Anna Orlova
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View article: A New PSMA-targeted Radiopharmaceutical for Single-Photon Emission Computed Tomography
A New PSMA-targeted Radiopharmaceutical for Single-Photon Emission Computed Tomography Open
Цель. Выполнение клинического исследования [99mTc]Tc-ПСМА-BQ (простат-специфического мембранного антигена) у больных раком предстательной железы (РПЖ) с оценкой переносимости и безопасности болюсного введения радиофармпрепарата, изучением …
View article: Modular molecular and nuclear design of scaffold protein -mediated PNA-based radionuclide pre-targeting: application for DARPins
Modular molecular and nuclear design of scaffold protein -mediated PNA-based radionuclide pre-targeting: application for DARPins Open
View article: Affibody-Derived Drug Conjugates Targeting The Epidermal Growth Factor Receptor Are Potent And Specific Cytotoxic Agents
Affibody-Derived Drug Conjugates Targeting The Epidermal Growth Factor Receptor Are Potent And Specific Cytotoxic Agents Open
View article: Preclinical Evaluation of a <sup>177</sup> Lu-Labeled Gastrin-Releasing Peptide Receptor Antagonist and Prostate Cancer Treatment with Monotherapy and in Combination with Everolimus
Preclinical Evaluation of a <sup>177</sup> Lu-Labeled Gastrin-Releasing Peptide Receptor Antagonist and Prostate Cancer Treatment with Monotherapy and in Combination with Everolimus Open
View article: Linker modifications in radiolabeled RM26-based antagonists to gastrin-releasing peptide receptor (GRPR) improved tracers’ pharmacokinetics
Linker modifications in radiolabeled RM26-based antagonists to gastrin-releasing peptide receptor (GRPR) improved tracers’ pharmacokinetics Open
Radionuclide targeting of gastrin-releasing peptide receptor (GRPR) holds significant diagnostic and therapeutic potential, particularly in PSMA-negative/low-grade prostate cancer, estrogen receptor-positive breast cancer, and other malign…
View article: Phase I Clinical Study with the GRPR-Antagonist [99mTc]Tc-DB8 for SPECT Imaging of Prostate Cancer: Does the Injected Peptide Mass Make a Difference?
Phase I Clinical Study with the GRPR-Antagonist [99mTc]Tc-DB8 for SPECT Imaging of Prostate Cancer: Does the Injected Peptide Mass Make a Difference? Open
Background/Objectives: The gastrin-releasing peptide receptor (GRPR) shows high-density expression in prostate cancer (PCa), especially in the early stages of the disease. The introduction of a safe radiotracer for assessing GRPR-expressio…
View article: Reduction of Negative Charge in Mercaptoacetyl-Based Chelators Influences the Biodistribution of Prostate-Specific Membrane Antigen-Targeting Pseudopeptides Labeled with Technetium-99m
Reduction of Negative Charge in Mercaptoacetyl-Based Chelators Influences the Biodistribution of Prostate-Specific Membrane Antigen-Targeting Pseudopeptides Labeled with Technetium-99m Open
Prostate cancer (PCa) is the most common cancer and the second leading cause of death among men worldwide. Significant progress has been made in managing PCa by targeting the prostate-specific membrane antigen (PSMA), which holds great pro…
View article: Preclinical Positron Emission Tomography Imaging of B7–H3 Expression Using Affibody Molecules Labeled with Gallium-68
Preclinical Positron Emission Tomography Imaging of B7–H3 Expression Using Affibody Molecules Labeled with Gallium-68 Open
Affibody molecules, nonimmunoglobulin scaffold proteins, have a high potential as probes for molecular imaging of different molecular targets. One of the molecular targets for radionuclide diagnosis and therapy is B7-H3 (known as CD276), w…
View article: A preclinical study on the influence of linkers in [68Ga]Ga-NOTA-X-RM26 radiotracers for PET imaging of GRPR expression
A preclinical study on the influence of linkers in [68Ga]Ga-NOTA-X-RM26 radiotracers for PET imaging of GRPR expression Open
