ChemBioChem

Cover image for Vol. 18 Issue 14

Editor: Meghan Campbell; Editorial Board Chairs: Thomas Carell, Donald Hilvert, Barbara Imperiali

Online ISSN: 1439-7633

Associated Title(s): ChemCatChem, ChemMedChem, ChemPhysChem, ChemSusChem

12_05/2011Cover Picture: STD and trNOESY NMR Study of Receptor–Ligand Interactions in Living Cancer Cells (ChemBioChem 5/2011)

The cover picture shows a schematic NMR tube in which our cyclic RGD mimic (targeting integrin αvβ3) interacts with a suspension of intact bladder cancer cells. The integrin αvβ3 overexpressed on the cell membrane is labelled in red. The interaction between small ligands and membrane-bound proteins can be observed by NMR techniques directly on living cells, without the need to isolate the protein receptor. The saturation transfer difference (STD) spectrum, shown on the right, identifies the epitope of the mimic. The insight provided by NMR spectroscopy is completed by docking calculations, thus defining the ligand's integrin-bound conformation and the ligand–receptor interactions at a molecular level. The binding mode of our RGD mimic into the crystal structure of the αvβ3 integrin is shown at the bottom. For further information, see the communication by D. Potenza et al. on p. 695 ff.

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