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A credit-card library approach for disrupting protein-protein interactions.

Abstract：

:Protein-protein interfaces are prominent in many therapeutically important targets. Using small organic molecules to disrupt protein-protein interactions is a current challenge in chemical biology. An important example of protein-protein interactions is provided by the Myc protein, which is frequently deregulated in human cancers. Myc belongs to the family of basic helix-loop-helix leucine zipper (bHLH-ZIP) transcription factors. It is biologically active only as heterodimer with the bHLH-ZIP protein Max. Herein, we report a new strategy for the disruption of protein-protein interactions that has been corroborated through the design and synthesis of a small parallel library composed of 'credit-card' compounds. These compounds are derived from a planar, aromatic scaffold and functionalized with four points of diversity. From a 285 membered library, several hits were obtained that disrupted the c-Myc-Max interaction and cellular functions of c-Myc. The IC50 values determined for this small focused library for the disruption of Myc-Max dimerization are quite potent, especially since small molecule antagonists of protein-protein interactions are notoriously difficult to find. Furthermore, several of the compounds were active at the cellular level as shown by their biological effects on Myc action in chicken embryo fibroblast assays. In light of our findings, this approach is considered a valuable addition to the armamentarium of new molecules being developed to interact with protein-protein interfaces. Finally, this strategy for disrupting protein-protein interactions should prove applicable to other families of proteins.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Xu Y,Shi J,Yamamoto N,Moss JA,Vogt PK,Janda KD

doi

10.1016/j.bmc.2005.11.052

subject

Has Abstract

pub_date

2006-04-15 00:00:00

pages

2660-73

issue

8

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)01139-9

journal_volume

14

pub_type

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