期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 19, 期 8, 页码 -出版社
MDPI
DOI: 10.3390/ijms19082237
关键词
pepducin therapy; GPCRs; invasion; breast; lung and ovarian cancer; PAR1
资金
- NHLBI [P50 HL110789, R01 HL136485, R01 HL57905]
- NCI [R01 CA104406, R01 CA122992]
- Aid for Cancer Research, Boston, MA
- Susan G. Komen, United Against Lung Cancer Legacy Program [BCTR0706763, BCTR0601348]
The G-protein coupled receptors (GPCRs) belong to a large family of diverse receptors that are well recognized as pharmacological targets. However, very few of these receptors have been pursued as oncology drug targets. The Protease-activated receptor 1 (PAR1), which is a G-protein coupled receptor, has been shown to act as an oncogene and is an emerging anti-cancer drug target. In this paper, we provide an overview of PAR1's biased signaling role in metastatic cancers of the breast, lungs, and ovaries and describe the development of PAR1 inhibitors that are currently in clinical use to treat acute coronary syndromes. PAR1 inhibitor PZ-128 is in a Phase II clinical trial and is being developed to prevent ischemic and thrombotic complication of patients undergoing cardiac catheterization. PZ-128 belongs to a new class of cell-penetrating, membrane-tethered peptides named pepducins that are based on the intracellular loops of receptors targeting the receptor G-protein interface. Application of PZ-128 as an anti-metastatic and anti-angiogenic therapeutic agent in breast, lung, and ovarian cancer is being reviewed.
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