasing awareness of the principles governing the development of drugs for protein-protein interactions.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Linfocinas
/
Interleucina-2
/
Subunidade alfa de Receptor de Interleucina-2
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
Curr Top Microbiol Immunol
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos