Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor

Journal of Medicinal Chemistry

Volumn 52, Issue 12, 2009, Pages 3627-3635

  Qu, Hongchang ^a   Cai, Minying ^a   Mayorov, Alexander V ^a   Grieco, Paolo ^a,b   Zingsheim, Morgan ^a   Trivedi, Dev ^a   Hruby, Victor J ^a  

^a University of Arizona   (United States)

^b UNIVERSITY OF NAPLES FEDERICO II   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLNORLEUCINECYCLO[ASPARTYLHISTIDYL DEXTRO PHENYLALANYLARGINYLTRYPTOPHYLLYSINAMIDE]; ACETYLTYROSYLVALYLNORLEUCYLGLYCYLHISTIDYLPHENYLALANYLARGINYLTRYPTOPHYLASPARTYLAR GINYLPHENYLALANYLGLYCINAMIDE; ADENYLATE CYCLASE; AGOUTI PROTEIN; ARGININE; HISTIDINE; INTERMEDIN; INTERMEDIN DERIVATIVE; MELANOCORTIN 3 RECEPTOR; MELANOCORTIN 4 RECEPTOR; N ACETYL ALPHA INTERMEDIN[4-10]CYCLO[4 NORLEUCINE 5 ASPARTIC ACID 7 [3 (2 NAPHTHYL)ALANINE] 10 LYSINAMIDE]; PROLINE; PROLINE DERIVATIVE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ARTICLE; BETA TURN; BINDING AFFINITY; BINDING ASSAY; CONTROLLED STUDY; DOSE RESPONSE; DRUG DESIGN; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION;

ARGININE; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; HUMANS; LIGANDS; MELANOCYTE-STIMULATING HORMONES; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PROLINE; RECEPTOR, MELANOCORTIN, TYPE 4; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 67549105045     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm801300c     Document Type: Article

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