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G
rowth hormone releasing peptide 6 (GHRP-6) was Feeding Regulatory
the first synthetic peptide that was shown to re- Peptides Series
lease growth hormone (GH) and stimulate weight
gain by binding to growth hormone secretagogue Peptides International offers obestatin, truncated obestatin,
receptor type 1a (GSR1a).1-2 Ghrelin, the endogenous ligand full length acyl and des-acyl ghrelin and ghrelin fragments,
for GSR1a, was later isolated.3 This orexigenic and GH releas- and several ghrelin antagonists to complete your research
ing peptide is derived from ghrelin preproprotein. It is ex- needs. Our acyl and des-acyl ghrelin fragments consist-
pressed primarily in the stomach and has been shown to de- ing of the first 5, 10, 14 or 18 amino acids and contain the
crease insulin levels and increase appetite, body weight gain, core amino acids required for proper binding and activa-
fat accumulation, and glucose and GH levels, suggesting this tion of GHSR1a.13 [Dap3]-Ghrelin (Rat) (PGH-3680-PI) and
peptide plays a highly important physiological role in metab- [Dap3]-Ghrelin (Human, Rat, 1-5) (PGH-3681-PI) analogs
olism.3,4-7 In addition, it may also modulate cell proliferation are replaced with 2,3-diaminopropionic acid (Dap) at Ser3.
of cancer cells and cardiomyocytes. 8-9 This substitution should make the analogs more stable and
less susceptible to esterases and acyl migration.13 Ghrelin
Two forms of ghrelin can be found in circulation: an acyl- analogs with the Dap substitution have been shown to acti-
ated form and a non-acylated form. The acylated form of vate growth hormone secretagogues receptor 1a (GHSR1a)
ghrelin contains an n-octanoic acid at the Ser3 residue that is just as efficiently as the parent peptide.13 The variety
required for activation of GSR1a. Therefore, it was originally of research tools we are able to offer at Peptides
believed that des-acyl ghrelin, which lacks this esterification International may help scientists elucidate the complex regu-
at Ser3, is an inactive form though it is the predominant one lation of appetite and weight gain.
found in circulation. Accumulating evidence, however, in-
dicates that des-acyl ghrelin can counteract some metabolic Nesfatin-1 was discovered in 2006 by Oh-I and colleagues.14
responses of acylated ghrelin in humans, and mice injected The peptide is secreted from hypothalamic nuclei, which
with or over expressed with the des-acyl form were found to are responsible for controlling appetite. In this same report,
decrease food intake and gastric emptying.4, 5, 10 Other studies nesfatin-1 suppressed food intake in obese mice with a
showed both forms of ghrelin mediate cell proliferation and leptin gene knockout. This finding implies that the peptide
fat accumulation.8, 9, 11 Collectively, these studies suggest an may function as an appetite suppressant independent of the
alternative receptor exists for ghrelin that is not dependent leptin pathway.15
on n-octanoylation of Ser3 for activation. Studying des-acyl Peptides International is pleased to offer our Nesfatin-1
ghrelin may offer new insight into the regulation of homeo- (Human), Nesfatin-1 (Rat), Nesfatin-1 Like Peptide
stasis and energy balance. (Mouse)and Nesfatin-1 (30-59) (Human), along with all of
O = C - (CH ) - CH our Ghelin and Obestatin products for your research activi-
26 3
O Ghrelin (Human) ties.
1. A.D. Howard et al., Science, 273, 974 (1996).
2. C.Y. Bowers, et al., Endocrinology, 114, 1537 (1984).
3. M. Kojima, et al., Nature, 402, 656 (1999).
4. F. Broglio, et al., J. Clin. Endoc. and Metabolism, 89, 3062 (2004).
Currently, in addition to ghrelin, a number of gastrointesti- 5. C. Gauna et al., J. Clin. Endoc. and Metabolism, 89, 5035 (2004).
6. M. Tschop, et al., Nature, 407, 908 (2000).
nal hormones have been identified that control appetite by 7. A. Asakawa, et al., Gastroenterology, 120, 337 (2001).
either stimulating food intake and gastric emptying or inhib- 8. P. Cassoni, et al., Eur. J. Endoc., 150, 173 (2004).
9. G. Baldanzi, et al., J. Cell Biol., 159, 1029 (2002).
iting these responses. Zhang et al. has recently identified one 10. A. Asakawa, et al., Gut, 54, 18 (2005).
of the newest members of this family by using bioinformatic 11. N.M. Thompson, et al., Endoc., 145, 234 (2004).
12 J.V. Zhang, et al., Science, 310, 996 (2005).
predictions about enzyme cleavage of the prepropeptide of 13. M.A. Bednarek, et al., J. Med. Chem., 43, 4370 (2000).
ghrelin.12 The newly identified 23 amino acid, ghrelin-asso- 14. I.S. Oh, et al., Nature, 443, 709 (2006).
ciated peptide was named obestatin (PGH-3890-PI and PGH- 15. M.A. Cowley and K.L. Grove, Cell Metab., 4, 421 (2006).
PGH-3656-PI H-His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH2 1 mg
[D-Lys3]-Growth Hormone Releasing Peptide-6 (GHRP-6) 5 mg
(M.W. 930.13) C49H63N13O6
Ghrelin Antagonist
K. Fujino, et al., J. Physiol., 550, 227 (2003).
PGH-3694-PI H-His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 1 mg
[His1,Lys6]-Growth Hormone Releasing Peptide (GHRP-6) 5 mg
(M.W. 873.04) C46H56N12O6
Growth Hormone Releasing Peptide
C.Y. Bowers, et al., Endocrinol., 114, 1537 (1984).
PGH-3908-PI H-Lys-d-Trp-Phe-d-Trp-Leu-Leu-NH2
Potent Full Inverse Agonist for Ghrelin Receptor
B. Holst, et al., Mol. Pharmacol., 70, 936 (2006).
PGH-3911-PI H-d-Ala-d-Nal(2)-Ala-Trp-d-Phe-Lys-NH2
GHRP-2 or KP102
Ghrelin agonist growth hormone releasing peptide 2