The integrin αvβ3 receptor is a promising target for anticancer therapy.^1,2 However, there are no effective marketed treatments targeting αvβ3. One possible limitation of Arginine-Glycine-Aspartic (RGD)-mimetic αvβ3 antagonists has been shown to cause partial agonism, which could induce major conformational changes that trigger paradoxical cell adhesion and angiogenesis.