Chemokines, which have chemotactic abilities, are comprised of a family of
small cytokines with 8-10 kilodaltons. Chemokines work in immune cells by trafficking and
regulating cell proliferation, migration, activation, differentiation, and homing. CXCR-4 is an
alpha-chemokine receptor specific for stromal-derived-factor-1 (SDF-1, also known as
CXCL12), which has been found to be expressed in more than 23 different types of cancers.
Recently, the SDF-1/CXCR-4 signaling pathway has emerged as a potential therapeutic target
for human tumor because of its critical role in tumor initiation and progression by activating
multiple signaling pathways, such as ERK1/2, ras, p38 MAPK, PLC/ MAPK, and SAPK/
JNK, as well as regulating cancer stem cells. CXCL12/CXCR4 antagonists have been produced,
which have shown encouraging results in anti-cancer activity. Here, we provide a brief
overview of the CXCL12/CXCR4 axis as a molecular target for cancer treatment. We also
review the potential utility of targeting CXCL12/CXCR4 axis in combination of immunotherapy
and/or chemotherapy based on up-to-date literature and ongoing research progress.