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Design, synthesis, and molecular modeling of a novel amide-linked cyclic GnRH analogue cyclo(4-9)[Lys4,D-Trp6,Glu9]GnRH: stimulation of gonadotropin gene expression.
Keramida, Maria K; Tselios, Theodore; Mantzourani, Efthimia; Papazisis, Kostas; Mavromoustakos, Thomas; Klaussen, Christian; Agelis, George; Deraos, Spyros; Friligou, Irene; Habibi, Hamid; Matsoukas, John.
Afiliação
  • Keramida MK; Department of Chemistry, University of Patras, 26500 Patras, Greece. maria_keram@yahoo.gr
J Med Chem ; 49(1): 105-10, 2006 Jan 12.
Article em En | MEDLINE | ID: mdl-16392796
This report describes the rational design, synthesis, and pharmacological properties of an amide-linked cyclic analogue of gonadotropin-releasing hormone (GnRH) namely Cyclo(4-9)[Lys(4),d-Trp(6),Glu(9)]GnRH. The conformationally restricted analogue is characterized by reduced flexibility of the peptide strand due to the introduction of a beta-turn mimetic through 4,9 residue amide cyclization. The cyclic analogue was found to stimulate gonadotropin gene expression in the goldfish pituitary with similar potency compared to two native forms of GnRH. Simulation studies based on ROE connectivities in linear GnRH and potency of cyclic analogue supports the His(2), Trp(3), Tyr(5) clustering considered important for triggering receptor activation.
Assuntos
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Base de dados: MEDLINE Assunto principal: Peptídeos Cíclicos / Modelos Moleculares / Regulação da Expressão Gênica / Hormônio Liberador de Gonadotropina / Amidas / Gonadotropinas Idioma: En Revista: J Med Chem Ano de publicação: 2006 Tipo de documento: Article País de afiliação: Grécia
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Base de dados: MEDLINE Assunto principal: Peptídeos Cíclicos / Modelos Moleculares / Regulação da Expressão Gênica / Hormônio Liberador de Gonadotropina / Amidas / Gonadotropinas Idioma: En Revista: J Med Chem Ano de publicação: 2006 Tipo de documento: Article País de afiliação: Grécia