Abstract：
:Using minimum energy calculations and molecular dynamics techniques the preferred conformational states of LHRH and its analogues have been reported to involve a modified beta-bend between residues 5 to 8. Based on some of these models cyclic peptide analogues of LHRH antagonists were synthesised using solid phase peptide synthesis methodology. The analogues were tested for their ability to inhibit ovulation in normal cycling rats. Some analogues were also tested in receptor binding and in vitro LH release assays. The most potent cyclic peptide analogue, Ac-D-Phe(p-C1)-D-Phe(p-C1)-D-Trp-Ser-Glu-D-Arg-Leu-Lys-Pro-D-Ala-NH2 (V), had an ED50 value of 91.9 micrograms/kg in the inhibition of ovulation test. The corresponding linear peptide (IV) was about three times less potent. Analogues with smaller or larger ring sizes or with modifications within the ring were also prepared but these were either less potent or inactive, up to a dose of 1000 micrograms/kg, in inhibiting ovulation in normal cycling rats.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Dutta AS,Gormley JJ,McLachlan PF,Woodburn JRdoi
10.1016/0006-291x(89)92224-9subject
Has Abstractpub_date
1989-03-31 00:00:00pages
1114-20issue
3eissn
0006-291Xissn
1090-2104pii
0006-291X(89)92224-9journal_volume
159pub_type
杂志文章abstract：:We examined the expression of a Caenorhabditis elegans (C. elegans) elav-like gene, which we designated elr-1. The elr-1 gene encodes a predicted 456-amino-acid protein containing three putative RNA-binding domains and belongs to the ELAV family, which is functionally involved in neuronal differentiation. Northern blo...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1999.0957
更新日期：1999-07-14 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1993.1811
更新日期：1993-07-15 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(86)91237-4
更新日期：1986-05-29 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
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journal_title：Biochemical and biophysical research communications
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doi：10.1016/j.bbrc.2013.11.099
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(86)80307-2
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2005.05.198
更新日期：2005-08-12 00:00:00
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journal_title：Biochemical and biophysical research communications
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更新日期：1983-09-30 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2008.12.169
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2004.10.140
更新日期：2004-12-17 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1993.1025
更新日期：1993-01-15 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2019.03.037
更新日期：2019-04-30 00:00:00
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更新日期：2009-11-06 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2008.05.056
更新日期：2008-07-25 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1998.8356
更新日期：1998-03-27 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
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更新日期：2020-11-28 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
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更新日期：2014-09-12 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
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journal_title：Biochemical and biophysical research communications
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更新日期：2018-01-01 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(05)80239-6
更新日期：1991-04-30 00:00:00
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journal_title：Biochemical and biophysical research communications
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更新日期：1999-10-05 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2008.03.153
更新日期：2008-06-20 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1996.1553
更新日期：1996-10-14 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(92)90812-y
更新日期：1992-07-31 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.2000.2109
更新日期：2000-02-16 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(90)92118-j
更新日期：1990-07-31 00:00:00
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journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1995.2639
更新日期：1995-11-02 00:00:00
abstract：:The alpha(1c) subunit of the cardiac L-type Ca(2+) channel, which contains the channel pore, voltage- and Ca(2+)-dependent gating structures, and drug binding sites, has been well studied in heterologous expression systems, but many aspects of L-type Ca(2+) channel behavior in intact cardiomyocytes remain poorly chara...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2005.02.015
更新日期：2005-04-08 00:00:00
