Abstract: Substantially pure preparations of cyclic boroProline compounds that bind, in cyclic or linear form, to CD26 are provided. Methods for using the cyclic compounds to stimulate the activation and/or proliferation of immune cells to achieve preselected normal in vivo levels of these cells also are provided. Evidence of the oral bioavailability and activity of a preferred cyclic compound, valine-prolineboronic acid (ValboroPro), also is provided.