Our demonstration of a successful assay for screening specific protein palmitoylation inhibitors opens the door to inhibiting palmitoylation in proteins responsible for a variety of human diseases, including hyper/autoimmunity (e.g. Lck, CD4, CD8), cardiovascular disease (phospholemman), neurodegenerative disease (Huntingtin), viral infection (influenza hemagglutinin), and a large subset of cancers (estrogen receptor, Ras, Fyn). Here, LCK is linked to cancer.