Article
Biochemistry & Molecular Biology
Mariia M. Efremova, Anastasia I. Govdi, Valeria V. Frolova, Andrey M. Rumyantsev, Irina A. Balova
Summary: A series of new triazole derivatives were synthesized through Cu-catalyzed 1,3-dipolar cycloaddition and subsequent Suzuki-Miyaura cross-coupling reaction, which exhibit fluorescence properties with significant Stokes shift values. The photophysical behavior of the most promising triazoles in different solvents was also investigated.
Article
Biochemistry & Molecular Biology
Andrey A. Bakhtyukov, Kira V. Derkach, Viktor N. Sorokoumov, Anna M. Stepochkina, Irina V. Romanova, Irina Yu. Morina, Irina O. Zakharova, Liubov V. Bayunova, Alexander O. Shpakov
Summary: In males with type 2 diabetes mellitus, metformin and LH/hCG-R agonists can restore steroidogenesis and spermatogenesis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Medicine, Research & Experimental
K. Derkach, E. A. Fokina, A. A. Bakhtyukov, V. N. Sorokoumov, A. M. Stepochkina, I. O. Zakharova, A. O. Shpakov
Summary: The thieno[2,3-d]-pyrimidine derivative TPY1 can suppress the synthesis of thyroid hormones stimulated by TSH and reduce the levels of thyroid hormones in the blood. These findings suggest that TPY1 may serve as a prototype drug for the treatment of autoimmune hyperthyroidism.
BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
A. A. Bakhtyukov, K. V. Derkach, E. A. Fokina, V. N. Sorokoumov, I. O. Zakharova, L. V. Bayunova, A. O. Shpakov
Summary: A new compound TPY3m was found to stimulate thyroxine production and increase thyroid gene expression, showing potential corrective effects in subclinical hypothyroidism.
DOKLADY BIOCHEMISTRY AND BIOPHYSICS
(2022)
Meeting Abstract
Endocrinology & Metabolism
A. A. Bakhtyukov, K. V. Derkach, A. M. Stepochkina, V. N. Sorokoumov, L. V. Bayunova, I. A. Lebedev, A. O. Shpakov
METABOLISM-CLINICAL AND EXPERIMENTAL
(2022)
Article
Biochemistry & Molecular Biology
Anastasia Govdi, Polina Tokareva, Andrey M. Rumyantsev, Maxim S. Panov, Johannes Stellmacher, Ulrike Alexiev, Natalia A. Danilkina, Irina A. Balova
Summary: The Cu-catalyzed synthesis of a series of triazole-based push-pull chromophores with fluorescence properties was successful, with the fluorescence easily adjustable based on substituents, showing potential as fluorescent tags for biological labeling.
Article
Chemistry, Organic
Anastasia A. Babushkina, Vladimir N. Mikhaylov, Alexander S. Novikov, Viktor N. Sorokoumov, Maxim A. Gureev, Mariya A. Kryukova, Alexander O. Shpakov, Irina A. Balova
Summary: The Richter cyclization was employed to synthesize 6-halo-3-(hydroxymethyl)cinnolin-4(1H)-ones. X-ray analysis revealed the dimeric state of these compounds in their crystal form, where two molecules are connected by intermolecular double and bifurcated hydrogen bonds, explaining their low solubility. Theoretical study of the bifurcated hydrogen bonds responsible for dimerization was carried out using DFT calculations and topological analysis of electron density distribution based on Bader's theory.
CHEMISTRY OF HETEROCYCLIC COMPOUNDS
(2022)
Article
Biochemistry & Molecular Biology
A. A. Bakhtyukov, I. Yu Morina, K. Derkach, I. Romanova, V. N. Sorokoumov, A. O. Shpakov
Summary: In type 1 diabetes mellitus, the synthesis of testosterone is impaired, leading to androgen insufficiency and disorders of spermatogenesis. This study found that treatment with the allosteric LH/hCG receptor agonist TP03 enhanced the stimulating effect of hCG on blood testosterone levels and improved testicular sensitivity to gonadotropins in diabetic rats. Furthermore, TP03 pretreatment followed by hCG stimulation resulted in improved morphometric parameters of the seminiferous tubules compared to the groups that received TP03 or hCG alone.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Natalia A. Danilkina, Ekaterina A. Khmelevskaya, Anna G. Lyapunova, Alexander S. D'yachenko, Alexander S. Bunev, Rovshan E. Gasanov, Maxim A. Gureev, Irina A. Balova
Summary: The scope and limitations of the Nicholas-type cyclization for the synthesis of 10-membered benzothiophene-fused heterocyclic enediynes with different functionalities were investigated. Among the investigated conditions, cyclization via an arenesulfonamide functional group was found to be the most promising, yielding high overall yields. The acylated 4-aminobenzenesulfonamide nucleophilic group was found to be the most convenient for the synthesis of functionalized 10-membered enediynes bearing a clickable function. The synthesized cyclic enediynes exhibited moderate activity against lung carcinoma cells.
