Abstract: Disclosed herein are methods for regulation of fat and/or cholesterol uptake from the gastrointestinal tract and/or regulation of plasma fat and/or cholesterol levels comprising administering to a mammal in need thereof an effective amount of a regulator of pancreatic IB PLA2 functionality. Also disclosed herein are methods of regulating the function of a polypeptide of interest comprising inserting of the 62-66 loop region of a pancreatic IB PLA2 amino acid sequence into the polypeptide of interest; and administering an effective amount of a regulatory molecule that effects its regulation through said amino acid sequence. Further disclosed are novel bile salt compounds that regulate pancreatic IB PLA2. Methods for detecting altered pancreatic IB PLA2 function and methods for identifying an agent suitable for regulating pancreatic IB PLA2 enzyme functionality are also disclosed.