Ontology highlight
ABSTRACT:
SUBMITTER: Jarvis A
PROVIDER: S-EPMC2841442 | biostudies-literature | 2010 Mar
REPOSITORIES: biostudies-literature
Jarvis Ashley A Allerston Charles K CK Jia Haiyan H Herzog Birger B Garza-Garcia Acely A Winfield Natalie N Ellard Katie K Aqil Rehan R Lynch Rosemary R Chapman Chris C Hartzoulakis Basil B Nally James J Stewart Mark M Cheng Lili L Menon Malini M Tickner Michelle M Djordjevic Snezana S Driscoll Paul C PC Zachary Ian I Selwood David L DL
Journal of medicinal chemistry 20100301 5
We report the molecular design and synthesis of EG00229, 2, the first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRP1) and the structural characterization of NRP1-ligand complexes by NMR spectroscopy and X-ray crystallography. Mutagenesis studies localized VEGF-A binding in the NRP1 b1 domain and a peptide fragment of VEGF-A was shown to bind at the same site by NMR, providing the basis for small molecule design. Compound 2 demonstrated inhibition of VEGF-A binding to NRP1 and a ...[more]