Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution

Autor:	Waleed Danho, Grazyna Kurylko, Adrian Wai-Hing Cheung, Joseph Swistok, Xin-Jie Chu, Keith A. Yagaloff, Li Chen, Lucia Franco
Rok vydání:	2003
Předmět:	Agonist Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Peptide Transfection Biochemistry Pentapeptide repeat Chemical synthesis Cell Line chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Peptide synthesis medicine Structure–activity relationship Humans Obesity Receptor Molecular Biology chemistry.chemical_classification Receptors Melanocortin Organic Chemistry chemistry Amino Acid Substitution Molecular Medicine Receptor Melanocortin Type 4 Melanocortin Oligopeptides
Zdroj:	Bioorganicmedicinal chemistry letters. 13(4)
ISSN:	0960-894X
Popis:	A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Nal and Bta) were identified in this study.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::183fdb19a21d265efd8b3234b8544370 https://pubmed.ncbi.nlm.nih.gov/12639550 Zobrazit plný text záznamu Full Text from ScienceDirect