A potent HDAC inhibitor, 1-alaninechlamydocin, from a Tolypocladium sp. induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
A potent HDAC inhibitor, 1-alaninechlamydocin, from a Tolypocladium sp. induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
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DOI:
10.1021/np500387h
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发表时间:
2014-07-25
影响因子:
5.1
通讯作者:
Cichewicz, Robert H.
中科院分区:
文献类型:
--
作者:
Du, Lin;Risinger, April L.;King, Jarrod B.;Powell, Douglas R.;Cichewicz, Robert H.
The cyclic tetrapeptide 1-alaninechlamydocin was purified from a Great Lakes-derived fungal isolate identified as a Tolypocladium sp. Although the planar structure was previously described, a detailed analysis of its spectroscopic data and biological activity are reported here for the first time. Its absolute configuration was determined using a combination of spectroscopic (1H–1H ROESY, ECD, and X-ray diffraction) and chemical (Marfey’s analysis) methods. 1-Alaninechlamydocin showed potent antiproliferative/cytotoxic activities in a human pancreatic cancer cell line (MIA PaCa-2) at low-nanomolar concentrations (GI50 5.3 nM, TGI 8.8 nM, LC50 22 nM). Further analysis revealed that 1-alaninechlamydocin induced G2/M cell cycle arrest and apoptosis. Similar to other cyclic epoxytetrapeptides, the inhibitory effects of 1-alaninechlamydocin are proposed to be produced primarily via inhibition of histone deacetylase (HDAC) activity.
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DOI:
10.1016/b978-0-12-391494-1.00008-2
发表时间:
2013-01-01
期刊:
EPIGENETIC REGULATION IN THE NERVOUS SYSTEM: BASIC MECHANISMS AND CLINICAL IMPACT
影响因子:
--
作者:
Nott, Alexi;Fass, Daniel M.;Tsai, Li-Huei
通讯作者:
Tsai, Li-Huei
影响因子:
5.2
作者:
Cai S;Du L;Gerea AL;King JB;You J;Cichewicz RH
通讯作者:
Cichewicz RH
影响因子:
4
作者:
You, Jianlan;Du, Lin;King, Jarrod B.;Hall, Brian E.;Cichewicz, Robert H.
通讯作者:
Cichewicz, Robert H.
DOI:
10.1042/cs20120504
发表时间:
2013-06
期刊:
Clinical science (London, England : 1979)
影响因子:
--
作者:
Tang J;Yan H;Zhuang S
通讯作者:
Zhuang S
影响因子:
2.1
作者:
Mohseni, Jafar;Zabidi-Hussin, Z.A.M.H.;Sasongko, Teguh Haryo
通讯作者:
Sasongko, Teguh Haryo