Abstract:
:Our previous work has shown that the amino acid residues around 62-67 located in the connecting loop between helix I and II of human growth hormone (hGH) are important in eliciting the differentiation of preadipose 3T3-F442A cells to adipocytes. In this study, we evaluated the role of the charged residues around 62-67 in receptor binding and biological activity. Eight artificial mutant variants of hGH were prepared in Escherichia coli by site-directed mutagenesis. Replacement of Arg64 with Tyr (R64Y variant) resulted in a significant loss of binding to the somatogenic receptors on 3T3-F442A cells, but retained full adipose conversion activity on these cells. Replacement of Arg64 with Glu (R64E) produced a considerable loss in receptor binding and a significant loss in biological activity. hGH variants in which either Glu65 or Glu66 was replaced with Asp (E65D and E66D) and with Gln (E65Q and E66Q) showed a slight loss in binding activity and retained almost a full adipogenic activity. An E65P variant (replacement of Glu65 with Pro) possessed the same binding activity as hGH, although it failed to induce full biological activity. The insertion of Ala between Asn63 and Arg64 (63NAR) caused a marked loss in both activities. These results indicate that the positively charged Arg64 is important for receptor binding and thereby in eliciting the biological activity of hGH, while negatively charged Glu65 and Glu66 are less important. In addition, our findings confirm that the conformation and size of the loop region around Arg64 is important for the adipose conversion activity of hGH.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Uchida E,Shimokawa S,Takasu H,Ikehara M,Uesugi S,Tomita K,Tanaka A,Morikawa M,Nishikawa S,Hayakawa Tdoi
10.1248/bpb.18.797subject
Has Abstractpub_date
1995-06-01 00:00:00pages
797-801issue
6eissn
0918-6158issn
1347-5215journal_volume
18pub_type
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1995-05-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1995-09-01 00:00:00
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更新日期:2001-07-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1999-03-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 临床试验,杂志文章
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1995-04-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1998-04-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2009-05-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:1995-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2006-02-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2007-03-01 00:00:00
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更新日期:2011-01-01 00:00:00
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更新日期:2014-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2020-01-01 00:00:00
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journal_title:Biological & pharmaceutical bulletin
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更新日期:2011-01-01 00:00:00
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更新日期:1995-12-01 00:00:00