Alexander S. Tikhomirov
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View article: Olivomycin A Targets Epithelial–Mesenchymal Transition, Apoptosis, and Mitochondrial Quality Control in Renal Cancer Cells
Olivomycin A Targets Epithelial–Mesenchymal Transition, Apoptosis, and Mitochondrial Quality Control in Renal Cancer Cells Open
Here, we show that the aureolic acid-class antibiotic, olivomycin A, exerts potent anticancer activity in renal cell carcinoma (RCC) by disrupting both cell survival and metastatic programs. In A-498 (wild-type p53) and 786-O (loss-of-func…
View article: Discovery of cytotoxic indolo[1,2-<i>c</i>]quinazoline derivatives through scaffold-based design
Discovery of cytotoxic indolo[1,2-<i>c</i>]quinazoline derivatives through scaffold-based design Open
Indolo[1,2- c ]quinazoline derivatives have emerged as promising chemotype in drug discovery due to their versatile biological activities, including antimicrobial and antiviral properties. In this study, we report the design, synthesis, an…
View article: Dual Regulation of Epithelial-Mesenchymal Transition and Mitochondrial Quality Control by Olivomycin A in Renal Cancer Cells
Dual Regulation of Epithelial-Mesenchymal Transition and Mitochondrial Quality Control by Olivomycin A in Renal Cancer Cells Open
Here, we show that the aureolic acid-class antibiotic, olivomycin A, exerts potent anticancer activity in renal cell carcinoma (RCC) by disrupting both cell survival and metastatic programs. In A-498 (wild-type p53) and 786-O (loss-of-func…
View article: Non-split superstrings of dimension (1|2)
Non-split superstrings of dimension (1|2) Open
View article: Non-split superstrings of dimension $(1|2)$
Non-split superstrings of dimension $(1|2)$ Open
Any supermanifold diffeomorphic to one whose structure sheaf is the sheaf of sections of a~vector bundle over the underlying manifold is called split. Gaw\c{e}dzki (1977) and Batchelor (1979) were the first to prove that any smooth superma…
View article: Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives
Synthesis and Antibacterial Activity of New 6″-Modified Tobramycin Derivatives Open
Objectives: Aminoglycosides are one of the first classes of natural antibiotics which have not lost relevance due to their broad spectrum of action against Gram-positive, Gram-negative bacteria and mycobacteria. The high growth rate of ant…
View article: Author Response: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Author Response: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
Full text Figures and data Peer review Side by side Abstract eLife assessment Introduction Results Discussion Methods Data availability References Article and author information Metrics Abstract The antibiotic heliomycin (resistomycin), wh…
View article: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus , has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been h…
View article: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus, has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been hi…
View article: Joint Public Review: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Joint Public Review: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus, has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been hi…
View article: Author Response: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Author Response: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus, has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been hi…
View article: Hybrid Molecules of Azithromycin with Chloramphenicol and Metronidazole: Synthesis and Study of Antibacterial Properties
Hybrid Molecules of Azithromycin with Chloramphenicol and Metronidazole: Synthesis and Study of Antibacterial Properties Open
The sustained rise of antimicrobial resistance (AMR) causes a strong need to develop new antibacterial agents. One of the methods for addressing the problem of antibiotic resistance is through the design of hybrid antibiotics. In this work…
View article: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus , has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been h…
View article: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus, has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been hi…
View article: Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells
Water-soluble 4-(dimethylaminomethyl)heliomycin exerts greater antitumor effects than parental heliomycin by targeting the tNOX-SIRT1 axis and apoptosis in oral cancer cells Open
The antibiotic heliomycin (resistomycin), which is generated from Streptomyces resistomycificus , has multiple activities, including anticancer effects. Heliomycin was first described in the 1960s, but its clinical applications have been h…
View article: Design, Synthesis and In Vitro Investigation of Cabozantinib-Based PROTACs to Target c-Met Kinase
Design, Synthesis and In Vitro Investigation of Cabozantinib-Based PROTACs to Target c-Met Kinase Open
(1) Background: This investigation aimed at developing a series of c-Met-targeting cabozantinib-based PROTACs. (2) Methods: Purification of intermediate and target compounds was performed using column chromatography, in vitro antiprolifera…
View article: Computational and Biophysical Characterization of Heterocyclic Derivatives of Anthraquinone against Human Aurora Kinase A
Computational and Biophysical Characterization of Heterocyclic Derivatives of Anthraquinone against Human Aurora Kinase A Open
Human Aurora kinase A (AurA) has recently garnered the attention of researchers worldwide as a promising effective mitotic drug target for its involvement in cancer and related inflammatory anomalies. This study has explored the binding af…
View article: Bis(chloroacetamidino)-Derived Heteroarene-Fused Anthraquinones Bind to and Cause Proteasomal Degradation of tNOX, Leading to c-Flip Downregulation and Apoptosis in Oral Cancer Cells
Bis(chloroacetamidino)-Derived Heteroarene-Fused Anthraquinones Bind to and Cause Proteasomal Degradation of tNOX, Leading to c-Flip Downregulation and Apoptosis in Oral Cancer Cells Open
Anthraquinone-based intercalating compounds, namely doxorubicin and mitoxantrone, have been used clinically based on their capacity to bind DNA and induce DNA damage. However, their applications have been limited by side effects and drug r…
View article: СИНТЕЗ И АНТИПРОЛИФЕРАТИВНАЯ АКТИВНОСТЬ НОВЫХ ГЕТЕРОЦИКЛИЧЕСКИХ ПРОИЗВОДНЫХ АНТРАХИНОНА: ТИАДИАЗОЛА, СЕЛЕНОДИАЗОЛА И ТРИАЗОЛА
СИНТЕЗ И АНТИПРОЛИФЕРАТИВНАЯ АКТИВНОСТЬ НОВЫХ ГЕТЕРОЦИКЛИЧЕСКИХ ПРОИЗВОДНЫХ АНТРАХИНОНА: ТИАДИАЗОЛА, СЕЛЕНОДИАЗОЛА И ТРИАЗОЛА Open
View article: Photosensitization of pancreatic cancer cells by cationic alkyl-porphyrins in free form or engrafted into POPC liposomes: The relationship between delivery mode and mechanism of cell death
Photosensitization of pancreatic cancer cells by cationic alkyl-porphyrins in free form or engrafted into POPC liposomes: The relationship between delivery mode and mechanism of cell death Open
Cationic porphyrins bearing an alkyl side chain of 14 (2b) or 18 (2d) carbons dramatically inhibit proliferation of pancreatic cancer cells following treatment with light. We have compared two different ways of delivering porphyrin 2d: eit…
View article: Reductive Elimination of Alkoxy Group in Anthraquinone Derivatives
Reductive Elimination of Alkoxy Group in Anthraquinone Derivatives Open
View article: Antibiotic heliomycin and its water-soluble 4-aminomethylated derivative provoke cell death in T24 bladder cancer cells by targeting sirtuin 1 (SIRT1).
