NDLI: Synthetic peptides with the biological activities and specificity of human C3a anaphylatoxin.

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Synthetic peptides with the biological activities and specificity of human C3a anaphylatoxin.

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Synthetic peptides with the biological activities and specificity of human C3a anaphylatoxin.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Hugli, T. E. Erickson, B. W.
Abstract	Two peptides identical to the COOH-terminal sequence of human C3a anaphylatoxin and two analogs were synthesized by the solid-phase method and tested for biological activity. The synthetic COOH-terminal octapeptide, C3a-(70-77) or Ala-Ser-His-Leu-Gly-Leu-Ala-Arg, caused contraction of guinea pig ileum and uterus, release of vasoactive amines from rat mast cells, and increased vascular permeability in guinea pig and human skin. On a molar basis, the synthetic octapeptide possessed 1-2% of the biological activities of C3a and specifically desensitized smooth muscle to stimulation by C3a. Like natural C3a, the synthetic C3a=(70-77) was inactivated by digestion with carboxypeptidase B [peptidyl-L-lysine(-L-arginine) hydrolase, EC 3.4.12.3], which removed the essential COOH-terminal arginine. A synthetic nonapeptide [C3a-(70-77)-Gly], containing a glycyl instead of an arginyl COOH terminus, was approximately 1% as active as the octapeptide when assayed with smooth muscle. The COOH-terminal 13-residue peptide of C3a, C3a-(65-77), was equal in activity to C3a=(70-77); similarly, C3a-(65-77)-Gly expressed the same activity as C3a-(70-77)Gly. It is concluded that both the biological specificity and the activity of human C3a anaphylatoxin are determined by eight or fewer residues located at the COOH terminus of the natural protein. However, expression of full activity requires additional groups and the secondary conformational integrity of the C3a molecule.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	5
Volume Number	74
Language	English
Publisher	National Academy of Sciences
Publisher Date	1977-07-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Anaphylatoxins Complement C3 Complement System Proteins Oligopeptides Pharmacology Peptides Amino Acid Sequence Biological Assay Capillary Permeability Drug Effects Ileum Mast Cells Metabolism Muscle Contraction Muscle, Smooth Chemical Synthesis Serotonin Structure-Activity Relationship Uterus Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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