Effect of Replacing the Aspartic Acid/Glutamic Acid Residues of Bullfrog Sialic Acid Binding Lectin with Asparagine/Glutamine and Arginine on the Inhibition of Cell Proliferation in Murine Leukemia P388 Cells.
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- Ogawa Yuko
- Department of Microbiology, Hoshi College of Pharmacy
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- Iwama Masanori
- Department of Microbiology, Hoshi College of Pharmacy
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- Ohgi Kazuko
- Department of Microbiology, Hoshi College of Pharmacy
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- Tsuji Tsutomu
- Department of Microbiology, Hoshi College of Pharmacy
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- Irie Masachika
- Department of Microbiology, Hoshi College of Pharmacy
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- Itagaki Tadashi
- Department of Microbiology, College of Pharmacy, Nihon University
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- Kobayashi Hiroko
- Department of Microbiology, College of Pharmacy, Nihon University
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- Inokuchi Norio
- Department of Microbiology, College of Pharmacy, Nihon University
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Abstract
The sialic acid binding lectin from bullfrog oocytes (cSBL) is known to have anti-tumor activity. In a previous report, to elucidate the relationship between the net charge and anti-tumor activity of cSBL, we examined the effect of chemical modifications of cSBL with a water-soluble carbodiimide in the presence of various nucleophiles. The results suggested that the anti-tumor activity and internalization into tumor cells increased with an increase in the net charge of cSBL. However, in the chemically modified cSBL, a modification site was observed on average in two of the carboxyl groups of cSBL. To confirm these previous results and to determine which modified carboxyl group contributes to the increase in anti-tumor activity, we prepared mutants with substitutions of Asn/Gln and Arg at three acidic amino acid residues of cSBL and studied their anti-tumor activity and internalization efficiency. The results showed the enhancing effect of charge on anti-tumor activity and internalization, and suggested that the replacement of D24 and E88 of cSBL with arginine is more effective than that of E97. The double mutant D24RE88R showed comparable anti-tumor activity to the ethylenediamine-modified cSBL reported previously. The mutant was well-characterized as a pure cSBL derivative suitable for studying the mechanism of the anti-tumor action of cSBL.
Journal
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- Biological and Pharmaceutical Bulletin
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Biological and Pharmaceutical Bulletin 25 (6), 722-727, 2002
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390001204628294272
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- NII Article ID
- 110003638746
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- NII Book ID
- AA10885497
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- COI
- 1:CAS:528:DC%2BD38XkvV2hu7c%3D
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- ISSN
- 13475215
- 09186158
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- NDL BIB ID
- 6174945
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- PubMed
- 12081136
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed