The Rexinoid V-125 Reduces Tumor Growth in Preclinical Models of Breast and Lung Cancer
| Autor: | Sarah Carapellucci, Karen T. Liby, Carl E. Wagner, Peter W. Jurutka, Jessica A. Moerland, Pamela A. Marshall, Lyndsey A. Reich, Ana S. Leal, Di Zhang, Beth Lockwood |
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| Rok vydání: | 2021 |
| Předmět: |
Lung Neoplasms
Time Factors Science Antineoplastic Agents Breast Neoplasms Mice Transgenic Article medicine Animals Tumor growth Lung cancer Cell Proliferation Cancer Multidisciplinary Drug discovery business.industry medicine.disease Tumor Burden Gene Expression Regulation Neoplastic Retinoid X Receptors Cancer research Medicine Female business Signal Transduction |
| Zdroj: | Scientific Reports, Vol 12, Iss 1, Pp 1-12 (2022) Scientific Reports |
| DOI: | 10.21203/rs.3.rs-826798/v1 |
| Popis: | Rexinoids are ligands which activate retinoid X receptors (RXRs), regulating transcription of genes involved in cancer-relevant processes. Rexinoids have anti-neoplastic activity in multiple preclinical studies. Bexarotene, used to treat cutaneous T cell lymphoma, is the only FDA-approved rexinoid. Bexarotene has also been evaluated in clinical trials for lung and metastatic breast cancer, wherein subsets of patients responded despite advanced disease. By modifying structures of known rexinoids, we can improve potency and toxicity. We previously screened a series of novel rexinoids and selected V-125 as the lead based on performance in optimized in vitro assays. To validate our screening paradigm, we tested V-125 in clinically relevant mouse models of breast and lung cancer. V-125 significantly (p |
| Databáze: | OpenAIRE |
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