View article: The Impact of the Injected Mass of the Gastrin-Releasing Peptide Receptor Antagonist on Uptake in Breast Cancer: Lessons from a Phase I Trial of [99mTc]Tc-DB8
The Impact of the Injected Mass of the Gastrin-Releasing Peptide Receptor Antagonist on Uptake in Breast Cancer: Lessons from a Phase I Trial of [99mTc]Tc-DB8 Open
Background/Objectives: Gastrin-releasing peptide receptor (GRPR) is overexpressed in breast cancer and might be used as a theranostics target. The expression of GRPR strongly correlates with estrogen receptor (ER) expression. Visualization…
View article: Targeting of Epithelial Cell Adhesion Molecule-Expressing Malignant Tumors Using an Albumin-Binding Domain-Fused Designed Ankyrin Repeat Protein: Effect of the Molecular Architecture
Targeting of Epithelial Cell Adhesion Molecule-Expressing Malignant Tumors Using an Albumin-Binding Domain-Fused Designed Ankyrin Repeat Protein: Effect of the Molecular Architecture Open
Designed ankyrin repeat protein (DARPin) Ec1, a small scaffold protein (18 kDa), binds with high affinity the epithelial cell adhesion molecule (EpCAM) that is overexpressed in several carcinomas. To enhance the targeted delivery of cytoto…
View article: Temporal indicators of the implementation of attacks as a result of active preparatory actions and the assessment of sensorimotor responses in matches among qualified karate practitioners
Temporal indicators of the implementation of attacks as a result of active preparatory actions and the assessment of sensorimotor responses in matches among qualified karate practitioners Open
The purpose of the study is to determine the criteria for assessing the ability to apply active preparatory actions, for which an analysis of the temporal indicators of the performance of motor action components in the context of simulatin…
View article: Synthesis and preclinical evaluation of gastrin releasing peptide receptor antagonist [18F]MeTz-PEG2-RM26 for positron emission tomography
Synthesis and preclinical evaluation of gastrin releasing peptide receptor antagonist [18F]MeTz-PEG2-RM26 for positron emission tomography Open
View article: Single-Photon Emission Computer Tomography Imaging of Prostate-Specific Membrane Antigen (PSMA) Expression in Prostate Cancer Patients Using a Novel Peptide-Based Probe [<sup>99m</sup>Tc]Tc-BQ0413 with Picomolar Affinity to PSMA: A Phase I/II Clinical Study
Single-Photon Emission Computer Tomography Imaging of Prostate-Specific Membrane Antigen (PSMA) Expression in Prostate Cancer Patients Using a Novel Peptide-Based Probe [<sup>99m</sup>Tc]Tc-BQ0413 with Picomolar Affinity to PSMA: A Phase I/II Clinical Study Open
Radionuclide imaging of prostate-specific membrane antigen (PSMA) expression can be used for staging prostate cancer. The pseudo-peptide [99mTc]Tc-BQ0413 demonstrated high affinity and specificity to PSMA in preclinical evaluati…
View article: First-in-human experience with GRPR antagonist [68Ga]Ga-NOTA-PEG2-RM26 in prostate and breast cancer patients using PET/CT
First-in-human experience with GRPR antagonist [68Ga]Ga-NOTA-PEG2-RM26 in prostate and breast cancer patients using PET/CT Open
View article: Impact of Radiometal Chelates on In Vivo Visualization of Immune Checkpoint Protein Using Radiolabeled Affibody Molecules
Impact of Radiometal Chelates on In Vivo Visualization of Immune Checkpoint Protein Using Radiolabeled Affibody Molecules Open
The immune checkpoint protein B7-H3 (CD276) is overexpressed in various cancers and is an attractive target for the treatment of malignant tumors. Radionuclide molecular imaging of B7-H3 expression using engineered scaffold proteins such a…
View article: Evaluation of maSSS/maSES-PEG2-RM26 for their potential therapeutic use after labeling with Re-188. Could their [99mTc]Tc-labeled counterparts be used to estimate dosimetry?
