Glucosylceramides (GluCer) are the most widely distributed glycosphingolipids in cells serving as precursors for the formation of over 200 known glycosphingolipids.  GluCer is formed by the glycosylation of ceramide in an organelle called Golgi via enzymes called glucosylceramide synthase (GCS) or by the breakdown of complex glycosphingolipids (GSLs) through the action of specific hydrolase enzymes.  In turn, certain β-glucosidases hydrolyze these lipids to regenerate ceramide.  GluCer appears to be synthesized in the inner leaflet of the Golgi.  Studies show that GluCer has to flip to the inside of the Golgi or transfer to the site of GSL synthesis to initiate the synthesis of complex GSLs.  Transferring to the GSL synthesis site is done with the help of a transport protein known as four phosphate adaptor protein 2 (FAPP2) while the flipping to the inside of the Golgi is made possible by the ABC transporter P-glycoprotein, also known as the multi-drug resistance 1 transporter (MDR1). GluCer is implicated in post-Golgi trafficking and drug resistance particularly to chemotherapeutic agents.  For instance, a study demonstrated a correlation between cellular drug resistance and modifications in GluCer metabolism.
In addition to their role as building blocks of biological membranes, glycosphingolipids have long attracted attention because of their supposed involvement in cell growth, differentiation, and formation of tumors.  The production of GluCer from Cer was found to be important in the growth of neurons or brain cells. On the other hand, pharmacological inhibition of GluCer synthase is being considered a technique to avoid insulin resistance.