?
Chemical elicitors of antibiotic biosynthesis in actinomycetes
Microorganisms. 2018. Vol. 6. P. 52.
Vladimir A. Korshun
Whole genome sequencing of actinomycetes has uncovered a new immense realm of microbial chemistry and biology. Most biosynthetic gene clusters present in genomes were found to remain “silent” under standard cultivation conditions. Some small molecules—chemical elicitors—can be used to induce the biosynthesis of antibiotics in actinobacteria and to expand the chemical diversity of secondary metabolites. Here, we outline a brief account of the basic principles of the search for regulators of this type and their application.
В.А. Коршун, Russian Chemical Bulletin 2019 Vol. 68 No. 5 P. 955-966
New biologically active substances isolated from natural sources provide valuable information
on structural motifs that are important for a specifi c type of activity and can also be used
as drugs or serve as raw materials for chemical modifi cation in order to develop new pharmaceuticals.
This review considers natural antibiotics combining two pharmacophores in their
structure: a redox-active ...
Added: November 8, 2019
Lohan S., Mandal D., Choi W. et al., Journal of Medicinal Chemistry 2022 Vol. 65 No. 1 P. 665-687
We report the synthesis and antibacterial activities of a series of amphiphilic membrane-active peptides composed, in part, of various non-genetically coded hydrophobic amino acids. Lead cyclic peptides, 8C and 9C, showed broad-spectrum activity against drug-resistant Gram-positive (MIC=1.5-6.2 µg/mL) and Gram-negative (MIC=12.5-25 µg/mL) bacteria. Cytotoxicity study showed the predominant lethal action of the peptides against bacteria ...
Added: February 1, 2022
Krasavin M., Lukin A., Sukhanov I. et al., Biomolecules 2022 Vol. 12 No. 11 Article 1650
A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenethylamine (PEA) or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely related hits displaying EC50 values in the upper submicromolar range. Extensive analog synthesis and testing ...
Added: February 8, 2024
М. : Энциклопедия, Инфра-М, 2017
The New Russian Encyclopedia is a fundamental reference publication in 18 volumes that characterizes nature, population, economy, history, science, art, technology and other important aspects. Contains about 60,000 articles, about 30,000 biographies, about 15,000 color illustrations, maps, charts, diagrams, tables. Leaves since 2003. ...
Added: October 29, 2018
Mikhaylov A. A., Ikonnikova V., Solyev P., Natural Product Reports 2021 Vol. 38 P. 1506-1517
The unusual framework of the middle C-ring, “broken” as a result of biotransformations and oxidations in vivo and bearing an sp3-C connection, is of interest for biosynthetic investigations. The reported 39 natural compounds (55 including stereoisomers) have been analyzed and arranged into three structural groups. The biosynthetic origin of all these compounds has been thoroughly reviewed and ...
Added: February 2, 2021
Terekhov S., Mokrushina Y., Nazarov A. et al., Science advances 2020 Vol. 6 No. 26 P. eaaz9861
Microbial communities are self-controlled by repertoires of lethal agents, the antibiotics. In their turn, these antibiotics are regulated by bioscavengers that are selected in the course of evolution. Kinase-mediated phosphorylation represents one of the general strategies for the emergence of antibiotic resistance. A new subfamily of AmiN-like kinases, isolated from the Siberian bear microbiome, inactivates ...
Added: October 29, 2020
Abramov V., Abramova A., Bayazitov V. et al., Processes 2022 Vol. 10 No. 10 Article 2063
Although water contamination with drug residues is a threat to public health, there are currently barely any effective methods of purifying water from pharmaceutical substances. In this study, continuous-flow sonoplasma treatment was used for the complete degradation of tetracycline and ciprofloxacin in polluted municipal water. The addition of CeO2 nanoparticles as catalysts significantly increased the degradation ...
Added: October 23, 2022
Galenko E., Galenko A., Novikov M. et al., ChemistrySelect 2017 Vol. 2 No. 25 P. 7508-7513
New β‐diazopyrrole and β‐triazenylpyrrole derivatives were synthesized from isoxazoles and pyridinium salts in two and three steps, respectively. The apoptotic/necrotic difference for these compounds was estimated on THP‐1 cell line. The most effective of the panel is methyl 3‐diazo‐2‐(2,4‐dimethylphenyl)‐4‐phenyl‐3H‐pyrrole‐5‐carboxylate which demonstrated cytotoxic activity from the lowest concentration of 3.3 μM with a steep rise of the ...
