Design and synthesis of highly potent and selective melanotropin analogues of SHU9119 modified at position 6

Biochemical and Biophysical Research Communications

Volumn 292, Issue 4, 2002, Pages 1075-1080

  Grieco, Paolo ^a   Han, Guoxia ^a   Hruby, Victor J ^a   Weinberg, David ^b   Van der Ploeg, L H T ^b  

^a University of Arizona   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC AMP; INTERMEDIN DERIVATIVE; MELANOCORTIN RECEPTOR; MELANOTAN II; N ACETYL ALPHA INTERMEDIN[4-10]CYCLO[4 NORLEUCINE 5 ASPARTIC ACID 7 [3 (2 NAPHTHYL)ALANINE] 10 LYSINAMIDE]; PG 901; PG 908; PG 909; PG 910; PG 911; PG 948; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG CONFORMATION; DRUG DESIGN; DRUG POTENCY; DRUG PURIFICATION; DRUG SELECTIVITY; DRUG SYNTHESIS; IC 50; NONHUMAN; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

EID: 0036283824     PISSN: 0006291X     EISSN: None     Source Type: Journal    
DOI: 10.1006/bbrc.2002.6739     Document Type: Article

References (49)

1. Regulation of the synthesis of steroidogenic in the adrenal cortical cells by ACTH
2. Melanocortin antagonists define two distinct pathway of cardiovascular control by α- and γ- melanocyte-stimulating hormones
3. 2-melanocyte-stimulating hormone and related melanotropins depend on the arousal potential of the rat
4. Antipyretic role of endogenous melanocortins mediated by central melanocortin receptors during endotoxin-induced fever
5. Melanocortins in peripheral nerve regeneration: Influence of dosage forms and routes of administration
6. Neuropeptide hormones as neurotrophic factors
7. Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
8. Antipyretic role of endogenous melanocortins mediated by central melanocortin receptors during endotoxin-induced fever
9. Melanocortin antagonists define two distinct pathways of cardiovascular control by α- and γ- melanocyte-stimulating hormones
10. Prevention of reflex natriuresis after acute unilateral nephrectomy by melanocortin receptor antagonists
11. The cloning of a family of genes that encode the melanocortin receptors
12. Cloning and functional characterization of family of receptors for the melanotrophic peptides
13. Obesity, diabetes and functions for proopiomelanocortin-derived peptides
14. Molecular cloning of a novel melanocortin receptor
15. Distribution of cDNA for melanocortin receptor subtypes in human tissues
16. Molecular cloning, expression, and gene localization of a fourth melanocortin receptor
17. Molecular cloning of a mouse melanocortin 5 receptor gene widely expressed in peripheral tissues
18. Cloning and expression of a member of the melanocyte-stimulating hormone receptor family
19. Characterization of melanocortin receptor subtypes by radioligand binding analysis
20. Characterization of melanocortin 4 receptor by radioligand binding analysis
21. Melanocortins and their implications in melanoma
22. Exocrine gland dysfunction in MC5-R-deficient mice: Evidence for coordinated regulation of exocrine gland function by melanocortin peptides
23. Melanotropin peptides for therapeutic and cosmetic tanning of the skin
24. Three-dimensional molecular models of the hMC1R melanocortin receptor: Complexes with melanotropin peptide agonists
25. Functional variants of the MSH receptor (MC1-R), agouti and their effects on mammalian pigmentation
26. α-Melanotropin. The minimal active sequence in the lizard skin bioassay
27. α-Melanotropin the minimal active sequence in frog skin bioassay
28. 7]-α-MSH. Discovery of a tripeptidyl agonist exhibiting sustained bioactivity
29. Design of a new class of superpotent cyclic α-melanotropins based on quenched dynamic stimulations
30. 10]- α-MSH(4 -10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency, and selectivity at specific melanocortin receptor
31. Design of new small cyclic melanocortin receptor-binding peptides using molecular modelling: Role of the His residue in the melanocortin peptide core
32. Preparation of "side-chain-to-side-chain" cyclic peptides by allyl and alloc strategy: Potential for library synthesis
33. Minimization of tryptophan alkylation following 9-fluorenylmethoxycarbonyl solid-phase peptide-synthesis
34. Trialkylsilanes as scavengers for the trifluoroacetic acid deblocking of protecting groups in peptide-synthesis
35. 4-Norleucine, 7-D-phenylalanine-3-melanocyte-stimulating hormone: A highly potent α-melanotropin with ultra long biological activity
36. Melanotropin: Structural, conformational and biological considerations in the development of superpotent and superprolonged analogs
37. A new class of positively charged melanotropin analogs: A new concept in peptide design
38. Cationized melanotropin analogues: Structure-function relationships
39. Studies of conformational isomerism in α-melanocyte stimulating hormone by design of cyclic analogues
40. Emerging approaches in the molecular design of receptor-selective peptide ligands: Conformational, topographical and dynamic consideration
41. Design of peptides, protein, and peptidomimetics in chi space
42. 2): A potent and specific agonist for morphine (μ) receptors
43. Ac-[3-and 4-Alkylthioproline]-CCK4 analogs: Synthesis and implications for the CCK-b receptor-bound conformation
44. Pseudo-proline induction of cis/trans-conformational interconversion by decreased transition state barriers
45. Pseudoproline (ψPro) in drug design: Direct insertion of ψPro system into cyclosporin
46. Structure-function studies of the cyclic peptide MT-II lactam derivatives of α-melanotropin