Russian Journal of Bioorganic Chemistry最新文献

{"title":"Mannich Bases in Antiviral Drug Development: Synthetic Approaches and Biological Potential","authors":"Vaishnavi D. Magar,&nbsp;Neha V. Bhilare,&nbsp;Vinayak S. Marulkar,&nbsp;Vasant Y. Lokhande,&nbsp;Harinath N. More,&nbsp;Dileep Kumar","doi":"10.1134/S1068162025602794","DOIUrl":"10.1134/S1068162025602794","url":null,"abstract":"<p>The persistent global burden of viral diseases, exemplified by endemic infections and pandemic outbreaks such as COVID-19, underscores the critical need for effective antiviral therapies. While current agents such as nucleoside analogs and direct-acting antivirals (DAAs) have improved the treatment of infections like HIV, hepatitis C, and influenza, they face limitations including narrow target specificity, resistance development, and adverse effects. These challenges are intensified by the rise of emerging zoonotic viruses driven by climate change, globalization, and urbanization, creating an urgent demand for broad-spectrum antivirals with novel mechanisms of action. Mannich base (MB) derivatives have emerged as promising scaffolds in antiviral drug discovery due to their synthetic accessibility, structural diversity, and ability to enhance solubility, permeability, and bioactivity. In addition to these advantages, MBs exhibit broad-spectrum antiviral activity through unique mechanisms, including viral fusion inhibition and allosteric modulation of viral polymerases, distinguishing them from traditional antivirals and offering potential solutions to resistance. Their capacity to target both RNA and DNA viruses further underscores their therapeutic promise. Recent studies have demonstrated the antiviral efficacy of MBs against a wide range of viruses, including yellow fever virus (YFV), respiratory syncytial virus (RSV), hepatitis C virus (HCV), human immunodeficiency virus (HIV), bovine viral diarrhea virus (BVDV), influenza A, and SARS-CoV-2. Structure–activity relationship (SAR) analyses have highlighted the importance of core scaffolds, ring substitutions, amine types, substitution sites, and linker flexibility in modulating antiviral activity. Electron-withdrawing groups (e.g., Cl, Br, NO₂, F) generally enhance potency, while electron-donating groups such as OCH₃ have shown variable effects. This review presents a comprehensive analysis of MB-based antivirals developed over the past two decades, with a focus on SAR insights, mechanistic understanding, and their potential in next-generation antiviral development.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 3","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147720937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Amide-Based Azetidine Derivatives as Anti-Inflammatory and Antimicrobial Agents: Synthesis, Reaction Optimization, Characterization, and In Silico Pharmacokinetic Properties","authors":"P. Pathak,&nbsp;I. J. Modasiya,&nbsp;P. S. Mori,&nbsp;R. Talaviya,&nbsp;G. G. Dubal","doi":"10.1134/S1068162025602770","DOIUrl":"10.1134/S1068162025602770","url":null,"abstract":"<p><b>Objective:</b> To develop a highly efficient protocol for the synthesis of novel amide-based azetidine derivatives and evaluate their anti-inflammatory, antimicrobial, and <i>in silico</i> pharmacokinetic properties. <b>Methods:</b> A series of carbonyl-azetidine derivatives (<b>PP-S1-C1­–PP-S1-C11</b>) were synthesized via amidation of functionalized aromatic acids with an azetidine salt using oxalyl chloride and catalytic DMF at 0°C. The reaction conditions were optimized by screening various coupling reagents (HATU, HBTU, EDC·HCl, T₃P, PyBOP, TBTU, DCC) and chlorinating agents. All synthesized compounds were characterized by ¹H, ¹³C NMR, and mass spectrometry. Anti-inflammatory activity was evaluated <i>in vitro</i> using the bovine serum albumin denaturation assay. Antimicrobial activity was assessed by minimum inhibitory concentration (MIC) determination against Gram-positive and Gram-negative bacterial strains and fungal cultures. <i>In silico</i> ADME properties were predicted using SwissADME. <b>Results and Discussion:</b> Optimization studies revealed that amidation <i>via</i> acid chloride formation using oxalyl chloride with catalytic DMF afforded the target compounds in excellent yields (up to 94%), outperforming conventional coupling reagents. A library of eleven derivatives was successfully synthesized with broad functional group compatibility. Anti-inflammatory evaluation showed that all compounds exhibited &gt;50% inhibition of protein denaturation, with <b>PP-S1-C5</b> demonstrating the highest activity (96.34%) compared to the standard drug diclofenac sodium (98.81%). Antimicrobial screening revealed moderate to good inhibition against the tested bacterial and fungal strains, with MIC values ranging from 16 to 512 μg/mL. <i>In silico</i> ADME studies indicated favorable pharmacokinetic profiles: all compounds exhibited high gastrointestinal absorption, TPSA values within 78.69–102.7 Ų, log<i>P</i>_o/w in the range of 2.6–3.46, and good bioavailability scores, with most compounds complying with Lipinski’s rule of five. <b>Conclusions:</b> A highly efficient and scalable protocol for the synthesis of carbonyl-azetidine derivatives <i>via</i> acid chloride-mediated amidation has been developed. The synthesized compounds demonstrated promising anti-inflammatory and antimicrobial activities, with <b>PP-S1-C5</b> emerging as the most potent anti-inflammatory agent. Favorable <i>in silico</i> pharmacokinetic properties suggest these compounds warrant further investigation as potential therapeutic candidates for inflammatory diseases and bacterial infections.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147606456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Pyrrole-Based Thiazole Conjugates: Design, Synthesis, Antioxidant, Antidiabetic Assessment, Molecular Docking, Simulation, and In Silico ADME Studies","authors":"Bhawana Sati,&nbsp;Anuradha Sharma,&nbsp;Aakash Deep,&nbsp;Harsh Kumar","doi":"10.1134/S1068162025604033","DOIUrl":"10.1134/S1068162025604033","url":null,"abstract":"<p><b>Objective:</b> In the current study, novel heterocyclic molecules of pyrrole-conjugated thiazole were synthesized for the development of antidiabetic drugs. <b>Methods: </b>(<i>E</i>)-2-(2-((1-substituted-1<i>H</i>-pyrrol-2-yl)methylene)hydrazineyl)thiazole analogues (<b>A1–A12</b>) were synthesized by reacting thiosemicarbazide and substituted formyl pyrrole in ethanol to yield the intermediate 1-substituted pyrrol-2-carbaldehyde thiosemicarbazone, followed by the addition of α-bromoacetophenone in anhydrous ethanol and refluxing for 8 h. The synthesized derivatives were evaluated for antioxidant and antidiabetic activity. <b>Results and Discussion:</b> Compound <b>A11</b> was found to be the most efficient antioxidant among all synthesized derivatives, with an IC₅₀ value of 15.28 μg/mL. In the α-amylase inhibitory activity assay, derivatives <b>A9</b> (IC₅₀ = 2.10 ± 0.04 μg/mL), <b>A7</b> (IC₅₀ = 8.20 ± 0.04 μg/mL), and <b>A11</b> (IC₅₀ = 12.10 ± 0.04 μg/mL) demonstrated significantly higher potency, with activities surpassing that of acarbose (IC₅₀ = 20.30 ± 0.20 μg/mL). Significant blood glucose lowering effects were displayed by compounds <b>A9</b> and <b>A11</b> (162 ± 0.21 and 176 ± 0.15 mg/dL, respectively). <b>Conclusions:</b> The appropriate molecular docking studies, ADME properties, and suitable binding interactions make the pyrrole-substituted thiazole analogues a promising structural motif for further clinical evaluation and the development of a new antidiabetic drug molecule.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607220","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and In Silico Docking-Guided Synthesis of Novel Aromatic Amides with Potential Anti-Inflammatory Activity","authors":"Mariam Dawlat Fahmi,&nbsp;Dana Muhammad Hamad Ameen","doi":"10.1134/S1068162025603994","DOIUrl":"10.1134/S1068162025603994","url":null,"abstract":"<p><b>Objective:</b> Inflammation is a major contributor to several chronic illnesses, making it an essential target for anti-inflammatory studies. <b>Methods:</b> Using molecular docking, a virtual library of 100 aromatic amides was designed to target cyclooxygenase-2 (COX-2), leading to the selection of eleven candidates (<b>M1–M11</b>) for synthesis and biological testing. The aromatic amides were synthesized <i>via</i> the Schotten–Baumann reaction, and their pharmacological properties were evaluated. ADME predictions showed Lipinski compliance, high gastrointestinal absorption, and balanced polarity. In vitro COX activity was measured using the Cayman screening kit. <b>Results and Discussion:</b> All candidates demonstrated favorable binding to COX-2, with binding energies ranging from –8.92 to –6.61 kcal/mol. Notably, <b>M10</b> and <b>M7</b> achieved the most favorable docking scores, –8.92 and –8.56 kcal/mol, respectively, while <b>M6</b> showed a stable COX-2 binding mode (–7.14 kcal/mol) and high predicted activity. Compound <b>M6</b> showed IC₅₀ values of 1.563 µM (COX-1) and 0.461 