Molecular Mechanism Underlying the Action of Substituted Pro-Gly Dipeptide Noopept.

Vakhitova YV, Sadovnikov SV, Borisevich SS, Ostrovskaya RU, A Gudasheva T, Seredenin SB

Acta naturae1 Jan 2016Cited by 4 (Europe PMC)

PMID27099787PMCIDPMC4837574DOI10.32607/20758251-2016-8-1-82-89PepBankPUB-27099787

Summary

This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells transiently transfected with luciferase reporter constructs containing sequences for CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, HSF1, and HIF-1. Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1. Noopept provoked an additional increase in the DNA-binding activity of HIF-1 when applied in conditions of CoCl2-induced HIF- 1 stabilization. The degree of this HIF-positive effect of Noopept was shown to be concentration-dependent. Piracetam (1 mM) failed to affect significantly any of the TF under study. The results of molecular docking showed that Noopept (L-isomer), as well as its metabolite, L-isomer of N-phenyl-acetylprolyl, unlike its pharmacologically ineffective D-isomer, is able to bind to the active site of prolyl hydroxylase 2. Taking into account the important role of the genes activated by HIF-1 in the formation of an adaptive response to hypoxia, data on the ability of Noopept to provoke a selective increase in the DNA-binding activity of HIF-1 explain the wide spectrum of neurochemical and pharmacological effects of Noopept revealed before. The obtained data allow one to propose the HIF-positive effect as the primary mechanism of the activity of this Pro-Gly-containing dipeptide.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study12

11 results from studies that gave the peptide. No result from this study comes from people.

01LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept increased HIF-1 DNA-binding activity.
In plain wordsIn cells, Noopept increased HIF-1 DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
IncreaseHIF-1 DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978701
02LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect CREB DNA-binding activity.
In plain wordsIn cells, Noopept did not change CREB DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeCREB DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978702
03LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect NFAT DNA-binding activity.
In plain wordsIn cells, Noopept did not change NFAT DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeNFAT DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978703
04LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect NF-κB DNA-binding activity.
In plain wordsIn cells, Noopept did not change NF-κB DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeNF-κB DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978704
05LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect p53 DNA-binding activity.
In plain wordsIn cells, Noopept did not change p53 DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changep53 DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978705
06LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect STAT1 DNA-binding activity.
In plain wordsIn cells, Noopept did not change STAT1 DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeSTAT1 DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978706
07LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect GAS DNA-binding activity.
In plain wordsIn cells, Noopept did not change GAS DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeGAS DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978707
08LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect VDR DNA-binding activity.
In plain wordsIn cells, Noopept did not change VDR DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeVDR DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978708
09LabIn vitro (cells)Mechanism
In HEK293 cells, Noopept did not affect HSF1 DNA-binding activity.
In plain wordsIn cells, Noopept did not change HSF1 DNA-binding activity.
Peptide
Noopept (omberacetam)
Outcome
No significant changeHSF1 DNA-binding activity
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
10 μMAs given in this study.
Source sentences
Summary
Noopept (10 μM) was shown to increase the DNA-binding activity of HIF-1 only, while lacking the ability to affect that of CREB, NFAT, NF-κB, p53, STAT1, GAS, VDR, and HSF1.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978709
10LabIn vitro (cells)Mechanism
In HEK293 cells with CoCl2-stabilized HIF-1, Noopept further increased HIF-1 DNA-binding activity.
In plain wordsIn cells with CoCl2-stabilized HIF-1, Noopept increased HIF-1 DNA-binding activity further than stabilization alone.
Peptide
Noopept (omberacetam)
Outcome
IncreaseHIF-1 activity under CoCl2 stabilization
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Comparator
CoCl2-induced HIF-1 stabilization without Noopept
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
Noopept provoked an additional increase in the DNA-binding activity of HIF-1 when applied in conditions of CoCl2-induced HIF- 1 stabilization.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978710
11LabIn vitro (cells)Mechanism
In HEK293 cells, the HIF-positive effect of Noopept depended on concentration.
In plain wordsIn cells, the HIF-positive effect of Noopept depended on concentration.
Peptide
Noopept (omberacetam)
Outcome
Direction not reportedHIF-1 concentration dependence
Study
n: not reported in source
HEK293 cells with transcription-factor luciferase reporters
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
The degree of this HIF-positive effect of Noopept was shown to be concentration-dependent.
1 context sentence(design, population, supporting numbers)
Summary · context
This study was performed in order to reveal the effect of Noopept (ethyl ester of N-phenylacetyl-Lprolylglycine, GVS-111) on the DNA-binding activity of transcriptional factors (TF) in HEK293 cells
Show in the study text Report a problemFND-2709978711

Studies that did not test the peptide alone1

In this study, Noopept (omberacetam) 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 Noopept (omberacetam).

12Computer modelNot a test of Noopept (omberacetam) aloneIn silicoMechanism
Molecular docking predicted prolyl hydroxylase 2 active-site binding by Noopept L-isomer and its L-isomer metabolite, unlike the ineffective D-isomer.
In plain wordsComputer modeling predicted that Noopept L-isomer and its L-isomer metabolite could bind prolyl hydroxylase 2, unlike the ineffective D-isomer.
Peptide
Noopept (omberacetam)
Outcome
Not applicableProlyl hydroxylase 2 binding
Study
n: not reported in source
Molecular docking
Comparator
Pharmacologically ineffective D-isomer
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
The results of molecular docking showed that Noopept (L-isomer), as well as its metabolite, L-isomer of N-phenyl-acetylprolyl, unlike its pharmacologically ineffective D-isomer, is able to bind to the active site of prolyl hydroxylase 2.
In this study, Noopept (omberacetam) 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 Noopept (omberacetam).
Show in the study text Report a problemFND-2709978712

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
21 Oct 2026, 15:58 UTC
Study results updated
Version 1
21 Oct 2026, 12:50 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

Keywords

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