Evaluation of maSSS/maSES-PEG2-RM26 for their potential therapeutic use after labeling with Re-188. Could their [99mTc]Tc-labeled counterparts be used to estimate dosimetry? Open
View article: Affibody-Drug Conjugates Targeting the Human Epidermal Growth Factor Receptor-3 Demonstrate Therapeutic Efficacy in Mice Bearing Low Expressing Xenografts
Affibody-Drug Conjugates Targeting the Human Epidermal Growth Factor Receptor-3 Demonstrate Therapeutic Efficacy in Mice Bearing Low Expressing Xenografts Open
The outcome of clinical trials evaluating drugs targeting the human epidermal growth factor receptor 3 (HER3) has been poor, with primary concerns related to lack of efficacy. HER3 is considered a difficult target since its overexpression …
View article: Evaluation of ABD-Linked RM26 Conjugates for GRPR-Targeted Drug Delivery
Evaluation of ABD-Linked RM26 Conjugates for GRPR-Targeted Drug Delivery Open
Targeting the gastrin-releasing peptide receptor (GRPR) with the bombesin analogue RM26, a 9 aa peptide, has been a promising strategy for cancer theranostics, with recent success in radionuclide imaging of prostate cancer. However, therap…
View article: Phase I Clinical Evaluation of Designed Ankyrin Repeat Protein [99mTc]Tc(CO)3-(HE)3-Ec1 for Visualization of EpCAM-Expressing Lung Cancer
Phase I Clinical Evaluation of Designed Ankyrin Repeat Protein [99mTc]Tc(CO)3-(HE)3-Ec1 for Visualization of EpCAM-Expressing Lung Cancer Open
A 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 trea…
View article: Evaluation of a novel 177Lu-labelled therapeutic Affibody molecule with a deimmunized ABD domain and improved biodistribution profile
Evaluation of a novel 177Lu-labelled therapeutic Affibody molecule with a deimmunized ABD domain and improved biodistribution profile Open
View article: Half-life extension via ABD-fusion leads to higher tumor uptake of an affibody-drug conjugate compared to PAS- and XTENylation.
Half-life extension via ABD-fusion leads to higher tumor uptake of an affibody-drug conjugate compared to PAS- and XTENylation. Open
A critical parameter during the development of protein therapeutics is to endow them with suitable pharmacokinetic and pharmacodynamic properties. Small protein drugs are quickly eliminated by kidney filtration, and in vivo half-life exten…
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: Shorter Peptide Nucleic Acid Probes Improve Affibody-Mediated Peptide Nucleic Acid-Based Pretargeting
Shorter Peptide Nucleic Acid Probes Improve Affibody-Mediated Peptide Nucleic Acid-Based Pretargeting Open
Affibody-mediated PNA-based pretargeting shows promise for HER2-expressing tumor radiotherapy. In our recent study, a 15-mer ZHER2:342-HP15 affibody-PNA conjugate, in combination with a shorter 9-mer [177Lu]Lu-HP16 ef…
View article: Comparison of approaches for increasing affinity of affibody molecules for imaging of B7-H3: dimerization and affinity maturation
Comparison of approaches for increasing affinity of affibody molecules for imaging of B7-H3: dimerization and affinity maturation Open
View article: Preclinical Evaluation of HER2-Targeting DARPin G3: Impact of Albumin-Binding Domain (ABD) Fusion
Preclinical Evaluation of HER2-Targeting DARPin G3: Impact of Albumin-Binding Domain (ABD) Fusion Open
Designed ankyrin repeat protein (DARPin) G3 is an engineered scaffold protein. This small (14.5 kDa) targeting protein binds with high affinity to human epidermal growth factor receptor 2 (HER2). HER2 is overexpressed in several cancers. T…
View article: Two Novel [<sup>68</sup>Ga]Ga-Labeled Radiotracers Based on Metabolically Stable [Sar<sup>11</sup>]RM26 Antagonistic Peptide for Diagnostic Positron Emission Tomography Imaging of GRPR-Positive Prostate Cancer
Two Novel [<sup>68</sup>Ga]Ga-Labeled Radiotracers Based on Metabolically Stable [Sar<sup>11</sup>]RM26 Antagonistic Peptide for Diagnostic Positron Emission Tomography Imaging of GRPR-Positive Prostate Cancer Open
Gastrin releasing peptide receptor (GRPR) is overexpressed in prostate cancer (PC-3) and can be used for diagnostic purposes. We herein present the design and preclinical evaluation of two novel NOTA/NODAGA-containing peptides suitable for…
View article: GRPR-Antagonists Carrying DOTAGA-Chelator via Positively Charged Linkers: Perspectives for Prostate Cancer Theranostics
GRPR-Antagonists Carrying DOTAGA-Chelator via Positively Charged Linkers: Perspectives for Prostate Cancer Theranostics Open
Gastrin-releasing peptide receptor (GRPR)-antagonists have served as motifs in the development of theranostic radioligands for prostate cancer. Our efforts have been focused on the development of radiolabeled RM26 (H-DPhe6–Gln7–Trp8–Ala9–V…
View article: Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m
Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m Open
Previously, we designed the EuK-based PSMA ligand BQ0413 with an maE3 chelator for labeling with technetium-99m. It showed efficient tumor targeting, but our preclinical data and preliminary clinical results indicated that the renal excret…
View article: Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology
Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology Open