Aleksei E. Machulkin
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View article: Synthesis of Bispidine-Based Prostate-Specific Membrane Antigen-Targeted Conjugate and Initial Investigations
Synthesis of Bispidine-Based Prostate-Specific Membrane Antigen-Targeted Conjugate and Initial Investigations Open
Nowadays, PSMA ligands are widely used for radiotheragnostic purposes in prostate cancer. The synthesis of a PSMA-Bisp conjugate was developed and realized with good yield (overall yield ~58% for the last two steps). All newly synthesized …
View article: Synthesis of bispidine based PSMA targeted conjugate and initial investigations.
Synthesis of bispidine based PSMA targeted conjugate and initial investigations. Open
Nowadays PSMA ligands are widely used for radiotheragnostic purposes of prostate cancer. The goal of this study was to synthesize and estimate stability in vitro of copper complex with diacetate bispidine ligand (Bisp1), its bifunctional d…
View article: Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation
Routes to PSMA/GRPr Targeted Heterobivalent Conjugates: Synthetic Strategies and Their Evaluation Open
Heterodimeric approach has emerged as a promising method for simultaneously targeting multiple receptors on tumor cells using a single molecule. Simultaneous targeting of the prostate-specific membrane antigen (PSMA) and the gastrin-releas…
View article: Synthesis and Preclinical Evaluation of Urea-Based Prostate-Specific Membrane Antigen-Targeted Conjugates Labeled with <sup>177</sup>Lu
Synthesis and Preclinical Evaluation of Urea-Based Prostate-Specific Membrane Antigen-Targeted Conjugates Labeled with <sup>177</sup>Lu Open
177Lu-labeled small-molecule prostate-specific membrane antigen (PSMA) targeted tracers are therapeutic agents for metastatic castration-resistant prostate cancer. Optimizing molecular design holds the potential to further enhan…
View article: Structure-activity relationship study of mesyl and busyl phosphoramidate antisense oligonucleotides for unaided and PSMA-mediated uptake into prostate cancer cells
Structure-activity relationship study of mesyl and busyl phosphoramidate antisense oligonucleotides for unaided and PSMA-mediated uptake into prostate cancer cells Open
Phosphorothioate (PS) group is a key component of a majority of FDA approved oligonucleotide drugs that increase stability to nucleases whilst maintaining interactions with many proteins, including RNase H in the case of antisense oligonuc…
View article: Pentamethine Cyanine Dyes with Alkynyl Group as Perspective Structure for Conjugation with Targeting Moiety
Pentamethine Cyanine Dyes with Alkynyl Group as Perspective Structure for Conjugation with Targeting Moiety Open
View article: Synthesis, 123I-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with a Tributylstannyl Prosthetic Group in Their Structures
Synthesis, 123I-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with a Tributylstannyl Prosthetic Group in Their Structures Open
Prostate-specific membrane antigen (PSMA) has been identified as a target for the development of theranostic agents. In our current work, we describe the design and synthesis of novel N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-L-lysine (…
View article: Synthesis of Prostate-Specific Membrane Antigen-Targeted Bimodal Conjugates of Cytotoxic Agents and Antiandrogens and Their Comparative Assessment with Monoconjugates
Synthesis of Prostate-Specific Membrane Antigen-Targeted Bimodal Conjugates of Cytotoxic Agents and Antiandrogens and Their Comparative Assessment with Monoconjugates Open
Prostate cancer is the second most common cancer among men. We designed and synthesized new ligands targeting prostate-specific membrane antigen and suitable for bimodal conjugates with diagnostic and therapeutic agents. In vitro studies o…
View article: Synthesis, <sup>123</sup>I-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with Tributylstannyl Prosthetic Group in Their Structures
Synthesis, <sup>123</sup>I-Radiolabeling Optimization, and Initial Preclinical Evaluation of Novel Urea-Based PSMA Inhibitors with Tributylstannyl Prosthetic Group in Their Structures Open
Prostate-specific membrane antigen (PSMA) has been identified as a target for the development of theranostic agents. In our current work, we describe the design and synthesis of novel N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-(S)-L-lysine (…
View article: Bifunctional Magnetite–Gold Nanoparticles for Magneto-Mechanical Actuation and Cancer Cell Destruction
Bifunctional Magnetite–Gold Nanoparticles for Magneto-Mechanical Actuation and Cancer Cell Destruction Open
Magnetite–gold dumbbell nanoparticles are essential for biomedical applications due to the presence of two surfaces with different chemical natures and the potential combination of magnetic and plasmonic properties. Here, the remote actuat…
View article: Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate
Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate Open
Prostate cancer is the second most common type of cancer among men. The main method of its treatment is androgen deprivation therapy, which has a wide range of side effects. One of the solutions to this challenge is the targeted delivery o…
View article: Synthesis and initial in vitro evaluation of PSMA-targeted ligands with optimized structural motifs.
Synthesis and initial in vitro evaluation of PSMA-targeted ligands with optimized structural motifs. Open
An improved series of ligands targeting prostatic specific membrane antigen (PSMA) has been reported. Varying compounds and their biological parameters were due to changes in the linker structure. Highly selective compounds with nanomolar …
View article: Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom
Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom Open
View article: Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate Open
Prostate cancer is the second most common type of cancer among men. Its main method of treatment is chemotherapy, which has a wide range of side effects. One of the solutions to this challenge is targeted delivery to prostate cancer cells.…
View article: PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation
PSMA-targeted small-molecule docetaxel conjugate: Synthesis and preclinical evaluation Open
View article: PSMA-targeted low-molecular double conjugates for diagnostics and therapy
PSMA-targeted low-molecular double conjugates for diagnostics and therapy Open
View article: Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them
Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them Open
Prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II (GCPII), is a suitable target for specific delivery of antitumor drugs and diagnostic agents due to its overexpression in prostate cancer cells. In the …
View article: Novel potent PSMA ligands and their docetaxel conjugates: in vitro and in vivo evaluation
Novel potent PSMA ligands and their docetaxel conjugates: in vitro and in vivo evaluation Open
View article: Polypeptide-Based Molecular Platform and Its Docetaxel/Sulfo-Cy5-Containing Conjugate for Targeted Delivery to Prostate Specific Membrane Antigen
Polypeptide-Based Molecular Platform and Its Docetaxel/Sulfo-Cy5-Containing Conjugate for Targeted Delivery to Prostate Specific Membrane Antigen Open
A strategy for stereoselective synthesis of molecular platform for targeted delivery of bimodal therapeutic or theranostic agents to the prostate-specific membrane antigen (PSMA) receptor was developed. The proposed platform contains a ure…
View article: Pharmacokinetic Properties of 68Ga-labelled Folic Acid Conjugates: Improvement Using HEHE Tag
Pharmacokinetic Properties of 68Ga-labelled Folic Acid Conjugates: Improvement Using HEHE Tag Open
The folate receptor (FR) is a promising cell membrane-associated target for molecular imaging and radionuclide therapy of cancer (FR-α) and potentially also inflammatory diseases (FR-β) through use of folic acid-based radioconjugate. FR is…
View article: Synthesis and biological evaluation of PSMA-targeting paclitaxel conjugates
Synthesis and biological evaluation of PSMA-targeting paclitaxel conjugates Open
View article: Synthesis and biological evaluation of paclitaxel conjugates with prostate-specific membrane antigen inhibitor for the treatment of prostate cancer . .
Synthesis and biological evaluation of paclitaxel conjugates with prostate-specific membrane antigen inhibitor for the treatment of prostate cancer . . Open
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View article: CCDC 1832089: Experimental Crystal Structure Determination
CCDC 1832089: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …