Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues.

Feighner SD, Howard AD, Prendergast K, Palyha OC, Hreniuk DL, Nargund R, Underwood D, Tata JR, Dean DC, Tan CP, McKee KK, Woods JW, Patchett AA, Smith RG, Van der Ploeg LH

Molecular endocrinology (Baltimore, Md.)1 Jan 1998Cited by 89 (Europe PMC)

PMID9440817DOI10.1210/mend.12.1.0051PepBankPUB-09440817

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study4

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone4

In this study, MK-677 (ibutamoren) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking MK-677 (ibutamoren).

01LabNot a test of MK-677 (ibutamoren) aloneIn vitro (cells)Mechanism
In receptor mutagenesis studies, peptide and nonpeptide secretagogues, including MK-0677, shared a binding domain in transmembrane region 3.
In plain wordsIn lab tests, secretagogue classes including MK-0677 shared a receptor binding domain.
Peptide
MK-677 (ibutamoren)
Outcome
Not applicableShared transmembrane binding domain
Study
n: not reported in source
Mutated human GHS-R
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
All peptide and nonpeptide ligand classes shared a common binding domain in transmembrane (TM) region 3 of the GHS-R.
1 context sentence(design, population, supporting numbers)
Summary · context
Restoration of function for the E124Q mutant was achieved by a complementary change in the MK-0677 ligand through modification of its amine side-chain to the corresponding alcohol.
In this study, MK-677 (ibutamoren) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking MK-677 (ibutamoren).
Report a problemFND-0944081701
02LabNot a test of MK-677 (ibutamoren) aloneIn vitro (cells)Mechanism
In receptor mutagenesis studies, E124Q eliminated the counter-ion for the basic group shared by secretagogues and produced a nonfunctional receptor.
In plain wordsIn lab tests, a receptor mutation removed function at the binding site shared by secretagogues including MK-0677.
Peptide
MK-677 (ibutamoren)
Outcome
DecreaseReceptor function after E124Q mutation
Study
n: not reported in source
Mutated human GHS-R
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
This finding was based on TM-3 mutation E124Q, which eliminated the counter-ion to the shared basic N+ group of all GHSs and resulted in a nonfunctional receptor.
1 context sentence(design, population, supporting numbers)
Summary · context
Restoration of function for the E124Q mutant was achieved by a complementary change in the MK-0677 ligand through modification of its amine side-chain to the corresponding alcohol.
In this study, MK-677 (ibutamoren) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking MK-677 (ibutamoren).
Report a problemFND-0944081702
03LabNot a test of MK-677 (ibutamoren) aloneIn vitro (cells)Mechanism
In receptor mutagenesis studies, changing the MK-0677 amine side-chain to an alcohol restored function of the E124Q receptor mutant.
In plain wordsIn lab tests, a modified MK-0677 molecule restored function of a mutated receptor.
Peptide
MK-677 (ibutamoren)
Outcome
IncreaseRestoration of mutant receptor function
Study
n: not reported in source
Mutated human GHS-R
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
Restoration of function for the E124Q mutant was achieved by a complementary change in the MK-0677 ligand through modification of its amine side-chain to the corresponding alcohol.
In this study, MK-677 (ibutamoren) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking MK-677 (ibutamoren).
Report a problemFND-0944081703
04LabNot a test of MK-677 (ibutamoren) aloneIn vitro (cells)Mechanism
In receptor mutagenesis studies, contacts outside the shared domain showed specificity for peptide, benzolactam and spiroindolane secretagogue classes.
In plain wordsIn lab tests, other receptor contacts differed across secretagogue classes including the MK-0677 class.
Peptide
MK-677 (ibutamoren)
Outcome
Not applicableBinding contact specificity
Study
n: not reported in source
Mutated human GHS-R
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
Contacts in other TM domains [TM-2 (D99N), TM-5 (M213K, S117A), TM-6 (H280F), and extracellular loop 1 (C116A)] of the receptor revealed specificity for the different peptide, benzolactam, and spiroindolane GHSs.
1 context sentence(design, population, supporting numbers)
Summary · context
Restoration of function for the E124Q mutant was achieved by a complementary change in the MK-0677 ligand through modification of its amine side-chain to the corresponding alcohol.
In this study, MK-677 (ibutamoren) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking MK-677 (ibutamoren).
Report a problemFND-0944081704

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
14 Oct 2026, 05:02 UTC
Study results updated
Version 1
14 Oct 2026, 01:46 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

Journal Article

MeSH terms

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