1
40
2
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1021/jm4004736" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/jm4004736</a>
Rights
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
Pages
5306-5320
Issue
13
Volume
56
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Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
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Synthesis and Anticancer Mechanism Investigation of Dual Hsp27 and Tubulin Inhibitors
Publisher
An entity responsible for making the resource available
Journal of Medicinal Chemistry
Date
A point or period of time associated with an event in the lifecycle of the resource
2013
2013-07
Subject
The topic of the resource
breast-cancer; c-dependent activation; cancer cells; chaperone activity; cytochrome-c; heat-shock proteins; in-vitro; nimesulide analog jcc76; pancreatic-cancer; Pharmacology & Pharmacy; self-association
Creator
An entity primarily responsible for making the resource
Zhong B; Chennamaneni S; Lama R; Yi X; Geldenhuys W J; Pink J J; Dowlati A; Xu Y; Zhou A M; Su B
Description
An account of the resource
Heat shock protein 27 (Hsp27) is a chaperone protein, and its expression is increased in response to various stress stimuli including anticancer chemotherapy, which allows the cells to survive and causes drug resistance. We previously identified lead compounds that bound to Hsp27 and tubulin via proteomic approaches. Systematic ligand based optimization in the current study significantly increased the cell growth inhibition and apoptosis inducing activities of the compounds. Compared to the lead compounds, one of the new derivatives exhibited much better potency to inhibit tubulin polymerization but a decreased activity to inhibit Hsp27 chaperone function, suggesting that the structural modification dissected the dual targeting effects of the compound. The most potent compounds 20 and 22 exhibited strong cell proliferation inhibitory activities at subnanomolar concentration against 60 human cancer cell lines conducted by Developmental Therapeutic Program at the National Cancer Institute and represented promising candidates for anticancer drug development.
Identifier
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<a href="http://doi.org/10.1021/jm4004736" target="_blank" rel="noreferrer noopener">10.1021/jm4004736</a>
Format
The file format, physical medium, or dimensions of the resource
Journal Article
2013
breast-cancer
c-dependent activation
cancer cells
chaperone activity
Chennamaneni S
cytochrome-c
Dowlati A
Geldenhuys W J
Heat-Shock Proteins
in-vitro
Journal Article
Journal of medicinal chemistry
Lama R
nimesulide analog jcc76
pancreatic-cancer
Pharmacology & Pharmacy
Pink J J
self-association
Su B
Xu Y
Yi X
Zhong B
Zhou A M
-
Text
A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text.
URL Address
<a href="http://doi.org/10.1021/jm300100d" target="_blank" rel="noreferrer noopener">http://doi.org/10.1021/jm300100d</a>
Rights
Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
Pages
3425-3435
Issue
7
Volume
55
Search for Full-text
Locate full-text within NEOMED Library's e-journal collections
<p>Users with a NEOMED Library login can search for full-text journal articles at the following url: <a href="https://libraryguides.neomed.edu/home">https://libraryguides.neomed.edu/home</a></p>
Dublin Core
The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/.
Title
A name given to the resource
Identification of a Class of Novel Tubulin Inhibitors
Publisher
An entity responsible for making the resource available
Journal of Medicinal Chemistry
Date
A point or period of time associated with an event in the lifecycle of the resource
2012
2012-04
Subject
The topic of the resource
agents; analog jcc76; biological evaluation; breast-cancer cells; halichondrin-b; heat-shock proteins; hsp27 phosphorylation; in-vivo; nimesulide; nonsteroidal antiinflammatory drugs; Pharmacology & Pharmacy; tumor-cells
Creator
An entity primarily responsible for making the resource
Yi X; Zhong B; Smith K M; Geldenhuys W J; Feng Y; Pink J J; Dowlati A; Xu Y; Zhou A M; Su B
Description
An account of the resource
We previously developed a series of anticancer agents based on cyclooxygenase-2 (COX-2) inhibitor nimesulide as a lead compound. However, the molecular targets of these agents still remain unclear. In this study, we synthesized a biotinylated probe based on a representative molecule of the compound library and performed protein pull-down assays to purify the anticancer targets of the compound. Via proteomic approaches, the major proteins bound to the probe were identified to be tubulin and heat shock protein 27 (Hsp27), and the compound inhibited tubulin polymerization by binding at the colchicine domain. However, the tubulin inhibitory effect of the compound activated the Hsp27 phosphorylation and possibly overrode the direct Hsp27 inhibitory effects, which made it difficult to solely validate the Hsp27 target. Taken together, the compound was a dual ligand of tubulin and Hsp27, inhibited tubulin polymerization, and had the potential to be a class of new chemotherapeutic agents.
Identifier
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<a href="http://doi.org/10.1021/jm300100d" target="_blank" rel="noreferrer noopener">10.1021/jm300100d</a>
Format
The file format, physical medium, or dimensions of the resource
Journal Article
2012
agents
analog jcc76
biological evaluation
breast-cancer cells
Dowlati A
Feng Y
Geldenhuys W J
halichondrin-b
Heat-Shock Proteins
hsp27 phosphorylation
in-vivo
Journal Article
Journal of medicinal chemistry
nimesulide
nonsteroidal antiinflammatory drugs
Pharmacology & Pharmacy
Pink J J
Smith K M
Su B
tumor-cells
Xu Y
Yi X
Zhong B
Zhou A M