Literature DB >> 21193867

G protein-coupled receptors: novel targets for drug discovery in cancer.

Rosamaria Lappano1, Marcello Maggiolini.   

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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Year:  2011        PMID: 21193867     DOI: 10.1038/nrd3320

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN: 1474-1776            Impact factor:   84.694


  218 in total

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Review 2.  From purified GPCRs to drug discovery: the promise of protein-based methodologies.

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Review 4.  New mechanisms in heptahelical receptor signaling to mitogen activated protein kinase cascades.

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Review 5.  Gastrin-releasing peptide links stressor to cancer progression.

Authors:  Xinqiu Li; Yunfu Lv; Aihua Yuan; Zongfang Li
Journal:  J Cancer Res Clin Oncol       Date:  2010-02-06       Impact factor: 4.553

6.  Anticancer activity of BIM-46174, a new inhibitor of the heterotrimeric Galpha/Gbetagamma protein complex.

Authors:  Grégoire P Prévost; Marie O Lonchampt; Susan Holbeck; Samir Attoub; Daniel Zaharevitz; Mike Alley; John Wright; Marie C Brezak; Hélène Coulomb; Ann Savola; Marion Huchet; Sophie Chaumeron; Quang-Dé Nguyen; Patricia Forgez; Erik Bruyneel; Mark Bracke; Eric Ferrandis; Pierre Roubert; Danièle Demarquay; Christian Gespach; Philip G Kasprzyk
Journal:  Cancer Res       Date:  2006-09-15       Impact factor: 12.701

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8.  Stromal gene expression predicts clinical outcome in breast cancer.

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Journal:  Cancer Res       Date:  2009-06-09       Impact factor: 12.701

Review 10.  Role of thrombin in angiogenesis and tumor progression.

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  291 in total

Review 1.  G protein-coupled receptors as therapeutic targets for multiple sclerosis.

Authors:  Changsheng Du; Xin Xie
Journal:  Cell Res       Date:  2012-06-05       Impact factor: 25.617

2.  Activation of the P2Y1 receptor induces apoptosis and inhibits proliferation of prostate cancer cells.

Authors:  Qiang Wei; Stefano Costanzi; Qiu-Zhen Liu; Zhan-Guo Gao; Kenneth A Jacobson
Journal:  Biochem Pharmacol       Date:  2011-05-23       Impact factor: 5.858

3.  Signaling pathways: Purinosomes under GPCR control.

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Journal:  Nat Chem Biol       Date:  2011-11-15       Impact factor: 15.040

Review 4.  Orphan G protein-coupled receptors (GPCRs): biological functions and potential drug targets.

Authors:  Xiao-long Tang; Ying Wang; Da-li Li; Jian Luo; Ming-yao Liu
Journal:  Acta Pharmacol Sin       Date:  2012-02-27       Impact factor: 6.150

5.  Imaging of Tissue-Specific and Temporal Activation of GPCR Signaling Using DREADD Knock-In Mice.

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Journal:  Methods Mol Biol       Date:  2019

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Journal:  Acta Biomater       Date:  2020-06-06       Impact factor: 8.947

7.  Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors.

Authors:  Xun Shang; Fillipo Marchioni; Chris R Evelyn; Nisha Sipes; Xuan Zhou; William Seibel; Matthew Wortman; Yi Zheng
Journal:  Proc Natl Acad Sci U S A       Date:  2013-02-04       Impact factor: 11.205

8.  A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators.

Authors:  Sandra Claes; Thomas D'huys; Anneleen Van Hout; Dominique Schols; Tom Van Loy
Journal:  J Vis Exp       Date:  2018-02-20       Impact factor: 1.355

9.  Lgr5 over-expression is positively related to the tumor progression and HER2 expression in stage pTNM IV colorectal cancer.

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Journal:  Int J Clin Exp Pathol       Date:  2014-03-15

10.  Genome-scale transcriptional activation by an engineered CRISPR-Cas9 complex.

Authors:  Silvana Konermann; Mark D Brigham; Alexandro E Trevino; Julia Joung; Omar O Abudayyeh; Clea Barcena; Patrick D Hsu; Naomi Habib; Jonathan S Gootenberg; Hiroshi Nishimasu; Osamu Nureki; Feng Zhang
Journal:  Nature       Date:  2014-12-10       Impact factor: 49.962

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