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Literature DB >> 21773579

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

Avinash Muppidi¹, Zhiyong Wang, Xiaolong Li, Jiandong Chen, Qing Lin.

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. This journal is © The Royal Society of Chemistry 2011

Entities: CellLine Chemical Disease Gene

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Year: 2011 PMID： 21773579 PMCID： PMC5428881 DOI： 10.1039/c1cc13320a

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

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Review 4. An enhanced functional interrogation/manipulation of intracellular signaling pathways with the peptide 'stapling' technology.

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6. Synthesis of cell-permeable stapled BH3 peptide-based Mcl-1 inhibitors containing simple aryl and vinylaryl cross-linkers.

Authors: Avinash Muppidi; Kenichiro Doi; Carlo P Ramil; Hong-Gang Wang; Qing Lin
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7. A new strategy for the in vitro selection of stapled peptide inhibitors by mRNA display.

Authors: Emil S Iqbal; Stacie L Richardson; Nicolas A Abrigo; Kara K Dods; H Estheban Osorio Franco; Heather S Gerrish; Hari Kiran Kotapati; Iain M Morgan; Douglas S Masterson; Matthew C T Hartman
Journal: Chem Commun (Camb) Date: 2019-07-10 Impact factor: 6.222