Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 6, Pages 2490-2499Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01752
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Funding
- International Graduate School for Science and Engineering (IGSSE) of the Technische Universitat Munchen (TUM)
- Reinhart Koselleck Grant of the Deutsche Forschungsgemeinschaft [DFG KE 147/42-1]
- CIPSM
- PRIN [FCHJ8E]
- DFG [822/4-1]
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Specific targeting of the integrin subtype alpha 5 beta 1 possesses high potential in cancer diagnosis and therapy. Through sequential N-methylation, we successfully converted the biselective alpha 5 beta 1/alpha v beta 6 peptide c(phg-isoDGR-k) into a potent peptidic RGD binding aSfil subtype selective ligand c(phg-isoDGR-(NMe)k). Nuclear magnetic resonance spectroscopy and molecular modeling clarified the molecular basis of its improved selectivity profile. To demonstrate its potential in vivo, c(phg-isoDGR-(NMe)k) was trimerized with the chelator TRAP and used as a positron-emission tomography tracer for monitoring alpha 5 beta 1 integrin expression in a M21 mouse xenograft.
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