1 Ocak 2019 Dergi makalesi Açık Erişim

Delman, Murat; Avci, Sanem Tercan; Akcok, Ismail; Kanbur, Tugce; Erdal, Esra; Cagir, Ali

JSON

{
  "conceptrecid": "74490", 
  "created": "2021-03-16T04:12:17.793251+00:00", 
  "doi": "10.1016/j.ejmech.2019.07.024", 
  "files": [
    {
      "bucket": "0f9feda7-53c9-431d-89ff-2ad4bfe60d7a", 
      "checksum": "md5:0fa9dd244238d11311755f0f8b415e96", 
      "key": "bib-3124df6e-7e44-4757-add0-b54abca9297d.txt", 
      "links": {
        "self": "https://aperta.ulakbim.gov.tr/api/files/0f9feda7-53c9-431d-89ff-2ad4bfe60d7a/bib-3124df6e-7e44-4757-add0-b54abca9297d.txt"
      }, 
      "size": 306, 
      "type": "txt"
    }
  ], 
  "id": 74491, 
  "links": {
    "badge": "https://aperta.ulakbim.gov.tr/badge/doi/10.1016/j.ejmech.2019.07.024.svg", 
    "bucket": "https://aperta.ulakbim.gov.tr/api/files/0f9feda7-53c9-431d-89ff-2ad4bfe60d7a", 
    "doi": "https://doi.org/10.1016/j.ejmech.2019.07.024", 
    "html": "https://aperta.ulakbim.gov.tr/record/74491", 
    "latest": "https://aperta.ulakbim.gov.tr/api/records/74491", 
    "latest_html": "https://aperta.ulakbim.gov.tr/record/74491"
  }, 
  "metadata": {
    "access_right": "open", 
    "access_right_category": "success", 
    "communities": [
      {
        "id": "tubitak-destekli-proje-yayinlari"
      }
    ], 
    "creators": [
      {
        "affiliation": "Izmir Inst Technol, Dept Biotechnol & Bioengn, TR-35430 Izmir, Turkey", 
        "name": "Delman, Murat"
      }, 
      {
        "name": "Avci, Sanem Tercan"
      }, 
      {
        "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
        "name": "Akcok, Ismail"
      }, 
      {
        "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
        "name": "Kanbur, Tugce"
      }, 
      {
        "name": "Erdal, Esra"
      }, 
      {
        "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
        "name": "Cagir, Ali"
      }
    ], 
    "description": "Cytotoxic effects of (R)-4'-methylklavuzon were investigated on hepatocellular carcinoma cells (HuH-7 and HepG2) and HuH-7 EpCAM(+)/CD133(+) cancer stem cells. IC50 of (R)-4'-methylklavuzon was found as 1.25 mu M for HuH-7 parental cells while it was found as 2.50 mu M for HuH-7 EpCAM(+)/CD133(+) cancer stem cells. (R)-4'-methylklavuzon tended to show more efficient in vitro cytotoxicity with its lower IC50 values on hepatocellular carcinoma cell lines compared to its lead molecule, goniothalamin and FDA-approved drugs, sorafenib and regorafenib. Cell-based Sirtuin/HDAC enzyme activity measurements revealed that endogenous Sirtuin/HDAC enzymes were reduced by 40% compared to control. SIRT1 protein levels were upregulated indicating triggered DNA repair mechanism. p53 was overexpressed in HepG2 cells. (R)-4'methylklavuzon inhibited CRM1 protein providing increased retention of p53 and RIOK2 protein in the nucleus. HuH-7 parental and EpCAM(+)/CD133(+) cancer stem cell spheroids lost intact morphology. 3D HepG2 spheroid viabilities were decreased in a correlation with upregulation in p53 protein levels. (C) 2019 Elsevier Masson SAS. All rights reserved.", 
    "doi": "10.1016/j.ejmech.2019.07.024", 
    "has_grant": false, 
    "journal": {
      "pages": "224-237", 
      "title": "EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY", 
      "volume": "180"
    }, 
    "license": {
      "id": "cc-by"
    }, 
    "publication_date": "2019-01-01", 
    "relations": {
      "version": [
        {
          "count": 1, 
          "index": 0, 
          "is_last": true, 
          "last_child": {
            "pid_type": "recid", 
            "pid_value": "74491"
          }, 
          "parent": {
            "pid_type": "recid", 
            "pid_value": "74490"
          }
        }
      ]
    }, 
    "resource_type": {
      "subtype": "article", 
      "title": "Dergi makalesi", 
      "type": "publication"
    }, 
    "title": "Antiproliferative activity of (R)-4 '-methylklavuzon on hepatocellular carcinoma cells and EpCAM(+)/CD133(+) cancer stem cells via SIRT1 and Exportin-1 (CRM1) inhibition"
  }, 
  "owners": [
    1
  ], 
  "revision": 1, 
  "stats": {
    "downloads": 8.0, 
    "unique_downloads": 8.0, 
    "unique_views": 35.0, 
    "version_downloads": 8.0, 
    "version_unique_downloads": 8.0, 
    "version_unique_views": 35.0, 
    "version_views": 39.0, 
    "version_volume": 2448.0, 
    "views": 39.0, 
    "volume": 2448.0
  }, 
  "updated": "2021-03-16T04:12:17.848453+00:00"
}