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Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.

ABSTRACT: We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.

SUBMITTER: Muppidi A

PROVIDER: S-EPMC5428881 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature

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Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.

Muppidi Avinash A Wang Zhiyong Z Li Xiaolong X Chen Jiandong J Lin Qing Q

Chemical communications (Cambridge, England) 20110719 33

We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity. ...[more]

PMID: 21773579

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