Publications by authors named "M V Larkina"
The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, Tc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective Tc chelators is 6-hydrazinylnicotinic acid (HYNIC), which, when combined with various vector molecules, can be used for targeted delivery of radionuclides to tumor tissues.
View Article and Find Full Text PDFA high level of EpCAM overexpression in lung cancer makes this protein a promising target for targeted therapy. Radionuclide visualization of EpCAM expression would facilitate the selection of patients potentially benefiting from such treatment. Single-photon computed tomography (SPECT) using Tc-labeled engineered scaffold protein DARPin Ec1 has shown its effectiveness in imaging tumors with overexpression of EpCAM in preclinical studies, providing high contrast just a few hours after injection.
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- Lu-labeled small-molecule PSMA tracers show promise as therapeutic agents for advanced prostate cancer, with potential improvements through optimized molecular design.* -
- Six novel DCL urea-based PSMA ligands were synthesized, achieving satisfactory yields and over 95% radiochemical labeling efficiency for preclinical evaluation.* -
- The study found that molecular modifications, like substituents on the aromatic fragment, significantly affect binding affinity and biodistribution, with certain variants showing improved accumulation in target tissues, although some had unfavorable pharmacokinetics.*
Article Synopsis
- Developing protein therapeutics requires optimizing their pharmacokinetic and pharmacodynamic properties, particularly to prolong their half-lives in the body.
- A study compared various half-life extension technologies (PAS polypeptides, XTEN polypeptides, and an albumin binding domain) using an HER2 affibody-drug conjugate, revealing that while these extensions lowered HER2 affinity slightly, they maintained cytotoxic effectiveness.
- The results indicated that the ABD-enhanced construct had the highest tumor uptake and the best overall performance, despite not having the longest half-life compared to others tested.
HER2 status determination is a necessary step for the proper choice of therapy and selection of patients for the targeted treatment of cancer. Targeted radiotracers such as radiolabeled DARPins provide a noninvasive and effective way for the molecular imaging of HER2 expression. This study aimed to evaluate tumor-targeting properties of three Tc-labeled DARPin G3 variants containing Gly-Gly-Gly-Cys (GC), (Gly-Gly-Gly-Ser)-Cys ((GS)C), or Glu-Glu-Glu-Cys (EC) amino acid linkers at the C-terminus and conjugated to the HYNIC chelating agent, as well as to compare them with the clinically evaluated DARPin G3 labeled with Tc(CO) using the (HE)-tag at the N-terminus.
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