this invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject in need thereof , and preferably in a human subject . the methods of the invention utilize conjugates comprising two or more α4β1 small molecule antagonists covalently attached to a biocompatible polymer . these methods of selectively inhibiting α4β1 may be used modulate both normal and pathological biological processes mediated at least in part through α4β1 activity .