| Literature DB >> 21827946 |
Matthew C Franklin1, Elizabeth C Navarro, Yujie Wang, Sheetal Patel, Pinki Singh, Yi Zhang, Kris Persaud, Amtul Bari, Heather Griffith, Leyi Shen, Paul Balderes, Paul Kussie.
Abstract
The anti-VEGF receptor 2 antibody IMC-1121B is a promising antiangiogenic drug being tested for treatment of breast and gastric cancer. We have determined the structure of the 1121B Fab fragment in complex with domain 3 of VEGFR2, as well as the structure of a different neutralizing anti-VEGFR2 antibody, 6.64, also in complex with VEGFR2 domain 3. The two Fab fragments bind at opposite ends of VEGFR2 domain 3; 1121B directly blocks VEGF binding, whereas 6.64 may prevent receptor dimerization by perturbing the domain 3:domain 4 interface. Mutagenesis reveals that residues essential for VEGF, 1121B, and 6.64 binding are nonoverlapping among the three contact patches.Entities:
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Year: 2011 PMID： 21827946 DOI： 10.1016/j.str.2011.01.019
Source DB: PubMed Journal: Structure ISSN： 0969-2126 Impact factor: 5.006