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Literature DB >> 30581241

Design of Stapled Oxyntomodulin Analogs Containing Functionalized Biphenyl Cross-Linkers.

Yulin Tian^1,2, Huafei Zou³, Peng An^1,2, Zhihong Zhou³, Weijun Shen³, Qing Lin^1,2.

Abstract

A panel of three lipid-modified, functionalized biphenyl cross-linkers (fBph) were synthesized and subsequently employed in the preparation of the stapled oxyntomodulin (OXM) analogs. In a luciferase-based reporter assay, these stapled OXM analogs showed varying degree of potency in activating GLP-1R and GCGR, presumably due to the disparate effect of the lipid chains on the local environment close to the ligand-receptor binding interface. In particular, the fBph-1 cross-linked peptide with the lipid chain attached to position-3 of the biphenyl cross-linker exhibited the highest dual agonist activity.

Entities: CellLine Chemical Disease Gene Species

Keywords: GCGR; GLP-1R; cross-linker; dual agonist; oxyntomodulin

Year: 2018 PMID： 30581241 PMCID： PMC6300064 DOI： 10.1016/j.tet.2018.11.060

Source DB: PubMed Journal: Tetrahedron ISSN： 0040-4020 Impact factor: 2.457

24 in total

1. Differential effects of oxyntomodulin and GLP-1 on glucose metabolism.

Authors: Xiaobing Du; Jennifer R Kosinski; Julie Lao; Xiaolan Shen; Aleksandr Petrov; Gary G Chicchi; George J Eiermann; Alessandro Pocai
Journal: Am J Physiol Endocrinol Metab Date: 2012-05-22 Impact factor: 4.310

2. Design of a long acting peptide functioning as both a glucagon-like peptide-1 receptor agonist and a glucagon receptor antagonist.

Authors: Clark Q Pan; Joanne M Buxton; Stephanie L Yung; Irene Tom; Ling Yang; Hongxing Chen; Margit MacDougall; Andrea Bell; Thomas H Claus; Kevin B Clairmont; James P Whelan
Journal: J Biol Chem Date: 2006-02-27 Impact factor: 5.157

3. Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction.

Authors: Avinash Muppidi; Xiaolong Li; Jiandong Chen; Qing Lin
Journal: Bioorg Med Chem Lett Date: 2011-10-12 Impact factor: 2.823

Review 4. Biologic actions and therapeutic potential of the proglucagon-derived peptides.

Authors: Daniel J Drucker
Journal: Nat Clin Pract Endocrinol Metab Date: 2005-11

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

Authors: Avinash Muppidi; Zhiyong Wang; Xiaolong Li; Jiandong Chen; Qing Lin
Journal: Chem Commun (Camb) Date: 2011-07-19 Impact factor: 6.222

Design of Stapled Oxyntomodulin Analogs Containing Functionalized Biphenyl Cross-Linkers.

1. Differential effects of oxyntomodulin and GLP-1 on glucose metabolism.

2. Design of a long acting peptide functioning as both a glucagon-like peptide-1 receptor agonist and a glucagon receptor antagonist.

3. Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction.

Review 4. Biologic actions and therapeutic potential of the proglucagon-derived peptides.

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

Review 6. The pharmacology of PEGylation: balancing PD with PK to generate novel therapeutics.

7. Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain.

8. Rational design of proteolytically stable, cell-permeable peptide-based selective Mcl-1 inhibitors.

9. One-point binding ligands for asymmetric gold catalysis: phosphoramidites with a TADDOL-related but acyclic backbone.

10. Bivalent argininamide-type neuropeptide y y(1) antagonists do not support the hypothesis of receptor dimerisation.

Review 1. Advances in therapeutic peptides targeting G protein-coupled receptors.

2. Design of Potent and Proteolytically Stable Biaryl-Stapled GLP-1R/GIPR Peptide Dual Agonists.