Several peptides generated from food protein have been shown to be beneficial to one`s health. Peptides have the potential to be exploited as nutraceuticals and active components of functional foods. However, physiological evidence may not always support the purported health benefits. Low bioavailability of peptides is a major problem that restricts their use. This is mostly due to reaction with the food matrix during food product development, gastrointestinal instability, poor intestinal intake and physiological instability when consumed orally. Yeast derived peptides are explored with multifunctional health improving properties. This research considers the intestinal transport, bioavailability and bioactivity of the yeast derived peptide with a variety of health properties, such as antioxidant, antihypertensive, and immunomodulatory properties, focusing on molecular transport mechanisms, and the relationship between structure and transport mechanism. The transport mechanism will be considered using Caco-2 cells as model and in the presence of Gly-sar (inhibitor of PepT1), Cytochalasin D (inhibitor of paracellular route), and wortmannin (inhibitor of Transcytosis), following by HPLC, Ms-spectroscopy, and fluorescence microscopy analysis.