PTHrP exerts its effects by binding to its receptor, PTH1R, a
G protein-coupled receptor (GPCR), activating the downstream cAMP signaling pathway. As an autocrine, paracrine, or intracrine factor,
PTHrP has been found to stimulate
cancer cell proliferation, inhibit apoptosis, and promote
tumor-induced
osteolysis of bone. Despite these findings, attempts to develop
PTHrP and PTH1R as
drug targets have not produced successful results in the clinic. Nevertheless, the efficacy of blocking
PTHrP and PTH1R has been shown in various types of
cancer, suggesting its potential for therapeutic applications. In light of these conflicting data, we conducted a comprehensive review of the studies of
PTHrP/PTH1R in
cancer progression and
metastasis and highlighted the strengths and limitations of targeting
PTHrP or PTH1R in
cancer therapy. This review also offers our perspectives for future research in this field.