Added: June 25, 2019
Tharra P., Mikhaylov Andrey A., Švejkar J. et al., Angewandte Chemie - International Edition 2022 Vol. 61 No. 17 Article e202116520
Added: February 17, 2022
Vladimir A. Korshun, RSC advances 2019 Vol. 9 No. 45 P. 26014-26023
The propargylamide of N3-Pom-protected 5-(perylen-3-ylethynyl)uracil acetic acid, a universal precursor, was used in a CuAAC click reaction for the synthesis of several derivatives, including three ramified molecules with high activities against tick-borne encephalitis virus (TBEV). Pentaerythritol-based polyazides were used for the assembly of molecules containing 2/4 antiviral 5-(perylen-3-ylethynyl) uracil scaffolds, the first examples of polyvalent perylene antivirals. Cluster compounds ...
Added: November 8, 2019
Goncharov N., Belinskaia D., Shmurak V. et al., Molecules 2017 Vol. 22 No. 7 P. 1-27
The albumin molecule, in contrast to many other plasma proteins, is not covered with a carbohydrate moiety and can bind and transport various molecules of endogenous and exogenous origin. The enzymatic activity of albumin, the existence of which many scientists perceive skeptically, is much less studied. In toxicology, understanding the mechanistic interactions of organophosphates with ...
Added: June 25, 2019
Sapegin A., Rogacheva E., Kraeva L. et al., Biomedicines 2022 Vol. 10 No. 9 Article 2203
A chemically diverse set of 13 5-nitrofuran-tagged heterocyclic compounds has been prepared via the Groebke–Blackburn–Bienaymé multicomponent reaction. The testing of these compounds against the so-called ESKAPE panel of pathogens identified an apparent lead compound—N-cyclohexyl-2-(5-nitrofuran-2-yl)imidazo[1,2-a]pyridine-3-amine (4a)—which showed an excellent profile against Enterobacter cloacae, Staphylococcus aureus, Klebsiella pneumoniae, and Enterococcus faecalis (MIC 0.25, 0.06, 0.25 and 0.25 µg/mL, respectively). Its antibacterial ...
Added: February 8, 2024
М. : Энциклопедия, Инфра-М, 2017
The New Russian Encyclopedia is a fundamental reference publication in 18 volumes that characterizes nature, population, economy, history, science, art, technology and other important aspects. Contains about 60,000 articles, about 30,000 biographies, about 15,000 color illustrations, maps, charts, diagrams, tables. Leaves since 2003. ...
Added: October 31, 2018
Автономная некоммерческая организация «Национальный научно-образовательный центр «Большая российская энциклопедия» (АНО БРЭ), 2022
Основными задачами Портала являются создание и поддержание в актуальном состоянии электронной национальной базы знаний на русском языке, консолидирующей сведения об окружающем мире, предназначенной для широкого круга пользователей, а также популяризация науки, трансфер научных результатов в образование, культура использования данных и научные междисциплинарные коммуникации. Важнейшая социальная функция Портала — доступность правдивой научной информации и формирование доверия пользователя к ней.
Контент портала
Основу контента составляют дополненные и расширенные статьи «Большой ...
Added: September 12, 2022
Lukashina N., Kartysheva E., Spjuth O. et al., Journal of Cheminformatics 2022 Vol. 14 Article 49
Polypharmacy refers to the administration of multiple drugs on a daily basis. It has demonstrated effectiveness in treating many complex diseases , but it has a higher risk of adverse drug reactions. Hence, the prediction of polypharmacy side effects is an essential step in drug testing, especially for new drugs. This paper shows that the ...
Added: October 11, 2022
Krivovicheva V., Bubyrev A., Kalinin S. et al., ChemMedChem 2023 Vol. 18 No. 10 Article e202200607
A newly introduced diazo reagent, 1-diazo-N,N-bis(4-methoxybenzyl)methanesulfonamide, enables access to a range of azole-based primary sulfonamides via [3+2] cycloaddition followed by protecting group removal. Such compounds are representative of the sulfonamide chemical space highly relevant but hitherto not investigated in the context of inhibition of therapeutically relevant isoforms of carbonic anhydrase enzyme. Using this reagent, three ...
