Preparation of human melanocortin-4 receptor agonist libraries: Linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z- NH2

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 24, 2005, Pages 5504-5508

  Cheung, Adrian Wai Hing ^a   Qi, Lida ^a   Gore, Vijay ^a   Chu, Xin Jie ^a   Bartkovitz, David ^a   Kurylko, Grazyna ^a   Swistok, Joseph ^a   Danho, Waleed ^a   Chen, Li ^a   Yagaloff, Keith ^a  

^a HOFFMANN LA ROCHE INC   (United States)

Author keywords

Agonist; Melanocortin receptors; Peptides

Indexed keywords

MELANOCORTIN RECEPTOR 4 AGONIST; PEPTIDE DERIVATIVE; PEPTIDE LIBRARY; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; RADIOFREQUENCY;

AMINO ACID SEQUENCE; GLYCINE; HUMANS; OLIGOPEPTIDES; PEPTIDE LIBRARY; RECEPTOR, MELANOCORTIN, TYPE 4; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 27644553920     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.08.083     Document Type: Article

References (19)

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12. 15 were pooled for washing only. The Macrokans were sorted using Synthesis Manager, the resins in each Macrokan were cleaved with 95% trifluoroacetic acid, and the cleavage products were transferred to bar-coded scintillation vials. The above crude peptides were purified using reversed-phase HPLC and the purified samples all had purities >95% by LC/MS analysis.
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16. 2 displayed 32% activation at hMC4R and 40% activation at hMC1R at 100 nM and was not further profiled.
17. 3CN (buffer B) with UV detection at 280 nm.
18. For more information about the Quest 210 Synthesizer, see: www.argotech.com.
19. 2, was lost during purification and was not re-synthesized.