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Stapling eif4e interacting peptides

An unnatural amino acid, free technology, applied in the field of molecular biology

Inactive Publication Date: 2016-01-20
AGENCY FOR SCI TECH & RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

To date, no such drug-like inhibitors of eIF4E-cap interaction have been reported

Method used

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  • Stapling eif4e interacting peptides
  • Stapling eif4e interacting peptides
  • Stapling eif4e interacting peptides

Examples

Experimental program
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Embodiment approach

[0170] Inhibition of the protein interface between eIF4E and eIF4G is attractive for designing anticancer therapeutics. Peptides derived from eIF4G1 and 4EBP1 (inhibitors of eIF4E:eIF4G interaction) containing residues responsible for their interaction with eIF4E (YXXXXLΦ motif, where Φ denotes any hydrophobic residue) are structural mimics of each other. Tyrosine (Y4) ( image 3 ) is involved in various van der Waals contacts with eIF4E and the h-bond between its side chain hydroxyl and the carbonyl backbone of P38 of eIF4E. Leucine (L9) creates a shallow cavity on the surface of eIF4E and interacts with W73 of eIF4E through an h-bond between its backbone and the indole of tryptophan. A conserved hydrophobic residue (L10) squeezes L131 and L135 of eIF4E. The crystal structures of the two peptides in complex with eIF4E were approximately 50% α-helical; however, they contained negligible helical content in solution.

[0171] Therefore, the present inventors have improved sma...

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Abstract

The present invention relates to cross-linked peptides that are associated with human eIF4G and bind to eIF4E, uses thereof and pharmaceutical compositions comprising the peptides.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of priority from Singapore Application No. 201302065-6, filed 21 March 2013, and Singapore Application No. 201400336-2, filed 15 January 2014, the contents of which are for all purposes at This is incorporated by reference in its entirety. technical field [0003] The present invention belongs to the field of molecular biology and relates to cross-linked peptides and their pharmaceutical use. Background technique [0004] Human eukaryotic translation initiation factor 4E (eIF4E) binds to the cap structure (m 7 GTP) to initiate cap-dependent translation. eIF4F is often overexpressed in a large number of cancers and leads to increased translation of oncogenic proteins through deregulated cap-dependent translation. Inhibitors of the eIF4E:eIF4G interaction represent a viable approach that would normalize cap-dependent translation in cancer cells. [0005] mRNAs are assumed to compet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K7/06A61K38/10A61K38/08A61P35/00
CPCC07K14/4705A61K38/00A61P35/00C07K7/08
Inventor 克里斯托弗·约翰·布朗大卫·菲利普·雷恩柯淑婷迪尔拉什·拉玛钱德拉·谢卡尔·韦尔马
Owner AGENCY FOR SCI TECH & RES
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