Effects of macrocycle size and rigidity on melanocortin receptor-1 and -5 selectivity in cyclic lactam α-melanocyte-stimulating hormone analogs

Chemical Biology and Drug Design

Volumn 67, Issue 5, 2006, Pages 329-335

  Mayorov, Alexander V ^a   Han, So Yeop ^b   Cai, Minying ^a   Hammer, Matthew R ^a   Trivedi, Dev ^a   Hruby, Victor J ^a  

^a University of Arizona   (United States)

^b Ewha Womans University   (South Korea)

Author keywords

Melanocyte stimulating hormone; Antagonist; Human melanocortin 1 receptor; Human melanocortin 5 receptor; Macrocyclic; Melanocortin; Peptide

Indexed keywords

ALPHA AMINO ACID; ALPHA INTERMEDIN DERIVATIVE; DICARBOXYLIC ACID; FUNCTIONAL GROUP; HISTIDINE; LACTAM DERIVATIVE; LYSINE; MACROCYCLIC COMPOUND; MALEIC ACID DERIVATIVE; MELANOCORTIN 1 RECEPTOR; MELANOCORTIN 5 RECEPTOR; PHTHALIC ACID DERIVATIVE; PYRAZINE DERIVATIVE; PYRIDINE DERIVATIVE; RECEPTOR BLOCKING AGENT;

ARTICLE; BINDING ASSAY; BIOCHEMISTRY; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG CONFORMATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; EMBRYO; HUMAN; HUMAN CELL; HYDROPHILICITY; IC 50; MOLECULAR SIZE; PRIORITY JOURNAL; PROTEIN FUNCTION; RECEPTOR AFFINITY; RIGIDITY; STRUCTURE ACTIVITY RELATION;

ADENYLATE CYCLASE; ALPHA-MSH; BINDING, COMPETITIVE; CELL LINE; DRUG DESIGN; HUMANS; KIDNEY; LACTAMS, MACROCYCLIC; MOLECULAR STRUCTURE; RECEPTOR, MELANOCORTIN, TYPE 1; RECEPTORS, CORTICOTROPIN; TRANSFECTION;

EID: 33745232379     PISSN: 17470277     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1747-0285.2006.00383.x     Document Type: Article

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