A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab
Colorectal cancer: Potential treatment for drug-resistant cases A recently identified small molecule shows promise for tackling resistance to a leading colorectal cancer drug. Three proteins that are over-expressed in colorectal cancer are epidermal growth factor receptor (EGFR), RAS and β-catenin....
| Main Authors: | , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Nature Publishing Group
2018-11-01
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| Series: | Experimental and Molecular Medicine |
| Online Access: | https://doi.org/10.1038/s12276-018-0182-2 |
| _version_ | 1828883639980523520 |
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| author | Sang-Kyu Lee Yong-Hee Cho Pu-Hyeon Cha Jeong-Soo Yoon Eun Ji Ro Woo-Jeong Jeong Jieun Park Hyuntae Kim Tae Il Kim Do Sik Min Gyoonhee Han Kang-Yell Choi |
| author_facet | Sang-Kyu Lee Yong-Hee Cho Pu-Hyeon Cha Jeong-Soo Yoon Eun Ji Ro Woo-Jeong Jeong Jieun Park Hyuntae Kim Tae Il Kim Do Sik Min Gyoonhee Han Kang-Yell Choi |
| author_sort | Sang-Kyu Lee |
| collection | DOAJ |
| description | Colorectal cancer: Potential treatment for drug-resistant cases A recently identified small molecule shows promise for tackling resistance to a leading colorectal cancer drug. Three proteins that are over-expressed in colorectal cancer are epidermal growth factor receptor (EGFR), RAS and β-catenin. These proteins and their interconnected signaling pathways are therefore important therapeutic targets. EGFR is the target of the drug cetuximab, but many patients are resistant to this drug attributed to mutations in a gene that influences the signaling pathways of the three key proteins. Kang-Yell Choi at Yonsei University in Seoul, South Korea, and co-workers trialed a novel molecular drug on human colorectal cancer tissues and on mice. They confirmed that the new drug leads to reduced EGFR levels by degrading RAS and β-catenin and therefore suppresses the growth of colorectal cancer cells in samples with or without the resistant mutations. |
| first_indexed | 2024-12-13T10:53:09Z |
| format | Article |
| id | doaj.art-c1dade6e357447d6b4ce63e559f00cb7 |
| institution | Directory Open Access Journal |
| issn | 1226-3613 2092-6413 |
| language | English |
| last_indexed | 2024-12-13T10:53:09Z |
| publishDate | 2018-11-01 |
| publisher | Nature Publishing Group |
| record_format | Article |
| series | Experimental and Molecular Medicine |
| spelling | doaj.art-c1dade6e357447d6b4ce63e559f00cb72022-12-21T23:49:45ZengNature Publishing GroupExperimental and Molecular Medicine1226-36132092-64132018-11-01501111210.1038/s12276-018-0182-2A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximabSang-Kyu Lee0Yong-Hee Cho1Pu-Hyeon Cha2Jeong-Soo Yoon3Eun Ji Ro4Woo-Jeong Jeong5Jieun Park6Hyuntae Kim7Tae Il Kim8Do Sik Min9Gyoonhee Han10Kang-Yell Choi11Translational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityDepartment of Internal Medicine and Institute of Gastroenterology, College of Medicine, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityTranslational Research Center for Protein Function Control, Yonsei UniversityColorectal cancer: Potential treatment for drug-resistant cases A recently identified small molecule shows promise for tackling resistance to a leading colorectal cancer drug. Three proteins that are over-expressed in colorectal cancer are epidermal growth factor receptor (EGFR), RAS and β-catenin. These proteins and their interconnected signaling pathways are therefore important therapeutic targets. EGFR is the target of the drug cetuximab, but many patients are resistant to this drug attributed to mutations in a gene that influences the signaling pathways of the three key proteins. Kang-Yell Choi at Yonsei University in Seoul, South Korea, and co-workers trialed a novel molecular drug on human colorectal cancer tissues and on mice. They confirmed that the new drug leads to reduced EGFR levels by degrading RAS and β-catenin and therefore suppresses the growth of colorectal cancer cells in samples with or without the resistant mutations.https://doi.org/10.1038/s12276-018-0182-2 |
| spellingShingle | Sang-Kyu Lee Yong-Hee Cho Pu-Hyeon Cha Jeong-Soo Yoon Eun Ji Ro Woo-Jeong Jeong Jieun Park Hyuntae Kim Tae Il Kim Do Sik Min Gyoonhee Han Kang-Yell Choi A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab Experimental and Molecular Medicine |
| title | A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab |
| title_full | A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab |
| title_fullStr | A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab |
| title_full_unstemmed | A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab |
| title_short | A small molecule approach to degrade RAS with EGFR repression is a potential therapy for KRAS mutation-driven colorectal cancer resistance to cetuximab |
| title_sort | small molecule approach to degrade ras with egfr repression is a potential therapy for kras mutation driven colorectal cancer resistance to cetuximab |
| url | https://doi.org/10.1038/s12276-018-0182-2 |
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