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Ref Type Journal Article
PMID (27216191)
Authors Prunier C, Josserand V, Vollaire J, Beerling E, Petropoulos C, Destaing O, Montemagno C, Hurbin A, Prudent R, de Koning L, Kapur R, Cohen PA, Albiges-Rizo C, Coll JL, van Rheenen J, Billaud M, Lafanechère L
Title LIM Kinase Inhibitor Pyr1 Reduces the Growth and Metastatic Load of Breast Cancers.
Journal Cancer research
Vol 76
Issue 12
Date 2016 Jun 15
URL
Abstract Text LIM kinases (LIMK) are emerging targets for cancer therapy, and they function as network hubs to coordinate actin and microtubule dynamics. When LIMKs are inhibited, actin microfilaments are disorganized and microtubules are stabilized. Owing to their stabilizing effect on microtubules, LIMK inhibitors may provide a therapeutic strategy to treat taxane-resistant cancers. In this study, we investigated the effect of LIMK inhibition on breast tumor development and on paclitaxel-resistant tumors, using a novel selective LIMK inhibitor termed Pyr1. Treatment of breast cancer cells, including paclitaxel-resistant cells, blocked their invasion and proliferation in vitro and their growth in vivo in tumor xenograft assays. The tumor-invasive properties of Pyr1 were investigated in vivo by intravital microscopy of tumor xenografts. A striking change of cell morphology was observed with a rounded phenotype arising in a subpopulation of cells, while other cells remained elongated. Notably, although Pyr1 decreased the motility of elongated cells, it increased the motility of rounded cells in the tumor. Pyr1 administration prevented the growth of metastasis but not their spread. Overall, our results provided a preclinical proof of concept concerning how a small-molecule inhibitor of LIMK may offer a strategy to treat taxane-resistant breast tumors and metastases. Cancer Res; 76(12); 3541-52. ©2016 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Pyr1 Pyr1 1 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
Pyr1 Pyr1 inhibits LIM kinase (LIMK), potentially resulting in decreased tumor cell proliferation and tumor growth (PMID: 27216191).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown breast cancer not applicable Pyr1 Preclinical - Cell line xenograft Actionable In a preclinical study, Pyr1 inhibited proliferation and migration of breast cancer cell lines in culture, and inhibited growth of primary tumors and metastases in breast cancer cell line xenograft models (PMID: 27216191). 27216191