Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH-CH(CH2-S03H)COOH or Arg-Gly-NII-CH(CH2-S03H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, steroisomers, multimers, cyclic forms, linear forms, drug-conjugates, prodrugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibition cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.