The Lab was formed in 2018 succeeding Bioconjugation Group and Organic Synthesis Lab.  

• Site-specific modification of antibodies and the design of linkers for antibody–drug conjugates (ADCs)
• Molecular design of antivirals and study of their mechanisms of action
• Natural and synthetic antibiotics: structure, biosynthesis, mechanism of action, chemical modification
• Oligonucleotide conjugates for diagnostics and therapy: DNA-probes, aptamers, DNA-nanostructures
• Fluorescent dyes and photosensitizers: design, spectral and photophysical/photochemical properties, biological activity, conjugates with biomolecules
• Mass-spectrometric labels

Site-specific modification of antibodies and the design of linkers for antibody–drug conjugates (ADCs):

• An approach to obtaining homogeneous ADC was developed (10.3390/ijms252413356)
• Modifications of antibodies on carbohydrates with fluorescent dyes (10.1134/S1068162021050332, 10.3390/ijms222312845, 10.3390/molecules28010425) and cytostatic agents (10.3390/ijms24065134) were developed
• A review on carbonyl groups on antibodies (10.3390/molecules28237890)

Molecular design of antivirals and study of their mechanisms of action:

• The antiviral activity of perylene derivatives is based on their membrane activity and singlet oxygen-photogeneration ability (10.3390/ijms242216483, 10.3390/molecules28176278, 10.1016/j.virusres.2023.199158, 10.1016/j.antiviral.2022.105508). The damage to unsaturated lipids of viral envelopes causes inhibition of their fusion with the cellular membrane. The same mechanism of antiviral action is inherent in BODIPY derivatives (10.1021/acsami.4c17482)
• Reviews on mechanisms of antiviral activity of nucleoside derivatives (10.3390/cimb45080433), antiviral photosensitizers (10.3390/ijms24010188, 10.3390/molecules26133971), antiviral activity of perylene and hypericine derivatives (10.1016/bs.armc.2022.08.001)
• Broad-spectrum antiviral activity against enveloped viruses has been studied for several series of perylene derivatives, both nucleoside 0.3390/ph15101178, 10.1016/j.antiviral.2017.11.018, 10.1099/jgv.0.000991, 10.1016/j.ejmech.2018.05.040, 10.1016/j.ejmech.2017.06.014, 10.1039/C5MD00538H, 10.1128/JVI.02882-12, 10.1073/pnas.101002610, 10.1023/A:1023936516589), and non-nucleoside (10.3390/ph15101178, 10.1134/S1068162020030139, 10.1016/j.bmcl.2020.127100, 10.1016/j.ejmech.2019.03.029, 10.1039/c9ra06313g, 10.1016/j.antiviral.2017.11.018, 10.1099/jgv.0.000991). Antiviral activity was found to not correlate with the nucleoside nature of the compound

Natural and synthetic antibiotics: structure, biosynthesis, mechanism of action, chemical modification:

• Structures of new natural antibiotics, lipo(glyco)peptides gausemycins (10.1021/acs.jnatprod.3c00612, 10.1002/anie.202104528), polyketides 6-hydroxytetracenomycin X (10.1016/j.biochi.2021.09.014), O⁴-methyltetracenomycin C (10.1016/j.biochi.2022.10.016), isoirumamycin (10.1016/j.tetlet.2019.04.051), astolides (10.1016/j.tet.2018.11.015), were determined. Homologues of lipodepsipeptides antimycines were discovered (10.3390/microorganisms8121948). It was found that the fluorescence of gausemycins is caused by chlorokynurenine, a rare natural amino acid (10.1007/s00726-018-2642-3). The identity of crystallomycines discovered in the late 1950s to aspartocins found later was confirmed (10.1039/C8MD00002F)
• Biosynthesis pathways were elucidated for irumamycin (10.3390/antibiotics13121167) and gausemycins (10.1002/anie.202104528)
• Original fragmentation pattern of doubly-charged ions of cyclosporins and isocyclosporins in mass-spectrometry were found (10.1016/j.talanta.2020.121930)
• Reviews on visual profiling of antibacterial agents (10.1002/bab.2681), sensing of antibiotic-bacteria interactions (10.3390/antibiotics12081340), modern trends in natural antibiotic discovery (10.3390/life13051073), insect-associated producers of antibiotics (10.3390/biology11111676), antibiotics from extremophile micromycetes (10.1134/S1068162020060023), naththoquinone polyol macrolides (10.1007/s11172-019-2506-3), chemical elicitors of antibiotic biosynthesis (10.3390/microorganisms6020052), amicoumacins and related compounds (10.1016/B978-0-444-64068-0.00012-7)
• Production of antibiotics by nasal pig microbiota was studied (10.1134/S1068162024020237)

