Scientists Report Active Ghrelin Fragments and Ghrelin Antagonist
Ghrelin:  Endogenous Growth-Hormone Releasing Peptide with Novel Regulatory Mechanism

Ghrelin Peptides from Peptides International


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Ghrelin Peptide Increases Food Intake  - 7/19/2006

A novel pentapeptide (Gly-Ser-Trp-Phe-Arg) analog of ghrelin was recently shown to stimulate food intake following oral and intravenous administration in animals.1   The researchers took the original tetrapeptide active core [Gly-Ser-Ser(n-Octanoyl)-Phe] required for ghrelin activity and substituted the octanoyl Ser with Trp.  They found this substitution did not abolish activity though binding affinity to growth hormone secretagogue receptor (GSR) was reduced.  However, the addition of Arg at the C-terminus enhanced binding affinity while maintaining activity.  Gly-Ser-Trp-Phe-Arg or [Trp3, Arg5]-Ghrelin (1-5) (PGH-3902-PI) is currently a new addition to our existing ghrelin peptides and analogs.  It may prove to be a useful tool since this short analog can be absorbed more easily by mice compared to full length ghrelin and has been shown to be a successful ghrelin agonist.

1.  K. Ohinata, K. Kobayashi, M. Yoshikawa, Peptides, 27, 1632 (2006).

New! Ghrelin Antagonist and Non-Acylated Ghrelin Now Available

Recently, Holst and coworkers reported a substance P analog to be a low potency ghrelin antagonist.  In 1988, [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P was originally reported by Woll et al. to be a potent bombesin antagonist able to inhibit small cell lung cancer growth in vitro. Now the Danish researchers have found this ghrelin antagonist to be a full inverse agonist with an EC50 = 5.2 nM.

Also, Broglio and coworkers recently reported des-octanoyl ghrelin peptide did not possess endocrine activity in animal models.  However, Des-n-Octanoyl-[Ser3]-Ghrelin (Human) was shown to be as effective as ghrelin in exhibiting antiproliferative effects on tumor cell lines in in vitro studies.

These new products, non-acylated ghrelin and ghrelin antagonist, should serve as a valuable research tool to aid diabetes and obesity research efforts.  In addition, ghrelin active and inactive (negative control) fragments, are available from Peptides International.

 

CODE

New Ghrelin Products
Ghrelin PDF Brochure

QTY

USD

PGH-3902-PI
NEW!

[Trp3, Arg5]-Ghrelin (1-5)
 H-Gly-Ser-Trp-Phe-Arg-OH
GSWFR
(M.W. 651.73) C31H41N9O7
 Growth-Hormone Secretagogue (GHS) Receptor Agonist / Stimulates Food-Intake

K. Ohinata, K. Kobayashi, M. Yoshikawa, Peptides, 27, 1632 (2006).

1 mg
5 mg

 

35
95

PGH-3680-PI
NEW!

[Dap3]-Ghrelin (Rat)
H-Gly-Ser-Dap(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg-OH
(M.W. 3313.88)  C147H246N46O41
Growth-Hormone Releasing Peptide
Ser3 from parent peptide PGH-4373-s replaced with 2,3-diaminopropionic acid (Dap) to enhance stability.

M.A. Bednarek, S.D. Feighner, S.-S. Pong, K.K. McKee, D.L. Hreniuk, M.V. Silva, V.A. Warren, A.D. Howard, L.H.Y. Van der Ploeg, and J.V. Heck, J. Med. Chem., 43, 4370-4376 (2000).

0.5 mg

 

165
 

PGH-3681-PI
NEW!

[Dap3]-Ghrelin (Human, Rat, 1-5)
H-Gly-Ser-Dap(n-Octanoyl)-Phe-Leu-NH2
(M.W. 633.79) C31H51N7O7
Growth-Hormone Releasing Peptide
Ghrelin Analog Active Fragment
Ser3 from parent peptide PGH-4373-s replaced with 2,3-diaminopropionic acid (Dap) to enhance stability.

M.A. Bednarek, S.D. Feighner, S.-S. Pong, K.K. McKee, D.L. Hreniuk, M.V. Silva, V.A. Warren, A.D. Howard, L.H.Y. Van der Ploeg, and J.V. Heck, J. Med. Chem., 43, 4370-4376 (2000).

