Article

Development of N-terminally modified variants of the CXCR4-antagonizing peptide EPI-X4 with increased plasma stability

2022-11-01

Abstract excerpt

EPI-X4 is a natural peptide antagonist of CXCR4, an established drug target in inflammatory diseases and cancer. Advanced derivatives of EPI-X4, such as EPI-X4 JM#21, have shown promising therapeutic effects in animal models of CXCR4-associated diseases but suffer from poor stability in blood. We here aimed to design and characterize EPI-X4 analogs that effectively antagonize CXCR4 while remaining stable in human...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 95aeba7f-12d9-5584-a80f-ae5f5e7df977
DOI: 10.22541/au.166733107.78559129/v1

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Development of N-terminally modified variants of the CXCR4-antagonizing peptide EPI-X4 with increased plasma stabilityDOI 10.22541/au.166733107.78559129/v1Read

Computational modeling and experimental validation of the EPI-X4/CXCR4 complex allows rational design of small peptide antagonistsSemantic proximity Read

Biomolecular models of EPI-X4 binding to CXCR4 allow the rational optimization of peptides with therapeutic potentialSemantic proximity Read

An optimized derivative of an endogenous CXCR4 antagonist prevents atopic dermatitis and airway inflammationSemantic proximity Read

Targeting of CXCR4 by the naturally occurring CXCR4 antagonist EPI-X 4 in Waldenström’s MacroglobulinemiaSemantic proximity Read

Absence of the CXCR4 Antagonist EPI-X4 from Pharmaceutical Human Serum Albumin PreparationsSemantic proximity Read

Differential activity and selectivity of N-terminal modified CXCL12 chemokines at the CXCR4 and ACKR3 receptors.Semantic proximity Read

CXCR4 signaling in health and disease.Semantic proximity Read

Designing small molecule CXCR3 antagonistsSemantic proximity Read

Dimeric peptides of the C-terminal region of CXCL14 function as CXCL12 inhibitors.Semantic proximity Read

CXCR4 Is a Potential Target for Anti-HIV Gene TherapySemantic proximity Read

The negative charge of the 343 site is essential for maintaining physiological functions of CXCR4.Semantic proximity Read

Mutational analysis of the extracellular disulphide bridges of the atypical chemokine receptor ACKR3/CXCR7 uncovers multiple binding and activation modes for its chemokine and endogenous non-chemokine agonists.Semantic proximity Read