Identification of Ras-degrading small molecules that inhibit the transformation of colorectal cancer cells independent of β-catenin signaling
| Autor: | Wookjin Shin, Sang-Kyu Lee, Jeong-Ha Hwang, Jong-Chan Park, Yong-Hee Cho, Eun Ji Ro, Yeonhwa Song, Haeng Ran Seo, Kang-Yell Choi |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: | |
| Zdroj: | Experimental and Molecular Medicine, Vol 50, Iss 6, Pp 1-10 (2018) |
| Druh dokumentu: | article |
| ISSN: | 1226-3613 2092-6413 |
| DOI: | 10.1038/s12276-018-0102-5 |
| Popis: | Colorectal cancer: Finding new small molecule drug candidates Mutations in KRAS, a gene regulating cell proliferation, occur in 40–50% of colorectal cancer (CRC) patients. These cancers are usually insensitive to antibody drugs targeting the epidermal growth factor receptor (EGFR) on cancer cells. Kang-Yell Choi at Yonsei University, Seoul, South Korea and co-workers had previously identified small molecules that inhibited CRC by degrading the signaling proteins β-catenin and Ras. However, CRC cells with β-catenin mutations are resistant to Ras-degrading compounds. In this study, they screened 10,000 small molecules that could degrade Ras in CRC cells expressing nondegradable mutant β-catenin. They identified small molecules that inhibited growth of CRC cells resistant to EGFR-mediated antibody therapy. Further investigation of these molecules may help develop new drugs for treating CRC. |
| Databáze: | Directory of Open Access Journals |
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