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A Novel Dual HDAC6 and Tubulin Inhibitor, MPT0B451, Displays Anti-tumor Ability in Human Cancer Cells in Vitro and in Vivo

Overview of attention for article published in Frontiers in Pharmacology, March 2018
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Title
A Novel Dual HDAC6 and Tubulin Inhibitor, MPT0B451, Displays Anti-tumor Ability in Human Cancer Cells in Vitro and in Vivo
Published in
Frontiers in Pharmacology, March 2018
DOI 10.3389/fphar.2018.00205
Pubmed ID
Authors

Yi-Wen Wu, Kai-Cheng Hsu, Hsueh-Yun Lee, Tsui-Chin Huang, Tony E. Lin, Yi-Ling Chen, Ting-Yi Sung, Jing-Ping Liou, Wendy W. Hwang-Verslues, Shiow-Lin Pan, Wei-Chun HuangFu

Abstract

The combination cancer therapy is a new strategy to circumvent drug resistance for the treatment of high metastasis and advanced malignancies. Herein, we developed a synthesized compound MPT0B451 that display inhibitory effect against histone deacetylase (HDAC) 6 and tubulin assembly. Our data demonstrated that MPT0B451 significantly inhibited cancer cell growths in HL-60 and PC-3 cells due to inhibition of HDAC activity. MPT0B451 also markedly increased caspase-mediated apoptosis in these cells. The cell cycle analysis showed mitotic arrest induced by MPT0B451 with enhanced expression of G2/M transition proteins. Moreover, molecular docking analysis supported MPT0B451 as a dual HDAC6 and tubulin inhibitor. Finally, MPT0B451 led to tumor growth inhibition (TGI) in HL-60 and PC-3 xenograft models. These findings indicated that MPT0B451 has dual inhibition effects for HDAC6 and tubulin, and also contributed to G2/M arrest followed by apoptotic induction. Together, our results suggested that MPT0B451 may serve as a potent anti-cancer treatment regimen in human prostate cancer and acute myeloid leukemia.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 31 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 31 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 5 16%
Student > Bachelor 4 13%
Student > Master 4 13%
Researcher 2 6%
Student > Doctoral Student 2 6%
Other 3 10%
Unknown 11 35%
Readers by discipline Count As %
Chemistry 8 26%
Pharmacology, Toxicology and Pharmaceutical Science 4 13%
Biochemistry, Genetics and Molecular Biology 3 10%
Agricultural and Biological Sciences 1 3%
Nursing and Health Professions 1 3%
Other 2 6%
Unknown 12 39%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 15 March 2018.
All research outputs
#20,468,008
of 23,026,672 outputs
Outputs from Frontiers in Pharmacology
#10,242
of 16,337 outputs
Outputs of similar age
#294,725
of 333,594 outputs
Outputs of similar age from Frontiers in Pharmacology
#239
of 378 outputs
Altmetric has tracked 23,026,672 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 16,337 research outputs from this source. They receive a mean Attention Score of 5.0. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 378 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.