Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/13995
ชื่อเรื่อง: Novel small-molecule compounds that affect cellular morphogenesis in yeast and mammalian cells
ผู้แต่ง: Fukunaga T.
Nakamura M.
Kitagawa T.
Watanapokasin R.
Hoshida H.
Akada R.
Keywords: Actin polymerization
Bni1
Boi1
Formin
Pleckstrin homology domains
Cells
Cytology
Defects
Diagnosis
Mammals
Molecules
Morphology
Polymerization
Yeast
Proteins
actin
actin binding protein
Bni1 protein, S cerevisiae
BOI1 protein, S cerevisiae
Saccharomyces cerevisiae protein
signal transducing adaptor protein
animal
article
cell strain HEK293
chemistry
cytoskeleton
drug effect
human
metabolism
molecular library
morphogenesis
Saccharomyces cerevisiae
Actins
Adaptor Proteins, Signal Transducing
Animals
Cytoskeleton
HEK293 Cells
Humans
Microfilament Proteins
Morphogenesis
Saccharomyces cerevisiae
Saccharomyces cerevisiae Proteins
Small Molecule Libraries
วันที่เผยแพร่: 2013
บทคัดย่อ: Drugs affecting cellular morphological changes leading to tumor cell migration and invasion are desirable for cancer therapy. In the present study, we screened for small-molecule compounds that affect the cellular morphology of both unicellular yeast and mammalian HEK293 cells to identify drug candidates. The yeast formin protein Bni1 and Src homology 3 (SH3)-pleckstrin homology (PH) domain protein Boi1, which are required for proper morphogenesis, cause growth defects when overexpressed in yeast. Using this system, we screened a chemical library consisting of -8000 compounds to identify drug candidates that suppress these growth defects. None of the screened compounds induced morphological changes in vegetatively growing yeast cells, but several compounds had inhibitory effects on pheromone-induced projection formation and actin localization, suggesting that these compounds affected a specific stage of morphogenesis. Five of the compounds also induced morphological changes in mammalian HEK293 cells. Among the identified compounds, BTB03156, 2-[(4-chlorophenyl)sulfonyl]-1-methyl-3,5- dinitrobenzene, and BTB02467, 1-[(4-chlorophenyl)sulfonyl]- 2-nitro-4-(trifluoromethyl)benzene, although they have similar structures, displayed differing effects on the yeast growth defects caused by latrunculin A, an actin polymerization inhibitor. The chemical library compounds identified using this in vivo screening approach are simple, cell-permeable molecules, and therefore may be useful in the development of therapeutic drugs for cancer metastasis and other actinrelated diseases.
URI: https://ir.swu.ac.th/jspui/handle/123456789/13995
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84883718770&doi=10.1271%2fbbb.130212&partnerID=40&md5=e4b95eed234c5cffdcb4f62e0012529d
ISSN: 9168451
Appears in Collections:Scopus 1983-2021

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