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small molecule, MTBT, prevents cancer cell growth by activating p38 MAPK.

Title: A small molecule, MTBT, prevents cancer cell growth by activating p38 MAPK.
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Name(s): Li, Yan, author
Zhang, Xuelian, author
Zhang, Jing, author
Li, Yongzhen, author
Liu, Wei, author
Wang, Zhen, author
Wang, Yanchang, author
Si, Shuyi, author
Type of Resource: text
Genre: Journal Article
Text
Date Issued: 2014-04-01
Physical Form: computer
online resource
Extent: 1 online resource
Language(s): English
Abstract/Description: Cancer is a disease of unscheduled cell division and many anticancer drugs target the cell cycle to inhibit the proliferation of cancer cells. We conducted a screen for new anticancer drugs that induce cell cycle arrest using a small compound library. From this screen, we identified 2-(3-methyl-thiophen-2-yl)-4-(3,4-dioxybenzene) thiazole (MTBT), which causes accumulation of cancer cells with 4N DNA content and inhibits colony formation of several cancer cell lines. We further showed that the treatment of cancer cells with this compound for a longer time period leads to apoptosis, as indicated by the presence of cells with a sub-G1 peak and the appearance apoptotic markers. The increased phosphorylation of serine 10 on histone H3 in MTBT-treated cancer cells suggests cell cycle arrest in the M-phase. Strikingly, MTBT-induced cell cycle arrest and enhanced H3 (Ser10) phosphorylation are abrogated by the pretreatment with SB203580, a specific inhibitor of mitogen-activated protein kinase p38. Moreover, treatment of cancer cells with MTBT induces the phosphorylation of p38, indicative of p38 activation. Together, we have identified a new compound that inhibits cancer cell proliferation, which is likely a consequence of p38 activation.
Identifier: FSU_pmch_24441745 (IID), 10.1097/CAD.0000000000000074 (DOI), PMC4091034 (PMCID), 24441745 (RID), 24441745 (EID)
Grant Number: R01 GM102115, R15 GM097326, 1R01GM102115, R15GM097326-01
Publication Note: This NIH-funded author manuscript originally appeared in PubMed Central at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4091034.
Subject(s): Antineoplastic Agents/pharmacology
Apoptosis/drug effects
Benzothiazoles/pharmacology
Cell Line, Tumor
Cell Proliferation/drug effects
Enzyme Activation
Humans
M Phase Cell Cycle Checkpoints
Phosphorylation
Sulfoxides/pharmacology
p38 Mitogen-Activated Protein Kinases/metabolism
Persistent Link to This Record: http://purl.flvc.org/fsu/fd/FSU_pmch_24441745
Owner Institution: FSU
Is Part Of: Anti-cancer drugs.
1473-5741
Issue: iss. 4, vol. 25

Choose the citation style.
Li, Y., Zhang, X., Zhang, J., Li, Y., Liu, W., Wang, Z., … Si, S. (2014). A small molecule, MTBT, prevents cancer cell growth by activating p38 MAPK. Anti-Cancer Drugs. Retrieved from http://purl.flvc.org/fsu/fd/FSU_pmch_24441745