Oligonucleotide conjugates for diagnostics and therapy: DNA-probes, aptamers, DNA-nanostructures:

• Bioorthogonal Cu(I)-catalyzed click reaction of azides and alkynes was used for the synthesis of conjugates of aptamers with cytostatic agent MMAE of stoichoimetry 1:1, 2:2, 1:3, 3:1 (10.3390/pharmaceutics16111434), as well as of an [¹⁸F]-derivative of an aptamer for PET (10.3390/molecules28010294)
• Aliphatic polyazides were used for the synthesis of branched oligonucleotide conjugates (10.1021/acs.bioconjchem.7b00462, 10.1016/j.tet.2016.03.051) and DNA-nanostructures (10.1021/acs.langmuir.0c02696, 10.1039/c2cc37547h)
• Various fluorescent DNA-probes were prepared and used in real-time qPCR (10.1134/S1068162021030055, 10.1007/978-1-0716-0138-9_3, 10.1016/j.talanta.2018.10.043, 10.1016/j.mcp.2016.10.003, 10.1039/C6AY01304J, 10.1039/C4AN00081A, 10.1007/s00216-012-6114-4)
• Excimer fluorescence of pyrene (10.1021/acs.analchem.0c00270, 10.1021/acs.joc.7b01451, 10.1023/B:RUCB.0000030825.05631.40, 10.1002/cbic.200300678, 10.1080/07328319908044632, 10.1016/S0956-5663(98)00041-4) and 1-phenylethynylpyrene (10.1016/j.tet.2017.04.045, 10.1021/bc1005027, 10.1039/C0CC03026K, 10.1002/chem.200800380, 10.1002/chem.200801077, 10.1007/978-1-60327-411-1_13, 10.1021/bc700280h, 10.1016/j.mrfmmm.2006.02.007) was studied in DNA-probes and DNA-duplexes

Fluorescent dyes and photosensitizers: design, spectral and photophysical/photochemical properties, biological activity, conjugates with biomolecules:

• Spectral interactions of cyanine dyes sCy3 and sCy5 in linkers were studied (10.3390/molecules30010057)
• BODIPYs were found to possess bright fluorescence in gas phase (10.1016/j.dyepig.2024.112366); bromo and iodo-derivatives of BODIPY were recognized as antivirals (10.1021/acsami.4c17482)
• Oxyamine derivatives of fluorescent dyes were prepared and used for the labeling of antibodies (10.3390/ijms222312845, 10.3390/molecules28010425) and synthesis of steroid tracers for PIA (10.1134/S1068162024010060)
• Various derivatives of cyanine (10.1016/j.biochi.2022.09.015, 10.1002/pmic.201200393, 10.1002/ejoc.200701190, 10.1007/s11172-006-0230-2) and xanthene (10.1002/0471142700.nc0455s52, 10.1021/jo202229t, 10.1021/bc900037b, 10.1021/bc7001874) dyes were prepared

Mass-spectrometric labels:

• Trityl-acridine mass-labels were developed and used for the analysis of antibiotics containing an amino group (10.1021/acs.jnatprod.3c00612, 10.1134/S1068162016060078, 10.32607/20758251-2016-8-3-128-135), amines (10.1039/C5AN02642C, 1568026615666150330110131) and thiols (10.1039/C7AY01965C)

• Based on trityl compounds (10.1039/B008900L), mass-tags were developed (10.1039/B504913J, 10.1055/s-2005-872703, 10.1039/B810600B) and used for the detection of single-nucleotide polymorphism with MALDI MS (10.1021/ac071291y, 10.1007/978-1-60327-411-1_21)

Scientific projects

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Vladimir Korshun

Russia, Moscow, Ul. Miklukho-Maklaya 16/10 — On the map