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Oncogenic protein interfaces: small molecules, big challenges
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DOI：10.1038/nrc3690.png)
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Historically, targeting protein-protein interactions with small molecules was not thought possible because the corresponding interfaces were considered mostly flat and featureless and therefore 'undruggable'. Instead, such interactions were targeted with larger molecules, such as peptides and antibodies. However, the past decade has seen encouraging breakthroughs through the refinement of existing techniques and the development of new ones, together with the identification and exploitation of unexpected aspects of protein-protein interaction surfaces. In this Review, we describe some of the latest techniques to discover modulators of protein-protein interactions and how current drug discovery approaches have been adapted to successfully target these interfaces.
Keyword:
PAN-BCL-2 FAMILY ANTAGONIST
HIGH-HANGING FRUIT
DRUG DISCOVERY
PHASE-I
HOT-SPOT
POTENT ANTAGONISTS
OBATOCLAX MESYLATE
CRYSTAL-STRUCTURE
NEXT-GENERATION
INHIBITORS
期刊
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66.8
论文数:
3.8K
被引数:
6.0W
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引用论文
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