µM (COX-2), revealing stronger activity compared with indomethacin, for which the corresponding values were 1.96 and 25.98 µM. Additionally, <b>M7</b> and <b>M11</b> exhibited the highest COX-2 selectivity indices (13.533 and 12.097, respectively), while <b>M10</b> showed good dual potency with low COX-2 selectivity (2.331). Structure–activity relationship analysis indicates that COX-2 preference and potency in <b>M6</b>, <b>M7</b>, and <b>M11</b> are mainly driven by fused or extended aromatic systems and hydrogen-bonding features. The strong agreement between the docking-predicted binding affinities and the experimentally determined IC₅₀ values confirms that the theoretical model accurately reflected the biological behavior of the synthesized amides. <b>Conclusions:</b> Overall, these amides are promising enzyme inhibitors with favorable pharmacokinetic profiles. Although their assay results are still below those of celecoxib, they support further optimization to enhance COX-2 selectivity, as most outperform indomethacin.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607221","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"1,8-Naphthalimide-Based Fluorescent Bisphosphonates: Molecular Design, Spectral-Luminescent Properties, and Osteotropic Targeted Delivery Systems","authors":"D. Yu. Yuriev,&nbsp;I. V. Barabanshchikov,&nbsp;V. A. Strukova,&nbsp;S. V. Tkachenko,&nbsp;A. A. Pakhomov,&nbsp;S. M. Deev,&nbsp;M. G. Akimov,&nbsp;N. D. Ternovaya,&nbsp;G. D. Sherstyanykh,&nbsp;V. A. Sazonova,&nbsp;V. A. Kalinkina,&nbsp;S. A. Ulasevich,&nbsp;M. S. Oshchepkov","doi":"10.1134/S1068162025605105","DOIUrl":"10.1134/S1068162025605105","url":null,"abstract":"<p><b>Objective:</b> Pathological calcification and bone-metastatic cancers represent significant diagnostic and therapeutic challenges. This study aims to develop a novel theranostic platform based on 1,8-naphthalimide-derived fluorescent bisphosphonates for the selective detection of hydroxyapatite deposits and the creation of effective osteotropic drug delivery systems for bone cancer treatment. <b>Methods:</b> A series of new fluorescent bisphosphonates with systematically varied substituents were synthesized. Their photophysical properties were thoroughly characterized using spectrophotometric and spectrofluorimetric analysis in aqueous and viscous media. The lead compound, a 4-(2-hydroxyethylthio)-substituted derivative, was covalently conjugated to PLGA copolymer <i>via</i> Steglich esterification. PLGA nanoparticles were subsequently fabricated from the conjugate using an ultrasonic method. Internalization and distribution were visualized using fluorescence microscopy on Saos-2 and C2C12 cell lines. <b>Results and Discussion:</b> The synthesized bisphosphonates demonstrated excellent spectral-luminescent characteristics in water, with high quantum yields and viscosity-sensitive emission, confirming their suitability as microenvironment sensors. Cytotoxicity analysis confirmed the low toxicity of the lead compounds and of the nanoparticles on the Saos-2 cell line. The possibility of fluorescence imaging combined with the therapeutic effect of drug loading will further allow these nanoparticles to be considered a promising platform for simultaneous visualization and targeted therapy of bone cancer. <b>Conclusions:</b> We have developed and validated a versatile platform comprising novel fluorescent bisphosphonates and their functionalized PLGA nanocarriers. This study provides a robust foundation for the next generation of targeted theranostic agents for bone pathologies.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147561709","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of Potent Antimicrobial Isatin-Sulphonamide Derivatives: In Vitro and In Silico Studies","authors":"Samir Panda,&nbsp;Sudhir Kumar Paidesetty,&nbsp;Pronoy Kanti Das,&nbsp;Prasad Sanjay Dhiwar,&nbsp;Biswadeep Dutta,&nbsp;Ankan Jati,&nbsp;Monalisa Mahapatra,&nbsp;Sakshar Saha,&nbsp;Vishal P. Zambre","doi":"10.1134/S1068162025601181","DOIUrl":"10.1134/S1068162025601181","url":null,"abstract":"<p><b>Objective: </b>The rapid emergence of multidrug-resistant bacteria poses a serious threat to public health, highlighting an urgent need for the development of novel and potent antimicrobial agents. Antibiotic resistance is primarily driven by the overuse and misuse of antibiotics, which in many countries remain readily available without prescription. <b>Methods:</b> In this study, a novel series of isatin derivatives was designed and synthesized via a condensation