• Interaction

    AccNo. 50766 Score 0.49
    Name PM_3133968
    Kd 1.0

    Peptide

    AccNo. 50644
    Name YXXN
    Sequence YXXN
    50644_small
    Internalized no
    Is Motif no

    Interactor

    AccNo. 50266
    Name unknown

    Experiment

    AccNo. 50608
    Classification incorrect?
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    is used to improve the automatic classification.
    Voting_motivation
    CA CVD DM APO ANG MI BD
    0.67 0.69 1.00 1.00 0.12 0.20 1.00 Vote
    plus plus plus plus plus plus plus Yes
    minus minus minus minus minus minus minus No
    Name PM_3133968
    Detection unspecified method, MI:0686
    Source Pubmed Text Id 3133968
    Journal Ann N Y Acad Sci. 1988;527:44-50.
    Title Potent long-acting growth hormone releasing factor analogues.
    Authors Rivier J, Rivier C, Galyean R, Yammamoto G, Vale W
    Text Amidated fragments 1 to 29 of human growth hormone releasing factor, (GRF1-29NH2), were designed to encompass modifications that could prevent degradation by exopeptidases. The NH2-terminus was blocked by either N-methylation of Tyr1 or by introduction of NMeDAla2 while the COOH-terminus was blocked by an N-ethylamide. Other substitutions such as Nle in position 27 for methionine conferred stability toward air oxidation while Asn28, an amino acid substitution found in rat GRF, seemed to confer stronger binding affinity to the GRF receptor. Potency in vitro and duration of action in vivo of [NMeTyr1,Nle27,Asn28]hGRF1-29NHEt (4SG-29) were compared to those of hGRF1-40OH. 4SG-29 was found to be both ten times more potent than hGRF1-40)OH and exhibit significantly extended duration of action.
    Mesh Terms Amino Acid Sequence; Animals; Exopeptidases; Growth Hormone/blood; Growth Hormone-Releasing Hormone/analogs & derivatives; Growth Hormone-Releasing Hormone/chemical synthesis; Growth Hormone-Releasing Hormone/pharmacology; Kinetics; Male; Peptide Fragments/pharmacology; Peptide Hydrolases/metabolism; Rats; Rats, Inbred Strains; Structure-Activity Relationship
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