1 mg
5 mg

 

55
190

 

PGH-3652-PI
 

 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2
(M.W. 1516.87) C79H109N19O12
Ghrelin Antagonist / Potent Ghrelin Inverse Agonist
Bombesin Antagonist
P.J. Woll and E. Rozengurt, Proc. Natl. Acad. Sci. USA, 85, 1859 (1988). (Original: Bombesin Antagonist)
B. Holst, A. Cygankiewicz, T.H. Jensen, M. Ankersen, and T.W. Schwartz, Mol. Endocrin., 17, 2201 (2003). (Original: Ghrelin Antagonist)
B. Holst, M. Lang, E. Brandt, A. Bach, A. Howard, T.M. Frimurer, A Beck-Sickinger, and T.W. Schwartz, Mol. Pharmacol., online as doi:10.1124/mol.106.024422 (2006).

1 mg

55

PGH-3656-PI
 

 H-His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH2
[D-Lys3]-Growth Hormone Releasing Peptide-6 (GHRP-6)
(M.W. 930.12) C49H63N13O6
Ghrelin Antagonist
L. Pinilla, M.L. Barreiro, M. Tena-Sempere, and E. Aguilar, Neuroendocrinology, 77, 83 (2003).

1 mg
5 mg

25
49

PGH-3694-PI
NEW!

H-His-D-Trp-Ala-Trp-D-Phe-Lys-NH2
 [His1,Lys6]-Growth Hormone Releasing Peptide (GHRP-6)
(M.W. 873.04) C46H56N12O6
 Growth Hormone Releasing Peptide 6

1 mg
5 mg

25
65

PGH-3653-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Human)
Non-Acylated Ghrelin (Human)
Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-
Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-
Lys-Leu-Gln-Pro-Arg
(M.W. 3244.74) C141H235N47O41
Inactive Ghrelin
F. Broglio, A. Benso, C Gottero, F. Prodam, C. Gauna, L. Filtri, E. Arvat, A.J. van der Lely, R. Deghengi, and E. Ghigo, J. Endocrin. Invest., 26, 192 (2003).

0.5 mg

145

PGH-3654-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Rat)
Non-Acylated Ghrelin (Rat)
Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-
Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-
Pro-Ala-Lys-Leu-Gln-Pro-Arg
(M.W. 3188.67) C139H231N45O41
Inactive Ghrelin

0.5 mg

145

CODE

Active Fragments of Ghrelin

QTY

USD

PGH-3625-PI

 Ghrelin (Human, 1-18)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-
Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-NH2

1 mg
5 mg

95
285

PGH-3626-PI

 Ghrelin (Human, 1-14)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-
Glu-His-Gln-Arg-Val-Gln-Gln-OH

1 mg
5 mg

75
225

PGH-3627-PI

 Ghrelin (Human, Rat, 1-10)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-
Glu-His-Gln-NH2

1 mg
5 mg

60
180

PGH-3628-PI

 Ghrelin (Human, Rat, 1-5)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-NH2

1 mg
5 mg

45
135

Negative Control Ghrelin Fragments
Inactive Ghrelin without n-Octanoyl on Serine3

PGH-3645-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Human, 1-18)
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-
Val-Gln-Gln-Arg-Lys-Glu-Ser-NH2
Negative Control for Ghrelin (Human, 1-18)

1 mg
5 mg

65
195

PGH-3646-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Human, 1-14)
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-
Val-Gln-Gln-OH
Negative Control for Ghrelin (Human, 1-14)

1 mg
5 mg

55
155

PGH-3647-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Human, Rat, 1-10)
H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-NH2
Negative Control for Ghrelin (Human, 1-10)

1 mg
5 mg

45
125

PGH-3648-PI
 

 Des-n-Octanoyl-[Ser3]-Ghrelin (Human, Rat, 1-5)
H-Gly-Ser-Ser-Phe-Leu-NH2
Negative Control for Ghrelin (Human, 1-5)

