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G Protein-coupled Receptors: Novel Targets for Drug Discovery in Cancer

Overview
Specialty Pharmacology
Date 2011 Jan 4
PMID 21193867
Citations 340
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Abstract

G protein-coupled receptors (GPCRs) belong to a superfamily of cell surface signalling proteins that have a pivotal role in many physiological functions and in multiple diseases, including the development of cancer and cancer metastasis. Current drugs that target GPCRs - many of which have excellent therapeutic benefits - are directed towards only a few GPCR members. Therefore, huge efforts are currently underway to develop new GPCR-based drugs, particularly for cancer. We review recent findings that present unexpected opportunities to interfere with major tumorigenic signals by manipulating GPCR-mediated pathways. We also discuss current data regarding novel GPCR targets that may provide promising opportunities for drug discovery in cancer prevention and treatment.

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References
1.
Vazquez-Martin A, Oliveras-Ferraros C, Cufi S, Del Barco S, Martin-Castillo B, Menendez J . Metformin regulates breast cancer stem cell ontogeny by transcriptional regulation of the epithelial-mesenchymal transition (EMT) status. Cell Cycle. 2010; 9(18):3807-14. View

2.
Epstein R . The CXCL12-CXCR4 chemotactic pathway as a target of adjuvant breast cancer therapies. Nat Rev Cancer. 2004; 4(11):901-9. DOI: 10.1038/nrc1473. View

3.
Rosano L, Spinella F, Bagnato A . The importance of endothelin axis in initiation, progression, and therapy of ovarian cancer. Am J Physiol Regul Integr Comp Physiol. 2010; 299(2):R395-404. DOI: 10.1152/ajpregu.00304.2010. View

4.
Sun J, Lin X . Beta-arrestin 2 is required for lysophosphatidic acid-induced NF-kappaB activation. Proc Natl Acad Sci U S A. 2008; 105(44):17085-90. PMC: 2579382. DOI: 10.1073/pnas.0802701105. View

5.
Fischgrabe J, Gotte M, Michels K, Kiesel L, Wulfing P . Targeting endothelin A receptor enhances anti-proliferative and anti-invasive effects of the HER2 antibody trastuzumab in HER2-overexpressing breast cancer cells. Int J Cancer. 2009; 127(3):696-706. DOI: 10.1002/ijc.25076. View