Bioorganic Chemistry, volume 99, pages 103866
A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex
Publication type: Journal Article
Publication date: 2020-06-01
Journal:
Bioorganic Chemistry
Quartile SCImago
Q1
Quartile WOS
Q1
Impact factor: 5.1
ISSN: 00452068, 10902120
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Abstract
Aberrant expression of c-MYC oncogene is significantly associated with the occurrence and development of malignant melanoma. Suppression of the c-MYC transcriptional activity accordingly provides a new idea for treating melanoma. Notably, stabilizing the G-quadruplex (G4) structure in the promoter is proved to be effective in downregulating c-MYC transcription. In this work, we developed a drug-like imidazole-benzothiazole conjugate called IZTZ-1, which was confirmed to preferentially stabilize the promoter G4 and thus lower c-MYC expression. Intracellular assays revealed that IZTZ-1 induced cell cycle arrest, apoptosis, thereby inhibiting cell proliferation. Furthermore, IZTZ-1 was demonstrated to effectively inhibit tumor growth in a melanoma mouse model. Consequently, IZTZ-1 showed good potential in the treatment of melanoma. This study provides an alternative strategy to treat melanoma by targeting the c-MYC G4.
Top-30
Journals
|
1
2
|
|
|
Journal of Medicinal Chemistry
2 publications, 10%
|
|
|
International Journal of Biological Macromolecules
2 publications, 10%
|
|
|
International Journal of Molecular Sciences
1 publication, 5%
|
|
|
Molecular Cancer
1 publication, 5%
|
|
|
Cellular and Molecular Life Sciences
1 publication, 5%
|
|
|
Molecular Biotechnology
1 publication, 5%
|
|
|
Structural Chemistry
1 publication, 5%
|
|
|
Biomedicines
1 publication, 5%
|
|
|
Nucleic Acids Research
1 publication, 5%
|
|
|
Biochimica et Biophysica Acta - Reviews on Cancer
1 publication, 5%
|
|
|
European Journal of Medicinal Chemistry
1 publication, 5%
|
|
|
Biomedicine and Pharmacotherapy
1 publication, 5%
|
|
|
New Journal of Chemistry
1 publication, 5%
|
|
|
Archiv der Pharmazie
1 publication, 5%
|
|
|
Journal of Molecular Liquids
1 publication, 5%
|
|
|
Russian Chemical Reviews
1 publication, 5%
|
|
|
1
2
|
Publishers
|
1
2
3
4
5
6
7
|
|
|
Elsevier
7 publications, 35%
|
|
|
Springer Nature
4 publications, 20%
|
|
|
MDPI
2 publications, 10%
|
|
|
American Chemical Society (ACS)
2 publications, 10%
|
|
|
Wiley
2 publications, 10%
|
|
|
Oxford University Press
1 publication, 5%
|
|
|
Royal Society of Chemistry (RSC)
1 publication, 5%
|
|
|
Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 publication, 5%
|
|
|
1
2
3
4
5
6
7
|
- We do not take into account publications without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
Cite this
GOST |
RIS |
BibTex
Cite this
GOST
Copy
Wu T. Y. et al. A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex // Bioorganic Chemistry. 2020. Vol. 99. p. 103866.
GOST all authors (up to 50)
Copy
Wu T. Y., Huang Q., Huang Z., Hu M., Tan J. A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex // Bioorganic Chemistry. 2020. Vol. 99. p. 103866.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bioorg.2020.103866
UR - https://doi.org/10.1016/j.bioorg.2020.103866
TI - A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex
T2 - Bioorganic Chemistry
AU - Wu, Tian Ying
AU - Huang, Qiong
AU - Huang, Zhi-Shu
AU - Hu, Minghao
AU - Tan, Jia-Heng
PY - 2020
DA - 2020/06/01
PB - Elsevier
SP - 103866
VL - 99
SN - 0045-2068
SN - 1090-2120
ER -
Cite this
BibTex
Copy
@article{2020_Wu,
author = {Tian Ying Wu and Qiong Huang and Zhi-Shu Huang and Minghao Hu and Jia-Heng Tan},
title = {A drug-like imidazole-benzothiazole conjugate inhibits malignant melanoma by stabilizing the c-MYC G-quadruplex},
journal = {Bioorganic Chemistry},
year = {2020},
volume = {99},
publisher = {Elsevier},
month = {jun},
url = {https://doi.org/10.1016/j.bioorg.2020.103866},
pages = {103866},
doi = {10.1016/j.bioorg.2020.103866}
}