- Karumanchi, S Ananth;
- Jha, Vivekanand;
- Ramchandran, Ramani;
- Karihaloo, Anil;
- Tsiokas, Leonidas;
- Chan, Barden;
- Dhanabal, Mohanraj;
- Hanai, Jun-ichi;
- Venkataraman, Ganesh;
- Shriver, Zachary;
- Keiser, Nishla;
- Kalluri, Raghu;
- Zeng, Huiyan;
- Mukhopadhyay, Debabrata;
- Chen, Robert L;
- Lander, Arthur D;
- Hagihara, Kazuki;
- Yamaguchi, Yu;
- Sasisekharan, Ram;
- Cantley, Lloyd;
- Sukhatme, Vikas P
Endostatin, a collagen XVIII fragment, is a potent anti-angiogenic protein. We sought to identify its endothelial cell surface receptor(s). Alkaline phosphatase- tagged endostatin bound endothelial cells revealing two binding affinities. Expression cloning identified glypican, a cell surface proteoglycan as the lower-affinity receptor. Biochemical and genetic studies indicated that glypicans' heparan sulfate glycosaminoglycans were critical for endostatin binding. Furthermore, endostatin selected a specific octasulfated hexasaccharide from a sequence in heparin. We have also demonstrated a role for endostatin in renal tubular cell branching morphogenesis and show that glypicans serve as low-affinity receptors for endostatin in these cells, as in endothelial cells. Finally, antisense experiments suggest the critical importance of glypicans in mediating endostatin activities.