• Corpus ID: 42339639

Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.

  title={Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.},
  author={Richard M. Keenan and William Henry Miller and Chet Kwon and Fadia E. Ali and James Francis Callahan and Raul R. Calvo and S. M. Hwang and Kenneth D. Kopple and Catherine E. Peishoff and James M. Samanen and Angela S. Wong and C K Yuan and William F. Huffman},
  journal={Journal of medicinal chemistry},
  volume={40 15},
Shear Stress Induced Release of Von Willebrand Factor and Thrombospondin-1 in Uvec Extracellular Matrix Enhances Breast Tumour Cell Adhesion
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The Significance of G Protein-Coupled Receptor Crystallography for Drug Discovery
Supporting by structure-activity relationship information arising from empirical screening, a unified structural model of GPCR activation/inactivation promises to both accelerate drug discovery in this field and improve the fundamental understanding of structure-based drug design in general.
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Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.
This is the first report of an orally active alpha(v)beta(3) antagonist that is effective at inhibiting bone resorption when dosed in a pharmaceutically acceptable fashion and may provide a novel therapeutic agent for the treatment of postmenopausal osteoporosis.
Integrins and cardiovascular disease
There is now solid evidence that the major integrin on platelets, the fibrinogen receptor αIIb  β3 , has an important role in several aspects of cardiovascular diseases and that its regulated inhibition leads to a reduction in incidence and mortality due to these disorders.