Analogs of human growth hormone-releasing hormone, their preparation and use

Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab...

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Hauptverfasser: KUNCE DANUTA, ORLOWSKA ALICJA, IZDEBSKI JAN, BANKOWSKI KRZYSZTOF, KUTNER ANDRZEJ, WITKOWSKA EWA, SZELEJEWSKI WIESLAW, FRACKIEWICZ ELZBIETA
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creator KUNCE DANUTA
ORLOWSKA ALICJA
IZDEBSKI JAN
BANKOWSKI KRZYSZTOF
KUTNER ANDRZEJ
WITKOWSKA EWA
SZELEJEWSKI WIESLAW
FRACKIEWICZ ELZBIETA
description Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab or Gap; R21 is hArg, Orn, Gab or Gap; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino groups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.
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subjects CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Analogs of human growth hormone-releasing hormone, their preparation and use
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