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Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists.
- Source :
-
Future medicinal chemistry [Future Med Chem] 2015; Vol. 7 (10), pp. 1261-83. - Publication Year :
- 2015
-
Abstract
- Over the last 5 years, X-ray structures of CXCR4 in complex with three different ligands (the small-molecule antagonist IT1t, the polypeptide antagonist CVX15 and the viral chemokine antagonist vMIP-II) have been released. In addition to the inherent scientific value of these specific X-ray structures, they provide a reliable structural foundation for studies of the molecular interactions between CXCR4 and its key peptide ligands (CXCL12 and HIV-1 gp120), and serve as valuable templates for further development of small-molecule CXCR4 antagonists with therapeutic potential. We here review recent computational studies of the molecular interactions between CXCR4 and its peptide ligands - based on the X-ray structures of CXCR4 - and the current status of small-molecule peptide and peptidomimetic CXCR4 antagonists.
- Subjects :
- Animals
Drug Design
Humans
Models, Molecular
Receptors, CXCR4 chemistry
Receptors, CXCR4 metabolism
Peptides chemistry
Peptides pharmacology
Peptidomimetics chemistry
Peptidomimetics pharmacology
Receptors, CXCR4 antagonists & inhibitors
Small Molecule Libraries chemistry
Small Molecule Libraries pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1756-8927
- Volume :
- 7
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Future medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 26144264
- Full Text :
- https://doi.org/10.4155/fmc.15.64