A novel dimeric dipeptide mimetic of the BDNF selectively activates the MAPK-Erk signaling pathway

On the basis of the structure of beta-turn of loop 2 of brain-derived neurotrophic factor (BDNF), its new dimeric dipeptide mimetic bis -( N -hexanoyl- L -seryl- L -lysine) hexamethylenediamide (GTS-201) was created. It activated TrkB and Erk, did not activate Akt, and exhibited neuroprotective acti...

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Bibliographic Details
Published in:Doklady. Biochemistry and biophysics 2017-09, Vol.476 (1), p.291-295
Main Authors: Gudasheva, T. A., Tarasiuk, A. V., Sazonova, N. M., Povarnina, P. Yu, Antipova, T. A., Seredenin, S. B.
Format: Article
Language:English
Subjects:
AKT protein
Animals
Biochemistry
Biological and Medical Physics
Biomedical and Life Sciences
Biophysics
Brain-derived neurotrophic factor
Brain-Derived Neurotrophic Factor - chemistry
Cell Line
Dimerization
Dipeptides - chemistry
Extracellular signal-regulated kinase
Extracellular Signal-Regulated MAP Kinases - metabolism
Life Sciences
Lysine
MAP kinase
MAP Kinase Kinase Kinase 5 - drug effects
Mice
Molecular Biology
Neuroprotection
Neuroprotective Agents - chemistry
Neuroprotective Agents - pharmacology
Peptides
Peptidomimetics - chemistry
Peptidomimetics - pharmacology
Receptor, trkB - metabolism
Signal transduction
Signaling
TrkB receptors
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Summary:On the basis of the structure of beta-turn of loop 2 of brain-derived neurotrophic factor (BDNF), its new dimeric dipeptide mimetic bis -( N -hexanoyl- L -seryl- L -lysine) hexamethylenediamide (GTS-201) was created. It activated TrkB and Erk, did not activate Akt, and exhibited neuroprotective activity in vitro at concentrations of 10 –5 –10 –8 M. Unlike the mimetics that activate Erk and Akt, GTS-201 did not exhibit antidepressant properties. For the manifestation of the antidepressant activity of BDNF mimetics, the activation of its both major signaling pathways is required.
ISSN:1607-6729
1608-3091
DOI:10.1134/S1607672917050027