skip to main content
訪客
個人書架
我的帳戶
登出
登入
This feature requires javascript
檢索首頁
圖書館首頁
電子期刊
引用參考文獻查詢
指定參考書查詢
新書通報
標籤查詢
線上輔助
語言:
English
繁體中文
This feature required javascript
This feature requires javascript
Primo Search
館藏+文章
館藏+文章
館藏
查館藏
文章
查文章
機構典藏
機構典藏
Search For:
Clear Search Box
Search in:
館藏+文章
Or hit Enter to replace search target
Or select another collection:
Search in:
館藏+文章
進階檢索
瀏覽查詢
This feature requires javascript
資源種類
criteria input
圖書
期刊
視聽資料
全部館藏
顯示結果:
criteria input
包含在我的檢索語句內
完全相同
起始以
顯示結果:
查詢種類 索引
criteria input
任何地方
題名
ISBN
ISSN
Show Results with:
題名
Show Results with:
任何地方
題名
ISBN
ISSN
This feature requires javascript
1, 9-Pyrazoloanthrones downregulate HIF-1α and sensitize cancer cells to cetuximab-mediated anti-EGFR therapy
Lu, Yang ; Li, Xinqun ; Lu, Haiquan ; Fan, Zhen Gullberg, Donald
PloS one, 2010-12, Vol.5 (12), p.e15823-e15823
[同儕審閱期刊]
可取得全文
引用
被引用
線上檢視
詳細格式
評論和標籤
相關文章推薦
FullText@NUTN
引用次數
This feature requires javascript
傳送到
加入個人書架
從個人書架中移除
E-mail
列印
永久連結
引用
EndNote
導出 RiS
This feature requires javascript
題名:
1, 9-Pyrazoloanthrones downregulate HIF-1α and sensitize cancer cells to cetuximab-mediated anti-EGFR therapy
著者:
Lu, Yang
;
Li, Xinqun
;
Lu, Haiquan
;
Fan, Zhen
Gullberg, Donald
主題:
AKT protein
;
Androgens
;
Angiogenesis
;
Anthracenes - chemistry
;
Anthracenes - pharmacology
;
Antibodies, Monoclonal - pharmacology
;
Antibodies, Monoclonal, Humanized
;
Antineoplastic Agents - pharmacology
;
Apoptosis
;
Biology
;
Breast cancer
;
c-Jun protein
;
Cancer
;
Cancer therapies
;
Cell Line, Tumor
;
Cetuximab
;
Clinical outcomes
;
Colorectal cancer
;
Degradation
;
Down-Regulation
;
Epidermal growth factor
;
Epidermal growth factor receptors
;
Extracellular signal-regulated kinase
;
Gene expression
;
Gene Expression Regulation, Neoplastic
;
Head & neck cancer
;
Humans
;
Hypoxia
;
Hypoxia-inducible factor 1
;
Hypoxia-Inducible Factor 1 - metabolism
;
Hypoxia-inducible factor 1a
;
Hypoxia-inducible factors
;
Immunoglobulins
;
Immunotherapy
;
Inhibition
;
Kinases
;
MAP Kinase Kinase 4 - metabolism
;
Medicine
;
Metastasis
;
Monoclonal antibodies
;
Mutation
;
Oxygen
;
Patients
;
Phosphorylation
;
Prolyl hydroxylase
;
Prostate cancer
;
Proteasomes
;
Protein biosynthesis
;
Protein synthesis
;
Proteins
;
Pyrazoles - chemistry
;
Pyrazoles - pharmacology
;
Receptor, Epidermal Growth Factor - antagonists & inhibitors
;
Signaling
;
Solid tumors
;
Synergistic effect
;
Targeted cancer therapy
;
TOR protein
;
Transcription factors
;
Tumors
;
Ubiquitin - chemistry
;
Vascular Endothelial Growth Factor A - metabolism
所屬期刊:
PloS one, 2010-12, Vol.5 (12), p.e15823-e15823
描述:
Cetuximab, a monoclonal antibody that blocks the epidermal growth factor receptor (EGFR), is currently approved for the treatment of several types of solid tumors. We previously showed that cetuximab can inhibit hypoxia-inducible factor-1 alpha (HIF-1α) protein synthesis by inhibiting the activation of EGFR downstream signaling pathways including Erk, Akt, and mTOR. 1, 9-pyrazoloanthrone (1, 9 PA) is an anthrapyrazolone compound best known as SP600125 that specifically inhibits c-jun N-terminal kinase (JNK). Here, we report 1, 9 PA can downregulate HIF-1α independently of its inhibition of JNK. This downregulatory effect was abolished when the oxygen-dependent domain (ODD) of HIF-1α (HIF-1α-ΔODD, the domain responsible for HIF-1α degradation) was experimentally deleted or when the activity of HIF-1α prolyl hydroxylase (PHD) or the 26S proteasomal complex was inhibited, indicating that the 1, 9 PA downregulates HIF-1α by promoting PHD-dependent HIF-1α degradation. We found that the combination of 1, 9 PA and cetuximab worked synergistically to induce apoptosis in cancer cells in which cetuximab or 1, 9 PA alone had no or only weak apoptotic activity. This synergistic effect was substantially decreased in cancer cells transfected with HIF-1α-ΔODD, indicating that downregulation of HIF-1α was the mechanism of this synergistic effect. More importantly, 1, 9 PA can downregulate HIF-1α in cancer cells that are insensitive to cetuximab-induced inhibition of HIF-1α expression due to overexpression of oncogenic Ras (RasG12V). Our findings suggest that 1, 9 PA is a lead compound of a novel class of drugs that may be used to enhance the response of cancer cells to cetuximab through a complementary effect on the downregulation of HIF-1α.
出版者:
United States: Public Library of Science
語言:
英文
識別號:
ISSN: 1932-6203
EISSN: 1932-6203
DOI: 10.1371/journal.pone.0015823
PMID: 21209911
資源來源:
Publicly Available Content Database
EBSCOhost Academic Search Premier
Agricultural & Environmental Science Collection
DOAJ Directory of Open Access Journals
連結
View this record in MEDLINE/PubMed
This feature requires javascript
This feature requires javascript
返回到檢索清單
This feature requires javascript
This feature requires javascript
正在檢索遠程資料庫,請稍等
查詢:
在
scope:("NUTN"),scope:(NUTN_ALEPH),scope:(NUTN_IR),scope:(NUTN_SFX),primo_central_multiple_fe
顯示現有記錄
This feature requires javascript
This feature requires javascript