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Antidiabetic Effect of a New Original NT-3 Dipeptide Mimetic

Doklady Biochemistry and Biophysics, 2023
It was previously established that the original dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-monosuccinyl-L-asparaginyl-L-asparagine) (GTS-301), has a pronounced neuroprotective effect in vitro at concentrations of 10–5–10–12 М.
S S, Yagubova   +4 more
exaly   +3 more sources

Antiangiogenic Effects of Nerve Growth Factor Loop 4 Monomeric Dipeptide Mimetic

Bulletin of Experimental Biology and Medicine, 2017
The effects of GK-1, a monomeric dipeptide mimetic of nerve growth factor (NGF) loop 4, on angiogenesis were studied in vitro and in vivo. Experiments on human umbilical vein endothelial cells HUVEC showed that the test compound did not affect tubulogenesis (initial stage of angiogenesis) and prevented realization of the angiogenic effect of NGF and ...
Sergei V Nikolaev, Irina A Miroshkina
exaly   +3 more sources

An Achiral Dipeptide Mimetic That Promotes .beta.-Hairpin Formation

Journal of the American Chemical Society, 1995
Robb R. Gardner   +2 more
exaly   +2 more sources

Synthesis of constrained bicyclic dipeptide mimetics

Tetrahedron Letters, 1997
Abstract An efficient synthesis of constrained bicyclic peptidomimetics of (R)-Phe-Pro dipeptide is described. Such mimetics may provide an opportunity to develop inhibitors of thrombin possessing the desired pharmacological features.
M.Arshad Siddiqui   +7 more
openaire   +1 more source

Conformational analysis of dipeptide mimetics

Biopolymers, 1997
A compendium of compounds designed as dipeptide mimetics was collected from the literature. Conformational space available to these molecules was evaluated to obtain distance and torsion angle parameters to aid in selection of mimetics for specific target peptides or to explore diversity strategies.
Paul Gillespie   +2 more
openaire   +1 more source

The design of polar β-turn dipeptide mimetics

Bioorganic & Medicinal Chemistry Letters, 1995
Abstract The design and synthesis of conformationally constrained, non-peptide templates (3-substituted pyrrolidines) which allow the incorporation of two adjacent amino acid side-chains in an orientation similar to that found in the i+1 and i+1 positions of a β-turn are reported.
David C. Horwell   +3 more
openaire   +1 more source

Bradykinin antagonists modified with dipeptide mimetic β-turn inducers

Bioorganic & Medicinal Chemistry Letters, 2006
Bradykinin (BK) is involved in a wide variety of pathophysiological processes. Potent BK peptide antagonists can be developed introducing constrained unnatural amino acids, necessary to force the secondary structure of the molecule. In this paper, we report a structure-activity relationship study of two peptide analogues of the potent B2 antagonist HOE
M. C. ALCARO   +9 more
openaire   +6 more sources

Antidiabetic activity of a novel dipeptide mimetic of nerve growth factor

Doklady Biological Sciences, 2013
76 An antidiabetic effect of the new nerve growth fac tor (NGF) dipeptide mimetic GK 2 has been shown in rats with streptozotocininduced diabetes. The pep tide has a significant antihyperglycemic effect in the course of treatment: intraperitoneal injection at a dose of 0.5 mg/kg for two weeks before and four weeks after the toxin injection. GK 2 also
P Yu, Povarnina   +4 more
openaire   +2 more sources

Synthesis of an Optically Active, Bicyclic 2-Pyridone Dipeptide Mimetic

The Journal of Organic Chemistry, 2002
The eleven-step preparation of the bicyclic 2-pyridone dipeptide mimetic 1 [(3S)-6-(benzyloxycarbonylamino)-5-oxo-1,2,3,5-tetrahydroindolizine-3-carboxylic acid] in optically active form (60% ee) is described. Key steps in the synthesis of 1 include the osmium-catalyzed asymmetric dihydroxylation of olefin 13 [(6-but-3-enyl-2-methoxypyridin-3-yl ...
Peter S, Dragovich   +2 more
openaire   +2 more sources

Dipeptide Mimetics of Different NGF and BDNF Loops Activate PLC-γ1

Doklady Biochemistry and Biophysics, 2020
Previously, we designed and synthesized dipeptide mimetics of individual loops of the nerve growth factor (NGF) and the brain-derived neurotrophic factor (BDNF). It was shown that these mimetics activate the corresponding tyrosine kinase (Trk) receptors and have different patterns of activation of the PI3K/AKT and MAPK/ERK postreceptor signaling ...
T A, Gudasheva   +5 more
openaire   +2 more sources

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