Document Detail


Biological properties of two models of calcitonin gene related peptide with idealized amphiphilic alpha-helices of different lengths.
MedLine Citation:
PMID:  3264724     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Previous studies on calcitonin gene related peptide (CGRP) have demonstrated that it has the characteristics of an amphiphilic peptide, and from an examination of the sequence, we have proposed that it contains an amphiphilic alpha-helix. We have synthesized two analogues of CGRP which have different lengths of idealized amphiphilic alpha-helical secondary structure. The first model, CGRM-1, has been substituted with residues generating an idealized amphiphilic alpha-helix in the region between residues 8 and 25, equivalent to approximately five turns of an alpha-helix. This peptide is not an agonist in any of our bioassays, but it does bind with low affinity to rCGRP receptors in crude liver membranes. Our second model, CGRM-2, has an idealized amphiphilic alpha-helix between residues 8 and 18, which is equivalent to approximately three turns of an alpha-helix. In an in vitro rat vas deferens assay, this peptide is an agonist with a potency one-fourth that of the native hormone. However, the potency of CGRM-2 in an adenylate cyclase assay is much lower, only 1/140th the potency of CGRP. Both model peptides display amphiphilic characteristics commensurate with their design. We conclude that there is an amphiphilic alpha-helix in rCGRP between residues 8 and 18 and that this helix terminates in the vicinity of residue 18.
Authors:
B Lynch; E T Kaiser
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Biochemistry     Volume:  27     ISSN:  0006-2960     ISO Abbreviation:  Biochemistry     Publication Date:  1988 Oct 
Date Detail:
Created Date:  1989-02-23     Completed Date:  1989-02-23     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0370623     Medline TA:  Biochemistry     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  7600-7     Citation Subset:  IM    
Affiliation:
Laboratory of Bioorganic Chemistry and Biochemistry, Rockefeller University, New York, New York 10021.
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MeSH Terms
Descriptor/Qualifier:
Adenylate Cyclase / metabolism
Amino Acid Sequence
Animals
Calcitonin Gene-Related Peptide
Liver / metabolism
Male
Models, Chemical
Molecular Sequence Data
Neuropeptides / metabolism,  pharmacology*
Protein Conformation
Rats
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
RR 00862-14/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Neuropeptides; 83652-28-2/Calcitonin Gene-Related Peptide; EC 4.6.1.1/Adenylate Cyclase

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