Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 권영주 | * |
dc.contributor.author | 전경화 | * |
dc.contributor.author | 황수연 | * |
dc.date.accessioned | 2021-11-10T16:31:25Z | - |
dc.date.available | 2021-11-10T16:31:25Z | - |
dc.date.issued | 2021 | * |
dc.identifier.issn | 1422-0067 | * |
dc.identifier.other | OAK-30408 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/259419 | - |
dc.description.abstract | Castration-resistant prostate cancer (CRPC) is a clinical challenge in treatment because of its aggressive nature and resistance to androgen deprivation therapy. Topoisomerase II catalytic inhibitors have been suggested as a strategy to overcome these issues. We previously reported AK-I-190 as a novel topoisomerase II inhibitor. In this study, the mechanism of AK-I-190 was clarified using various types of spectroscopic and biological evaluations. AK-I-190 showed potent topoisomerase II inhibitory activity through intercalating into DNA without stabilizing the DNA-enzyme cleavage complex, resulting in significantly less DNA toxicity than etoposide, a clinically used topoisomerase II poison. AK-I-190 induced G1 arrest and effectively inhibited cell proliferation and colony formation in combination with paclitaxel in an androgen receptor-negative CRPC cell line. Our results confirmed that topoisomerase II catalytic inhibition inhibited proliferation and induced apoptosis of AR-independently growing prostate cancer cells. These findings indicate the clinical relevance of topoisomerase II catalytic inhibitors in androgen receptor-negative prostate cancer. | * |
dc.language | English | * |
dc.publisher | MDPI | * |
dc.subject | topoisomerase II inhibitor | * |
dc.subject | CRPC | * |
dc.subject | DNA intercalator | * |
dc.title | AK-I-190, a New Catalytic Inhibitor of Topoisomerase II with Anti-Proliferative and Pro-Apoptotic Activity on Androgen-Negative Prostate Cancer Cells | * |
dc.type | Article | * |
dc.relation.issue | 20 | * |
dc.relation.volume | 22 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.journaltitle | INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | * |
dc.identifier.doi | 10.3390/ijms222011246 | * |
dc.identifier.wosid | WOS:000747818300001 | * |
dc.identifier.scopusid | 2-s2.0-85117159249 | * |
dc.author.google | Jeon, Kyung-Hwa | * |
dc.author.google | Park, Seojeong | * |
dc.author.google | Jang, Hae Jin | * |
dc.author.google | Hwang, Soo-Yeon | * |
dc.author.google | Shrestha, Aarajana | * |
dc.author.google | Lee, Eung-Seok | * |
dc.author.google | Kwon, Youngjoo | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.contributor.scopusid | 전경화(42061515400) | * |
dc.contributor.scopusid | 황수연(57207836844) | * |
dc.date.modifydate | 20240422124907 | * |