Article
Biochemistry & Molecular Biology
K. Derkach, V. N. Sorokoumov, A. A. Bakhtyukov, V. M. Bondareva, A. O. Shpakov
Summary: Obesity impairs the insulin and leptin pathways in the brain and peripheral tissues. This study showed that the transport of insulin and leptin across the blood-brain barrier is attenuated in obese rats, resulting in increased concentration ratios of these hormones in the blood and brain structures. Treatment with metformin and PI4 restored the levels of insulin and leptin in the brain structures and improved metabolic parameters. Bromocriptine and intranasal insulin treatment were less effective.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Aleksandra A. Vidyakina, Andrey A. Shtyrov, Mikhail N. Ryazantsev, Alexander F. Khlebnikov, Ilya E. Kolesnikov, Vladimir V. Sharoyko, Dar'ya Spiridonova, Irina A. Balova, Stefan Braese, Natalia A. Danilkina
Summary: Fluorescent isocoumarin-fused cycloalkynes have been developed, which react in SPAAC and give fluorescent triazoles regardless of the azide nature. The introduction of a pi-acceptor group at the C6 position of the isocoumarin ring converts the non-fluorescent cycloalkyne/triazole pair to its fluorescent counterpart. The design of the fluorescent cycloalkyne/triazole pairs is based on theoretical studies of the deactivation mechanism and electron density redistribution.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Kira V. V. Derkach, Maxim A. A. Gureev, Anastasia A. A. Babushkina, Vladimir N. N. Mikhaylov, Irina O. O. Zakharova, Andrey A. A. Bakhtyukov, Viktor N. N. Sorokoumov, Alexander S. S. Novikov, Mikhail Krasavin, Alexander O. O. Shpakov, Irina A. A. Balova
Summary: This article describes the identification of dual inhibitors of protein phosphotyrosine phosphatase 1B (PTP1B)/T-cell protein phosphotyrosine phosphatase (TC-PTP) based on the 3-(hydroxymethyl)-4-oxo-1,4-dihydrocinnoline scaffold. The compounds were evaluated for their effects on obesity-related parameters and gene expressions. The results indicate the potential of these compounds as dual inhibitors for the treatment of metabolic disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
A. A. Bakhtyukov, K. V. Derkach, E. A. Fokina, I. A. Lebedev, V. N. Sorokoumov, L. V. Bayunova, A. O. Shpakov
Summary: The study aimed to investigate the effect of TP03 on ovarian steroidogenesis. The results showed that TP03 effectively stimulated ovarian steroidogenesis, similar to hCG, but without reducing the activity of the hypothalamic-pituitary-gonadal axis. These findings suggest good prospects for TP03-based drugs as controlled ovulation induction drugs.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
E. A. Fokina, K. V. Derkach, A. A. Bakhtyukov, V. N. Sorokoumov, I. A. Lebedev, I. Yu. Morina, A. O. Shpakov
Summary: Human chorionic gonadotropin (hCG) and luteinizing hormone (LH) have limitations in their use due to side effects. An alternative, TP03, has been developed as an allosteric agonist of the LH/hCG receptor. TP03 has been shown to increase progesterone levels, induce ovulation, and stimulate ovarian steroidogenesis in rats without causing an increase in vascular endothelial growth factor expression. TP03 shows similar activity to hCG but with a milder effect.
DOKLADY BIOCHEMISTRY AND BIOPHYSICS
(2022)
Article
Biochemistry & Molecular Biology
A. M. Stepochkina, A. A. Bakhtyukov, K. Derkach, V. N. Sorokoumov, A. O. Shpakov
Summary: This study aimed to evaluate the steroidogenic effects of the allosteric LHR agonist TP03 in male rats and compare it with hCG. The results showed that TP03 stimulated testosterone production more effectively via intraperitoneal administration and had a persistent steroidogenic effect, while subcutaneous hCG administration was more effective but reduced LHR gene expression.
JOURNAL OF EVOLUTIONARY BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Chemistry, Organic
Geeta Devi Yadav, Pooja Chaudhary, Balaram Pani, Surendra Singh
Summary: Chiral transition metal complexes with privileged ligands are efficient catalysts for various asymmetric organic transformations. Transition metal complexes of C1-symmetric pyrrolidine-based ligands have been widely used in asymmetric organic reactions. However, a comprehensive review article on the transition metal complexes of chiral C1-symmetric pyrrolidine-based ligands derived from (L)-proline has not been published.
TETRAHEDRON LETTERS
(2024)