reaction to form Schiff bases. The structures of all synthesized compounds were confirmed using various analytical techniques, including ¹H and ¹³C NMR spectroscopy and ESI mass spectrometry. The synthesized compounds were evaluated for their in vitro antimicrobial activity against <i>Escherichia coli</i>, <i>Klebsiella pneumoniae</i>, <i>Salmonella</i> Typhi, <i>Staphylococcus aureus</i>, and <i>Bacillus subtilis</i>. <b>Results and Discussion:</b> Among the tested compounds, <b>SP2</b> exhibited the most potent antimicrobial properties, demonstrating a considerable zone of inhibition and a low minimum inhibitory concentration (MIC) against both Gram-positive and Gram-negative strains. In the DPPH radical scavenging assay, compound <b>SP2</b> also showed the highest antioxidant activity, with an IC₅₀ value of 39.29 µg/mL. <i>In silico</i> molecular docking studies corroborated these findings, as compound <b>SP2</b> displayed the highest binding affinity, with a docking score of –9.9 kcal/mol toward the target protein (PDB ID: 1G2A). <b>Conclusions:</b> In summary, isatin-sulphonamide hybrid <b>SP2</b> demonstrated significant antioxidant activity (69.41% inhibition at 100 µg/mL; IC₅₀: 39.29 µg/mL), notable antimicrobial efficacy (MIC: 0.88–1.05 µmol/mL; zone of inhibition: 22–25 mm), and a strong binding affinity of –9.9 kcal/mol, which is comparable to that of the reference molecule.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147561867","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Acetate Metabolism in Malignant Tumors","authors":"D. A. Korshunov,&nbsp;E. E. Sereda,&nbsp;E. A. Sidenko,&nbsp;G. V. Kakurina,&nbsp;I. V. Kondakova","doi":"10.1134/S1068162025603908","DOIUrl":"10.1134/S1068162025603908","url":null,"abstract":"<p>Active tumor proliferation is always associated with the activation of metabolic pathways. Research into tumor metabolism over the past two decades has revealed numerous metabolomic differences compared to corresponding normal tissues. One of the most critical transformations supporting malignant tumor growth is the restructuring of lipid metabolism. Lipidomic studies have identified molecular changes that can serve as markers for the diagnosis and prognosis of cancer and are also potential targets for targeted therapy. One of the key features of lipogenesis in malignant tumors is the activation of acetate metabolism, which is virtually inactive in healthy tissues. Acetate is involved in various processes associated with lipogenesis. This review presents a detailed description of acetate metabolism and its critical importance in oncogenesis.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147561866","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Carboxyl Derivatives of Chloramphenicol with Stable Linkers in the Side Chain and Their Immunoreactive Conjugates with Horseradish Peroxidase","authors":"O. S. Kuprienko,&nbsp;A. L. Hurski,&nbsp;A. I. Zilberman,&nbsp;I. I. Vashkevich,&nbsp;O. V. Sviridov","doi":"10.1134/S1068162025603921","DOIUrl":"10.1134/S1068162025603921","url":null,"abstract":"<p><b>Objective:</b> In order to ensure the biosafety of food products, they are screened for the presence of the antibiotic chloramphenicol, which is prohibited for veterinary use. For rapid testing, various types of immunoassay are often used, including enzyme-linked immunosorbent assay (ELISA). Chloramphenicol hemisuccinate is an ester of succinic acid. It is often used to obtain the enzyme-labeled conjugate required in ELISA. Long-term storage of this compound in solution leads to hydrolysis of the ester bond, so chloramphenicol hemisuccinate conjugates are fairly labile compounds. The aim of the work is to obtain new derivatives of chloramphenicol at the C3 OH group, the conjugates of which with the enzyme would have greater stability over a long period of storage in the form of a dilute solution. <b>Methods:</b> The new ester and ether at the C3 OH group of chloramphenicol, as well as their conjugates with horseradish peroxidase, were synthesized. The compounds were studied in direct competitive ELISA. Storage at high temperatures or in the Tris-HCl buffer pH 8.7 was used to determine the stability of the conjugates. <b>Results and Discussion:</b> The first derivative of chloramphenicol was obtained by acylation of the C3 OH group with trans-methylcyclohexanedicarboxylic acid anhydride. The product of the reaction is an ester, the hydrolysis of which can be sterically hindered by the cyclohexane ring. Chloramphenicol ether was obtained by adding 