Antibiotic heliomycin and its water-soluble 4-aminomethylated derivative provoke cell death in T24 bladder cancer cells by targeting sirtuin 1 (SIRT1). Open
Bladder cancer is one of the most frequent cancers among males, and a poor survival rate reflects problems with aggressiveness and chemo-resistance. Accumulating evidence indicates that SIRT1 is involved in bladder cancer tumorigenesis and…
View article: 56P tNOX and Sirt1 as potential targets of antitumor action of heliomycin derivatives
56P tNOX and Sirt1 as potential targets of antitumor action of heliomycin derivatives Open
View article: Experimental Evaluation of Anticancer Efficiency and Acute Toxicity of Anthrafuran for Oral Administration
Experimental Evaluation of Anticancer Efficiency and Acute Toxicity of Anthrafuran for Oral Administration Open
The new antitumor agent anthrafuran has demonstrated a consistent effect in murine tumor models when administered parenterally due to the simultaneous inhibition of multiple cellular targets such as topoisomerases I/II and protein kinases.…
View article: Photodynamic Therapy for <i>ras</i>-Driven Cancers: Targeting G-Quadruplex RNA Structures with Bifunctional Alkyl-Modified Porphyrins
Photodynamic Therapy for <i>ras</i>-Driven Cancers: Targeting G-Quadruplex RNA Structures with Bifunctional Alkyl-Modified Porphyrins Open
Designing small molecules able to break down G4 structures in mRNA (RG4s) offers an interesting approach to cancer therapy. Here, we have studied cationic porphyrins (CPs) bearing an alkyl chain up to 12 carbons, as they bind to RG4s while…
View article: An algebraic-geometric construction of ind-varieties of generalized flags
An algebraic-geometric construction of ind-varieties of generalized flags Open
We define the class of admissible linear embeddings of flag varieties. The definition is given in the general language of algebraic geometry. We then prove that an admissible linear embedding of flag varieties has a certain explicit form i…
View article: Engagement with tNOX (ENOX2) to Inhibit SIRT1 and Activate p53-Dependent and -Independent Apoptotic Pathways by Novel 4,11-Diaminoanthra[2,3-b]furan-5,10-diones in Hepatocellular Carcinoma Cells
Engagement with tNOX (ENOX2) to Inhibit SIRT1 and Activate p53-Dependent and -Independent Apoptotic Pathways by Novel 4,11-Diaminoanthra[2,3-b]furan-5,10-diones in Hepatocellular Carcinoma Cells Open
Hepatocellular carcinoma (HCC) is the most frequent primary malignancy of the liver and is among the top three causes of cancer-associated death worldwide. However, the clinical use of chemotherapy for HCC has been limited by various chall…
View article: PO-458 The role of functional groups in the antitumor properties of antrafuran
PO-458 The role of functional groups in the antitumor properties of antrafuran Open
Introduction Recently we have discovered a promising anticancer agent Anthrafuran (LCTA-2034, ( S )−3-(3-aminopyrrolidine-1-carbonyl)−4,11-dihydroxy-2-methylanthra [2,3-b]furan-5,10-dione methanesulfonate) which targeted topoisomerases (T…
View article: Algebraic Cycles on Quadric Sections of Cubics in ℙ<sup>4</sup> Under the Action of Symplectomorphisms – Erratum
Algebraic Cycles on Quadric Sections of Cubics in ℙ<sup>4</sup> Under the Action of Symplectomorphisms – Erratum Open
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View article: Design of an Activity-Based Probe for Human Neutrophil Elastase: Implementation of the Lossen Rearrangement To Induce Förster Resonance Energy Transfers
Design of an Activity-Based Probe for Human Neutrophil Elastase: Implementation of the Lossen Rearrangement To Induce Förster Resonance Energy Transfers Open
Human neutrophil elastase is an important regulator of the immune response and plays a role in host defense mechanisms and further physiological processes. The uncontrolled activity of this serine protease may cause severe tissue alteratio…