Isoprenylation is a posttranslational modification of proteins in which a farnesyl (15-carbon) or a
geranylgeranyl (20-carbon) group is attached to a C-terminal cysteine. Isoprenylation provides a protein
with abilities that allow it to interact with cell membrane and with other molecules. Such interactions are
essential to the biological functions of a significant number of proteins involved in the signaling of cell
growth, differentiation, cytoskeletal function and vesicle trafficking. Thus, isoprenylation is extremely
relevant to the development of transformation-related cell phenotypes. There are extensive works in the
literature documenting the involvement of prenylated protein or their downstream signaling partners in
various aspects of pathogenesis of hematological malignancies. This chapter reviews the importance of
isoprenylation and these proteins to the biology of hematological malignancies and analyzes the results of
clinical studies evaluating the use of inhibitors of protein prenylation in the treatment of these disorders.
Keywords: Isoprenoids, Protein Prenylation, Ras GTPases, MAPK Pathway, PI3K/PKB/AKT pathway,
Inhibitors of HMG-COA Reductase, Farnesyl Transferase Inhibitors, non-Hodgkin‘s lymphoma; Hodgkin‘s
lymphoma; Acute Myeloid Leukemia; Chronic Myeloid Leukemia; Myeloproliferative Disorders;
Polycythemia Vera.