4-bromomethylphenylpropionic acid tert-butyl ester to the C3 OH group of the antibiotic. The design of the alkylating reagent allowed carrying out the reaction with chloramphenicol under mild conditions, deprotecting the introduced carboxyl group without the risk of reactions occurring on other functional groups of the antibiotic, and ensuring the increased distance between the chloramphenicol benzene ring and the polypeptide chain of the protein. Enzyme conjugates were obtained using the new derivatives of chloramphenicol and used as labels in ELISA. Storage experiments revealed significant differences in the stability of the conjugates and showed that the most stable was the one in which the antibiotic was tied to the linker by the ether bond. We found that the use of this conjugate in ELISA allowed the determination of chloramphenicol in milk with a limit of quantification of 0.04 μg/kg, the recovery of chloramphenicol additive was 105%. <b>Conclusions:</b> A chloramphenicol conjugate in which the antibiotic is bound to a linker by an ether bond exhibits high stability when stored in dilute solution. Testing of this new conjugate in the ELISA yielded results showing the achievement of the practically important goal of the study</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147559786","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Proteolytic Activity of Oligopeptidase B against Tryptophan-Rich Antiprotozoal Peptides","authors":"A. G. Mikhailova,&nbsp;D. E. Petrenko,&nbsp;D. M. Karlinsky,&nbsp;V. V. Britikov,&nbsp;E. V. Britikova,&nbsp;T. V. Rakitina","doi":"10.1134/S106816202560357X","DOIUrl":"10.1134/S106816202560357X","url":null,"abstract":"<p><b>Objective:</b> Antimicrobial peptides (AMPs), as well as their antiparasitic analogues, are becoming increasingly important for combating hospital-acquired (hospital) infections. Proline- and tryptophan-rich AMPs (PR- and TR-AMPs) are resistant to classical trypsin proteinases, but can be cleaved by oligopeptidases B (OpdB), which participate in protecting bacteria against AMPs. The aim of this study was to investigate the proteolytic activity of OpdB from <i>Serratia proteamaculans</i> (PSP) against model substrates, which are an antiparasitic peptide containing an Arg-Pro peptide bond and its truncated fragment containing a Lys residue in the <i>N</i>-terminal position. <b>Methods:</b> The results of the PSP-dependent peptide hydrolysis were assessed using HPLC and MALDI-TOF mass spectrometry. <b>Results and Discussion:</b> It was found that PSP hydrolyzes the Arg-Pro peptide bond and has aminopeptidase activity. A method was developed for quantitative assessment of the efficiency of cleavage of the model peptides containing several hydrolysis sites. <b>Conclusions:</b> The obtained results confirm the significant role of OpdB in the defense system of bacterial and protozoan cells against PR- and TR-AMPs and emphasize the importance of searching for specific inhibitors of the enzyme.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147559787","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Neurotrophin-4: Discovery, Tissue Distribution, and Biological Effects","authors":"T. A. Gudasheva,&nbsp;N. I. Sokolenko,&nbsp;K. N. Koliasnikova,&nbsp;P. Yu. Povarnina,&nbsp;V. L. Dorofeev","doi":"10.1134/S1068162025603635","DOIUrl":"10.1134/S1068162025603635","url":null,"abstract":"<p>Neurotrophin-4 (NT-4) is the least studied member of the neurotrophin family—proteins that play a key role in the development and functioning of the nervous system. The review presents current data on its discovery, structure, tissue localization, and biological functions. It has been shown that NT-4, like BDNF, interacts predominantly with the TrkB receptor but possesses a number of unique features in its mechanism of action and spectrum of physiological effects. The involvement of NT-4 in the regulation of sensory innervation, appetite control, long-term memory formation, maintenance of fertility, and motor innervation of muscles is considered. The neuroprotective properties of NT-4 in models of neurodegenerative diseases, brain injury, and stroke are summarized, as well as its possible role in the pathogenesis of psychiatric disorders, addiction, and other diseases. The therapeutic potential of NT-4 and the relevance of developing its low-molecular-weight mimetics is emphasized.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 2","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147559751","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}