1 mg
5 mg

35
95

Ghrelin and Related Products Available from the Peptide Institute
PGH-4372-s Ghrelin (Human)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-
Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-
Lys-Leu-Gln-Pro-Arg
(M.W. 3370.9) C149H249N47O42
Endogenous Growth-Hormone Releasing Peptide
with Novel Regulatory Mechanism
1) M. Kojima, H. Hosoda, Y. Date, M. Nakazato, H. Matsuo, and K. Kangawa,
Nature, 402, 656 (1999). (Original)
•This compound is distributed through the Peptide Institute under
license agreement with Dr. Kangawa.		 0.1 mg vial 235
PGH-4373-s Ghrelin (Rat)
Gly-Ser-Ser(n-Octanoyl)-Phe-Leu-Ser-Pro-Glu-His-Gln-
Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-
Lys-Leu-Gln-Pro-Arg
(M.W. 3314.8) C147H245N45O42
Endogenous Growth-Hormone Releasing Peptide
with Novel Regulatory Mechanism
1) M. Kojima, H. Hosoda, Y. Date, M. Nakazato, H. Matsuo, and K. Kangawa,
Nature, 402, 656 (1999). (Original)
•This compound is distributed through the Peptide Institute under
license agreement with Dr. Kangawa.		 0.1 mg vial 235
PGR-4127-s Growth Hormone Releasing Factor [GRF] (Human) 0.1 mg vial 125
For additional product information or bulk quotations please inquire.

Ghrelin Peptides

Human growth hormone (hGH) is secreted  throughout life.  hGH is implicated as an important factor in the aging process due to its significant decrease over the life cycle, and its involvement in many processes, such as fat, protein, carbohydrate, muscle, and bone metabolism. Therefore, hGH has been hailed by the popular press as the fountain of youth.

ghrelinhuman.jpg (23822 bytes)

Small synthetic molecules called growth-hormone secretagogues (GHSs) stimulate the release of growth hormone (GH) from the pituitary through human secretagogue receptor 1a (hGHSR1a) (1, 2, 3). The endogenous ligand for this receptor  was identified in 1999 as ghrelin (4). Kojima and co-workers reported ghrelin to be an octanoylated, 28-residue peptide with the n-octanoyl group at Ser3, the first observed to date. Ghrelin stimulates GH-release from rat primary cultured pituitary cells in a dose-dependent manner (EC50 = 2.1 nM) and it induces an increase of intracellular Ca2+ in GHS-R-expressing cells with EC50 of 2.5 nM (4). Rat and human peptide sequences are identical except for the amino acid substitutions at positions 11 and 12.

Although ghrelin and the known hypothalamic peptide, growth-hormone releasing factor, stimulate GH-release, they differ both in GH secretion mechanism and in a structural aspect, the octanoyl group attached on the side chain of Ser3 in ghrelin is essential for expressing activity. This octanoylated posttranslational modification is the first of this type observed to date. The major ghrelin-producing tissue is the stomach and ghrelin immunoreactivity is found in healthy human blood.  Recently Merck scientists, Bednarek and coworkers, report that only the first 5 residues are necessary to maintain the activity of endogenous ghrelin, but a large hydrophobic group on the Ser3 side chain is still required for activity (3). 

This peptide may constitute a new regulatory mechanism for GH-release. It is conceivable that ghrelin may have other functions in some tissues other than pituitary, because the GHS receptor is expressed in heart, lung, pancreas, intestine, and adipose tissue.

1. R.G. Smith, K. Cheng, W.R. Schoen, S.-S. Pong, G. Hickey, T. Jacks, B. Butler, W. W.-S. Chan, L.-Y. P. Chaung, F. Judith, J. Taylor, M. J. Wyvratt, and M.H. Fisher, Science, 260, 1640 (1993).
2. C.Y. Bowers, Cell. Mol. Life Sci., 54, 1316 (1998).
3. M.A. Bednarek, S.D. Feighner, S.-S. Pong, K.K. McKee, D.L. Hreniuk, M.V. Silva, V.A. Warren, A.D. Howard, L.H.Y. Van der Ploeg, and J.V. Heck, J. Med. Chem., 43, 4370-4376 (2000).
4. M. Kojima, H. Hosoda, Y. Date, M. Nakazato, H. Matsuo, and K. Kangawa, Nature, 402, 656 (1999). (Original)

 

 

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PO Box 24658
Louisville, Kentucky 40224 USA
Phone: 502-266-8787 or 800-777-4779
Fax: 502-267-1FAX (1329)
Email:  peptides@pepnet.com

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