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A new curcumin derivative, HBC, interferes with the cell cycle progression of colon cancer cells via antagonization of the Ca2+/calmodulin function
Joong Sup Shim1; Jiyong Lee1; Hyun-Ju Park2; So-Jung Park2; Ho Jeong Kwon1
2004
Source PublicationCHEMISTRY & BIOLOGY
ISSN1074-5521
Volume11Issue:10Pages:1455-1463
Abstract

HBC (4-{3,5-Bis-[2-(4-hydroxy-3-methoxy-phenyl)-ethyl]-4,5-dihydro-pyrazol-1-yl}-benzoic acid) is a recently developed curcumin derivative which exhibits potent inhibitory activities against the proliferation of several tumor cell lines. In the present study, we identified Ca2+/calmodulin (Ca2+/CaM) as a direct target protein of HBC using phage display biopanning. Ca2+/CaM-expressing phages specifically bound to the immobilized HBC, and the binding was Ca2+ dependent. Moreover, flexible docking modeling demonstrated that HBC is compatible with the binding cavity for a known inhibitor, W7, in the C-terminal hydrophobic pocket of Ca2+/CaM. In biological systems, HBC induced prolonged phosphorylation of ERK1/2 and activated p21WAF1 expression, resulting in the induction of G0/G1 cell cycle arrest in HCT15 colon cancer cells. These results suggest that HBC inhibits the cell cycle progression of colon cancer cells via antagonizing of Ca2+/CaM functions.

DOIhttps://doi.org/10.1016/j.chembiol.2004.08.015
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology
WOS SubjectBiochemistry & Molecular Biology
WOS IDWOS:000224668700017
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Cited Times [WOS]:75   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Corresponding AuthorHo Jeong Kwon
Affiliation1.Chemical Genomics National Research Laboratory, Department of Bioscience and Biotechnology, Institute of Bioscience, Sejong University, Seoul 143-747, South Korea
2.College of Pharmacy, Sungkyunkwan University, Suwon, Kyungkido 440-746, South Korea
Recommended Citation
GB/T 7714
Joong Sup Shim,Jiyong Lee,Hyun-Ju Park,et al. A new curcumin derivative, HBC, interferes with the cell cycle progression of colon cancer cells via antagonization of the Ca2+/calmodulin function[J]. CHEMISTRY & BIOLOGY,2004,11(10):1455-1463.
APA Joong Sup Shim,Jiyong Lee,Hyun-Ju Park,So-Jung Park,&Ho Jeong Kwon.(2004).A new curcumin derivative, HBC, interferes with the cell cycle progression of colon cancer cells via antagonization of the Ca2+/calmodulin function.CHEMISTRY & BIOLOGY,11(10),1455-1463.
MLA Joong Sup Shim,et al."A new curcumin derivative, HBC, interferes with the cell cycle progression of colon cancer cells via antagonization of the Ca2+/calmodulin function".CHEMISTRY & BIOLOGY 11.10(2004):1455-1463.
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