Short peptide with an inhibitory activity on the NMDA/Gly-induced currents

Karlov, Dmitry S.; Barygin, Oleg I.; Dron, Mikhail Y.; Palyulin, Vladimir A.; Grigoriev, V. V.; Fedorov, Maxim V.

doi:10.1080/1062936x.2019.1653965

Cited by 2 publications

(3 citation statements)

References 29 publications

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“…5) which have high affinity for sigma receptors and a peptide-based ifenprodil analog. 24 Compound 6 bearing a biaryl moiety was published as an NMDA receptor antagonist which competes with ifenprodil and has an unusual binding mode. 15 At the same time, the docking pose of a biphenyl-containing compound 10a (identified during the virtual screening of the in-house virtual library containing about 30 000 compounds, Fig.…”

Section: Introductionmentioning

confidence: 99%

Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity

et al. 2022

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Section: Introductionmentioning

confidence: 99%

Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity

et al. 2022

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“…In addition, the NMDA receptor is deemed to be one of the most prospective targets for treating depression, which are activated by the simultaneous action of glutamate and glycine. It was reported that a dipeptide d -Phe- l -Tyr showed a strong antidepressive activity by inhibiting the NMDA receptor . As shown in Figure E, the pretreatment of YPVEPF significantly downregulated the protein expression of the NMDA/Glu receptor in comparison with the model group.…”

Section: Resultsmentioning

confidence: 71%

“…It was reported that a dipeptide D-Phe-L-Tyr showed a strong antidepressive activity by inhibiting the NMDA receptor. 44 As shown in Figure 4E, the pretreatment of YPVEPF significantly downregulated the protein expression of the NMDA/Glu receptor in comparison with the model group. Therefore, YPVEPF could ameliorate stress-induced impairment of the neuroendocrine function and cause sleep-enhancing effects by regulating the GABA-Glu metabolic pathway.…”

Section: Effects Of Ypvepf On Related Neurotransmitter Receptors In S...mentioning

confidence: 79%

Potential Mechanisms of Casein Hexapeptide YPVEPF on Stress-Induced Anxiety and Insomnia Mice and Its Molecular Effects and Key Active Structure

Qian,

Zheng,

Huang

et al. 2024

J. Agric. Food Chem.

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The hexapeptide YPVEPF with strong sleep-enhancing effects could be detected in rat brain after a single oral administration as we previously proved. In this study, the mechanism and molecular effects of YPVEPF in the targeted stress-induced anxiety mice were first investigated, and its key active structure was further explored. The results showed that YPVEPF could significantly prolong sleep duration and improve the anxiety indexes, including prolonging the time spent in the open arms and in the center. Meanwhile, YPVEPF showed strong sleep-enhancing effects by significantly increasing the level of the GABA/Glu ratio, 5-HT, and dopamine in brain and serum and regulating the anabolism of multiple targets, but the effects could be blocked by bicuculline and WAY100135. Moreover, the molecular simulation results showed that YPVEPF could stably bind to the vital GABAA and 5-HT1A receptors due to the vital structure of Tyr-Pro-Xaa-Xaa-Pro-, and the electrostatic and van der Waals energy played dominant roles in stabilizing the conformation. Therefore, YPVEPF displayed sleep-enhancing and anxiolytic effects by regulating the GABA-Glu metabolic pathway and serotoninergic system depending on distinctive self-folding structures with Tyr and two Pro repeats.

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Short peptide with an inhibitory activity on the NMDA/Gly-induced currents

Cited by 2 publications

References 29 publications

Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity

Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity

Potential Mechanisms of Casein Hexapeptide YPVEPF on Stress-Induced Anxiety and Insomnia Mice and Its Molecular Effects and Key Active Structure

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