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Semisynthesis of human growth hormone-releasing factor by trypsin catalyzed coupling of leucine amide to a C-terminal acid precursor.
Bongers, J; Offord, R E; Felix, A M; Campbell, R M; Heimer, E P.
Afiliação
  • Bongers J; Department of Peptide Research, Roche Research Center, Hoffmann-La Roche Inc., Nutley, New Jersey.
Int J Pept Protein Res ; 40(3-4): 268-73, 1992.
Article em En | MEDLINE | ID: mdl-1478784
Human growth hormone-releasing factor, GRF(1-44)-NH2, was synthesized by trypsin catalyzed coupling of Leu-NH2 to Arg43 of the precursor, GRF(1-43)-OH, prepared by solid phase peptide synthesis. The semisynthetic GRF(1-44)-NH2 was fully characterized and showed full potency in the rat pituitary in vitro bioassay. Conversion to GRF(1-44)-NH2 was limited to 60-70% in both 75% v:v N,N'-dimethylacetamide and 95% v:v 1,4-butanediol due to competing transpeptidations at Arg41 and Arg38 generating [Leu42]-GRF(1-42)-NH2 and [Leu39]-GRF(1-39)-NH2 side-products, respectively. The rates of formation and yields of GRF(1-44)-NH2 versus pH, Leu-NH2 concentration, and solvent composition were also studied.
Assuntos
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Base de dados: MEDLINE Assunto principal: Fragmentos de Peptídeos / Tripsina / Hormônio Liberador de Hormônio do Crescimento / Leucina Idioma: En Ano de publicação: 1992 Tipo de documento: Article
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Base de dados: MEDLINE Assunto principal: Fragmentos de Peptídeos / Tripsina / Hormônio Liberador de Hormônio do Crescimento / Leucina Idioma: En Ano de publicação: 1992 Tipo de documento: Article