Cited 14 times in
Renal Cell Carcinoma Is Abrogated by p53 Stabilization through Transglutaminase 2 Inhibition
DC Field | Value | Language |
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dc.contributor.author | 라선영 | - |
dc.contributor.author | 권우선 | - |
dc.date.accessioned | 2019-02-14T01:51:07Z | - |
dc.date.available | 2019-02-14T01:51:07Z | - |
dc.date.issued | 2018 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/167253 | - |
dc.description.abstract | In general, expression of transglutaminase 2 (TGase 2) is upregulated in renal cell carcinoma (RCC), resulting in p53 instability. Previous studies show that TGase 2 binds to p53 and transports it to the autophagosome. Knockdown or inhibition of TGase 2 in RCC induces p53-mediated apoptosis. Here, we screened a chemical library for TGase 2 inhibitors and identified streptonigrin as a potential therapeutic compound for RCC. Surface plasmon resonance and mass spectroscopy were used to measure streptonigrin binding to TGase 2. Mass spectrometry analysis revealed that streptonigrin binds to the N-terminus of TGase 2 (amino acids 95⁻116), which is associated with inhibition of TGase 2 activity in vitro and with p53 stabilization in RCC. The anti-cancer effects of streptonigrin on RCC cell lines were demonstrated in cell proliferation and cell death assays. In addition, a single dose of streptonigrin (0.2 mg/kg) showed marked anti-tumor effects in a preclinical RCC model by stabilizing p53. Inhibition of TGase 2 using streptonigrin increased p53 stability, which resulted in p53-mediated apoptosis of RCC. Thus, targeting TGase 2 may be a new therapeutic approach to RCC. | - |
dc.description.statementOfResponsibility | open | - |
dc.format | application/pdf | - |
dc.language | English | - |
dc.publisher | MDPI | - |
dc.relation.isPartOf | CANCERS | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.rights | https://creativecommons.org/licenses/by-nc-nd/2.0/kr/ | - |
dc.title | Renal Cell Carcinoma Is Abrogated by p53 Stabilization through Transglutaminase 2 Inhibition | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Dept. of Internal Medicine (내과학교실) | - |
dc.contributor.googleauthor | Seon-Hyeong Lee | - |
dc.contributor.googleauthor | Won-Kyu Lee | - |
dc.contributor.googleauthor | Nayeon Kim | - |
dc.contributor.googleauthor | Joon Hee Kang | - |
dc.contributor.googleauthor | Kyung-Hee Kim | - |
dc.contributor.googleauthor | Seul-Gi Kim | - |
dc.contributor.googleauthor | Jae-Seon Lee | - |
dc.contributor.googleauthor | Soohyun Lee | - |
dc.contributor.googleauthor | Jongkook Lee | - |
dc.contributor.googleauthor | Jungnam Joo | - |
dc.contributor.googleauthor | Woo Sun Kwon | - |
dc.contributor.googleauthor | Sun Young Rha | - |
dc.contributor.googleauthor | Soo-Youl Kim | - |
dc.identifier.doi | 10.3390/cancers10110455 | - |
dc.contributor.localId | A01316 | - |
dc.relation.journalcode | J03449 | - |
dc.identifier.eissn | 2072-6694 | - |
dc.identifier.pmid | 30463244 | - |
dc.subject.keyword | apoptosis | - |
dc.subject.keyword | p53 | - |
dc.subject.keyword | renal cell carcinoma | - |
dc.subject.keyword | streptonigrin | - |
dc.subject.keyword | transglutaminase 2 | - |
dc.contributor.alternativeName | Rha, Sun Young | - |
dc.contributor.affiliatedAuthor | 라선영 | - |
dc.citation.volume | 10 | - |
dc.citation.number | 11 | - |
dc.citation.startPage | E455 | - |
dc.identifier.bibliographicCitation | CANCERS, Vol.10(11) : E455, 2018 | - |
dc.identifier.rimsid | 61458 | - |
dc.type.rims | ART | - |
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