3S1B: The Development Of Peptide-Based Tools For The Analysis Of Angiogenesis

Limitations to the application of molecularly targeted cancer therapies are the inability to accurately match patient with effective treatment and the absence of a prompt readout of posttreatment response. Noninvasive agents that rapidly report vascular endothelial growth factor (VEGF) levels using positron emission tomography (PET) have the potential to enhance anti-angiogenesis therapies. Using phage display, two distinct classes of peptides were identified that bind to VEGF with nanomolar affinity and high selectivity. Co-crystal structures of these different peptide classes demonstrate that both bind to the receptor-binding region of VEGF. (18)F-radiolabelling of these peptides facilitated the acquisition of PET images of tumor VEGF levels in a HM7 xenograph model. The images obtained from one 59-residue probe, (18)F-Z-3B, 2 hr postinjection are comparable to those obtained with anti-VEGF antibody B20 72 hr postinjection. Furthermore, VEGF levels in growing SKOV3 tumors were followed using (18)F-Z-3B as a PET probe with VEGF levels increasing with tumor size.
PDB ID: 3S1BDownload
MMDB ID: 92761
PDB Deposition Date: 2011/5/14
Updated in MMDB: 2011/08
Experimental Method:
x-ray diffraction
Resolution: 2.9  Å
Source Organism:
Homo sapiens
Similar Structures:
Biological Unit for 3S1B: tetrameric; determined by author and by software (PISA)
Molecular Components in 3S1B
Label Count Molecule
Proteins (4 molecules)
Vascular Endothelial Growth Factor a(Gene symbol: VEGFA)
Molecule annotation
Molecule annotation
* Click molecule labels to explore molecular sequence information.

Citing MMDB