PMID- 32878796
OWN - NLM
STAT- MEDLINE
DCOM- 20200918
LR  - 20200918
IS  - 1791-7530 (Electronic)
IS  - 0250-7005 (Linking)
VI  - 40
IP  - 9
DP  - 2020 Sep
TI  - Novel Imidazo[2,1-b]oxazole Derivatives Inhibit Epithelial Cell Transformation 
      and Triple Negative Breast Cancer Tumorigenesis.
PG  - 5081-5090
LID - 10.21873/anticanres.14511 [doi]
AB  - BACKGROUND/AIM: Triple negative breast cancer (TNBC) is an aggressive type of 
      breast cancer with limited targets for chemotherapy. This study evaluated the 
      inhibitory effects of novel imidazo[2,1-b]oxazole-based rapidly accelerated 
      fibrosarcoma (RAF) inhibitors, KIST0215-1 and KIST0215-2, on epithelial cell 
      transformation and TNBC tumorigenesis. MATERIALS AND METHODS: Immunoblotting, 
      BrdU incorporation assay, reporter gene assay, and soft agar assay analyses were 
      performed. In vivo effects were studied using the BALB/c mouse xenograft model. 
      RESULTS: KIST0215-1 and KIST0215-2 inhibited the RAFs-MEK1/2-ERK1/2 signalling 
      pathway induced by EGF in MDA-MB-231 cells, which inhibited c-fos transcriptional 
      activity and activator protein-1 transactivation activity. KIST0215-1 and 
      KIST0215-2 also prevented neoplastic transformation of JB6 C141 mouse epidermal 
      cells induced by EGF and consistently suppressed the growth of tumours formed by 
      4T1 cells in BALB/c mice. CONCLUSION: Inhibition of RAF kinases using KIST0215-1 
      and KIST0215-2 is a promising chemotherapeutic strategy to treat TNBC.
CI  - Copyright(c) 2020, International Institute of Anticancer Research (Dr. George J. 
      Delinasios), All rights reserved.
FAU - Bhattarai, Poshan Yugal
AU  - Bhattarai PY
AD  - College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
FAU - Oh, Chang-Hyun
AU  - Oh CH
AD  - Department Centre for Biomaterials, Korea Institute of Science and Technology, 
      Seoul, Republic of Korea.
FAU - Kim, Garam
AU  - Kim G
AD  - College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
FAU - Kim, Min Soo
AU  - Kim MS
AD  - College of Pharmacy, Chosun University, Gwangju, Republic of Korea.
FAU - Lee, Bong Sang
AU  - Lee BS
AD  - CTCScience Inc., Hwaseong, Republic of Korea.
FAU - Choi, Hong Seok
AU  - Choi HS
AD  - College of Pharmacy, Chosun University, Gwangju, Republic of Korea 
      chs@chosun.ac.kr.
LA  - eng
PT  - Journal Article
PL  - Greece
TA  - Anticancer Res
JT  - Anticancer research
JID - 8102988
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Imidazoles)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*pharmacology
MH  - Apoptosis/drug effects
MH  - Cell Line, Tumor
MH  - Cell Proliferation/drug effects
MH  - Cell Transformation, Neoplastic/*drug effects/genetics/metabolism
MH  - Disease Models, Animal
MH  - Epithelial-Mesenchymal Transition/*drug effects/genetics
MH  - Female
MH  - Genes, Reporter
MH  - Humans
MH  - Imidazoles/chemistry/*pharmacology
MH  - Mice
MH  - Molecular Structure
MH  - Signal Transduction/drug effects
MH  - Triple Negative Breast Neoplasms/*etiology/*metabolism/pathology
MH  - Xenograft Model Antitumor Assays
OTO - NOTNLM
OT  - Imidazo[2,1-b]oxazole derivatives
OT  - RAF inhibitors
OT  - TNBC
OT  - chemotherapy
EDAT- 2020/09/04 06:00
MHDA- 2020/09/20 06:00
CRDT- 2020/09/04 06:00
PHST- 2020/05/15 00:00 [received]
PHST- 2020/06/25 00:00 [revised]
PHST- 2020/06/30 00:00 [accepted]
PHST- 2020/09/04 06:00 [entrez]
PHST- 2020/09/04 06:00 [pubmed]
PHST- 2020/09/20 06:00 [medline]
AID - 40/9/5081 [pii]
AID - 10.21873/anticanres.14511 [doi]
PST - ppublish
SO  - Anticancer Res. 2020 Sep;40(9):5081-5090. doi: 10.21873/anticanres.14511.