The invention relates, in part, to of Glu-boroPro containing compounds and methods of use thereof in the prevention or management of conditions that are associated with impaired glucose tolerance such as diabetes. The invention also relates to compositions of Glu-boroPro containing compounds and methods of use thereof in the prevention or management of conditions such as metabolic syndrome, dyslipidemias, inflammation, cardiovascular disorders such as hypertension and atherosclerosis, and to reduce body weight or prevent weight gain. The compounds of the invention are also useful in lowering levels of triglycerides, free fatty acids, C-reactive protein (CRP), HbA1C, total glycosylated hemoglobin (TGHb), in increasing insulin sensitivity index and in stimulating insulin release.