Added: January 26, 2024
Rogacheva E., Kraeva L., Lukin A. et al., Molecules 2023 Vol. 28 No. 18 Article 6491
A series of eight 5-nitrofuran-tagged oxazolyl tetrahydropyrazolopyridines (THPPs) has been prepared in six stages with excellent regioselectivity. The testing of these compounds against pathogens of the ESKAPE panel showed a good activity of lead compound 1-(2-methoxyethyl)-5-(5-nitro-2-furoyl)-3-(1,3-oxazol-5-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c] pyridine (13g), which is superior to nitrofurantoin. These results confirmed the benefit of combining a THPP scaffold with a ...
Added: January 26, 2024
Derkach K., Maxim A. Gureev, Babushkina A. et al., International Journal of Molecular Sciences 2023 Vol. 24 No. 5 Article 4498
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 have been identified. Their dual affinity to both enzymes has been thoroughly corroborated by in silico modeling experiments. The compounds have been profiled in vivo for their effects on body weight and food intake in obese rats. Likewise, ...
Added: February 1, 2024
Babich O., Larina V., Krol O. et al., Pharmaceutics 2023 Vol. 15 No. 2 Article 616
Tanacetum vulgare is an herbaceous plant widely used in folk medicine. It is rich in phenolic acids and flavonoids, which have pharmacological and medicinal properties, such as anthelmintic, antispasmodic, tonic, antidiabetic, diuretic, and antihypertensive. This study aimed to confirm the presence of biologically active substances in Tanacetum vulgare and to determine the pharmacological spectrum of ...
Added: February 1, 2024
Panina I., Balandin S., Tsarev A. et al., International Journal of Molecular Sciences 2023 Vol. 24 No. 2 P. 1
To date, a number of lantibiotics have been shown to use lipid II — a highly conserved peptidoglycan precursor in the cytoplasmic membrane of bacteria — as their molecular target. The α-component (Lchα) of the two-component lantibiotic lichenicidin (Lchα), previously isolated from the Bacillus licheniformis VK21 strain, seems to contain two putative lipid II binding ...
Added: February 21, 2023
Springer, 2019
This unique work compiles the latest knowledge around veterinary nutraceuticals, commonly referred to as dietary supplements, from ingredients to final products in a single source. More than sixty chapters organized in seven sections collate all related aspects of nutraceutical research in animal health and disease, among them many novel topics: common nutraceutical ingredients (Section-I), prebiotics, ...
Added: June 25, 2019
Olloqui-Sariego J. L., Zakharova G., Poloznikov A. et al., Electrochimica Acta 2020 Vol. 351 P. 136465
A major challenge in the design of electrochemical biodevices is to achieve fast rates of electron exchange between proteins and electrodes. In this work, we show that a significant increase in the direct electron transfer rate between a graphite electrode and Tobacco Peroxidase takes place when a surface exposed leucine, located in the vicinity of ...
Added: July 22, 2020
Vladimir A. Korshun, Prokhorenko I., Tyurin A. et al., MedChemComm 2018 Vol. 9 No. 4 P. 667-675
The study of an archived sample of crystallomycin complex using HPLC, ESI HRMS, and 2D NMR showed
that two major components of the antibiotic, compounds 1 and 2, are lipopeptides having the same peptide
core, Asp1-cycloIJDab2-Pip3-MeAsp4-Asp5-Gly6-Asp7-Gly8-Dab9-Val10-Pro11-), N-acylated either
with Δ3-iso-tetradecenoyl or Δ3-anteiso-pentadecenoyl that are identical to aspartocins C and B, respectively.
According to the 2D NMR study, compound 2 ...
Added: November 8, 2019
В. А. Коршун, Prokhorenko I., Биоорганическая химия 2017 Т. 43 № 4 С. 377-387
The synthesis of phosphoramidite reagents and solid-phase supports for the preparation of oligonucleotides
labeled on various locations within the oligonucleotide chain (including multiple modification) with biotin,
lipoic acid, amino group and terminal acetylene, is described. The efficiency of the reagents and solid supports
is confirmed by the synthesis of corresponding modified oligonucleotides. ...
Added: November 6, 2019