{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,24]],"date-time":"2026-10-24T15:18:09Z","timestamp":1792855089556,"version":"4.5.0"},"reference-count":146,"publisher":"MDPI AG","issue":"6","license":[{"start":{"date-parts":[[2022,6,8]],"date-time":"2022-06-08T00:00:00Z","timestamp":1654646400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Institut National de la Sant\u00e9 et de la Recherche Medicale (Inserm)"},{"name":"TTO Ouest Valorisation (Oracle and Oracle2 projects)"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Biomedicines"],"abstract":"<jats:p>Bladder pathologies, very common in the aged population, have a considerable negative impact on quality of life. Novel targets are needed to design drugs and combinations to treat diseases such as overactive bladder and bladder cancers. A promising new target is the ubiquitous Rho GTPase Rac1, frequently dysregulated and overexpressed in bladder pathologies. We have analyzed the roles of Rac1 in different bladder pathologies, including bacterial infections, diabetes-induced bladder dysfunctions and bladder cancers. The contribution of the Rac1 protein to tumorigenesis, tumor progression, epithelial-mesenchymal transition of bladder cancer cells and their metastasis has been analyzed. Small molecules selectively targeting Rac1 have been discovered or designed, and two of them\u2014NSC23766 and EHT 1864\u2014have revealed activities against bladder cancer. Their mode of interaction with Rac1, at the GTP binding site or the guanine nucleotide exchange factors (GEF) interaction site, is discussed. Our analysis underlines the possibility of targeting Rac1 with small molecules with the objective to combat bladder dysfunctions and to reduce lower urinary tract symptoms. Finally, the interest of a Rac1 inhibitor to treat advanced chemoresistance prostate cancer, while reducing the risk of associated bladder dysfunction, is discussed. There is hope for a better management of bladder pathologies via Rac1-targeted approaches.<\/jats:p>","DOI":"10.3390\/biomedicines10061357","type":"journal-article","created":{"date-parts":[[2022,6,9]],"date-time":"2022-06-09T10:49:14Z","timestamp":1654771754000},"page":"1357","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Rac1 as a Target to Treat Dysfunctions and Cancer of the Bladder"],"prefix":"10.3390","volume":"10","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6187-0312","authenticated-orcid":false,"given":"Vincent","family":"Sauzeau","sequence":"first","affiliation":[{"name":"Universit\u00e9 de Nantes, CHU Nantes, CNRS, INSERM, Institut du Thorax, 44202 Nantes, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9740-6546","authenticated-orcid":false,"given":"Julien","family":"Beignet","sequence":"additional","affiliation":[{"name":"SATT Ouest Valorisation, 30 Boulevard Vincent G\u00e2che, CS 70211, CEDEX, 44202 Nantes, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2973-9357","authenticated-orcid":false,"given":"Christian","family":"Bailly","sequence":"additional","affiliation":[{"name":"OncoWitan, Scientific Consulting Office, 59290 Lille (Wasquehal), France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,6,8]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"1081","DOI":"10.1016\/j.urology.2010.08.039","article-title":"National community prevalence of overactive bladder in the United States stratified by sex and age","volume":"77","author":"Coyne","year":"2011","journal-title":"Urology"},{"key":"ref_2","first-page":"130","article-title":"Economic burden of urgency urinary incontinence in the United States: A systematic review","volume":"20","author":"Coyne","year":"2014","journal-title":"J. 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