Some food proteins exhibit hypocholesteromic activity, which is largely associated with peptide fragments released after their enzymatic hydrolysis. This review provides a highlight of the recent progress on the hypocholesterolemic mechanisms of food protein-derived peptides, which include bile acid binding, inhibition of cholesterol micellar solubility and 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (statin-like activity), and targeting of proprotein convertase subtilisin/kexin type 9 interaction with low-density lipoprotein receptor, and sterol regulatory element-binding protein and hepatocyte nuclear factor 1α pathways.