Integrin αvβ3 and EGFR dual-targeted [64Cu]Cu-NOTA-RGD-GE11 heterodimer for PET imaging in pancreatic cancer mouse model

Li, Huiqiang; Peng, Wenhua; Zhu, Zhen; Zhang, Weifeng; Liao, Shuguang; Wang, Xinyu; Wang, Li; Xuan, Ang; Gao, Yongju; Xu, Jibin

doi:10.1016/j.nucmedbio.2023.108364

Cited by 3 publications

(1 citation statement)

References 39 publications

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“…Снабжение транспортных систем (наночастиц, липосом, везикул) такими адресными лигандами представляет большой интерес [16]. За счет нацеливания циклического cRGD-пептида на интегрин α v β 3 , уровень которого существенно повышен на поверхности клеток различных типов злокачественных опухолей, таких как меланома, ГБМ, рак мочевого пузыря и поджелудочной железы, данный пептид можно считать уникальным молекулярным лигандом для таргетной химиотерапии рака [17][18][19]. В экспериментах in vitro и in vivo обнаружено усиление противоопухолевого действия наночастиц (НЧ), модифицированных cRGD-пептидом, по сравнению с нецелевым аналогом [20][21][22][23][24].…”

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Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Kostryukova,

Tereshkina,

Gisina

et al. 2023

BMCRM

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One of the methods of treating glioblastoma after surgery is chemotherapy; the drugs used in this case, due to their nonspecific distribution, lead to a number of complications. One way to overcome this drawback is to supply drugs with delivery systems with targeted molecules. This approach allows increasing the accumulation of therapeutic agents directly at the lesion site, minimizing side effects. This work is a continuation of the study of the mechanism of action of the previously obtained phospholipid composition of doxorubicin with a targeted cRGD peptide (NPh- Dox-cRGD). This peptide is capable of selectively interacting with integrin ?v?3, a receptor expressed on the surface of a number of tumor cells, including glioblastoma. The work assessed the cytotoxic effect of the NPh-Dox-cRGD composition in comparison with the free substance (Dox) and embedded in phospholipid nanoparticles without a targeted ligand (NPh-Dox). It was shown that after 24 h of incubation of U-87 MG cells with substances at the maximum concentration of Dox (30 ?g/ml), the percentage of viability cells was 6% for Dox, 21% for NPh-Dox-cRGD, and 21% for NPh-Dox � 17%, i.e. When Dox was incorporated into phospholipid NPs, its cytotoxic effect was observed to a lesser extent. No statistically significant differences were noted in the control line HeLa. Assessment of tumor cell death using flow cytometry indicated that most of the cells died via apoptosis. When incubated with a composition containing a targeting peptide, NPh-Dox-cRGD, at a concentration (Dox) of 0.5 ?g/ml, the percentage of cells susceptible to late apoptosis was 29.7%, for the free form � 24.4%. An assessment of cells susceptible to early apoptosis (Dox concentration 0.5 ?g/ml) showed that the percentage of these cells for the sample with the peptide was higher and amounted to 11.4%.

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Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Kostryukova,

Tereshkina,

Gisina

et al. 2023

BMCRM

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Development of a Novel Peptide-Based PET Tracer [⁶⁸Ga]Ga-DOTA-BP1 for BCMA Detection in Multiple Myeloma

Song,

Jiang,

Yang

et al. 2024

J. Med. Chem.

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B-cell maturation antigen (BCMA) has emerged as a promising tumor marker for the diagnosis and treatment of multiple myeloma. The noninvasive and rapid detection of BCMA expression in vivo provides significant value in screening and evaluating multiple myeloma patients receiving BCMA-targeted therapy. We identified the BCMA-targeting peptide BP1 from a one-bead-one-compound (OBOC) peptide library using a highthroughput microarray strategy. The BCMA-targeting specificity and affinity of BP1 were assessed by surface plasmon resonance imaging (SPRi), flow cytometry, and confocal imaging. BCMApositive (H929) and BCMA-negative (K562) subcutaneous tumor models were established and labeled with 68 Ga for BP1, followed by PET imaging and biodistribution studies. PET imaging demonstrated that 68 Ga-labeled BP1 has significant specific uptake in multiple myeloma, enabling rapid identification of BCMA expression and precise delineation of the disease. Thus, BP1 represents an ideal candidate for multiple myeloma imaging.

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EGFR- and Integrin αVβ3-Targeting Peptides as Potential Radiometal-Labeled Radiopharmaceuticals for Cancer Theranostics

Rodrigues Toledo,

Tantawy,

Lima Fuscaldi

et al. 2024

IJMS

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The burgeoning field of cancer theranostics has witnessed advancements through the development of targeted molecular agents, particularly peptides. These agents exploit the overexpression or mutations of specific receptors, such as the Epidermal Growth Factor receptor (EGFR) and αVβ3 integrin, which are pivotal in tumor growth, angiogenesis, and metastasis. Despite the extensive research into and promising outcomes associated with antibody-based therapies, peptides offer a compelling alternative due to their smaller size, ease of modification, and rapid bioavailability, factors which potentially enhance tumor penetration and reduce systemic toxicity. However, the application of peptides in clinical settings has challenges. Their lower binding affinity and rapid clearance from the bloodstream compared to antibodies often limit their therapeutic efficacy and diagnostic accuracy. This overview sets the stage for a comprehensive review of the current research landscape as it relates to EGFR- and integrin αVβ3-targeting peptides. We aim to delve into their synthesis, radiolabeling techniques, and preclinical and clinical evaluations, highlighting their potential and limitations in cancer theranostics. This review not only synthesizes the extant literature to outline the advancements in peptide-based agents targeting EGFR and integrin αVβ3 but also identifies critical gaps that could inform future research directions. By addressing these gaps, we contribute to the broader discourse on enhancing the diagnostic precision and therapeutic outcomes of cancer treatments.

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Integrin αvβ3 and EGFR dual-targeted [64Cu]Cu-NOTA-RGD-GE11 heterodimer for PET imaging in pancreatic cancer mouse model

Cited by 3 publications

References 39 publications

Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Development of a Novel Peptide-Based PET Tracer [⁶⁸Ga]Ga-DOTA-BP1 for BCMA Detection in Multiple Myeloma

EGFR- and Integrin αVβ3-Targeting Peptides as Potential Radiometal-Labeled Radiopharmaceuticals for Cancer Theranostics

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Integrin αvβ3 and EGFR dual-targeted [64Cu]Cu-NOTA-RGD-GE11 heterodimer for PET imaging in pancreatic cancer mouse model

Cited by 3 publications

References 39 publications

Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Influence of Adding cRGD Peptide to Phospholipide Nanoparticles with Doxorubicin Included on Apoptosis in Glioblastoma Cells in Vitro

Development of a Novel Peptide-Based PET Tracer [68Ga]Ga-DOTA-BP1 for BCMA Detection in Multiple Myeloma

EGFR- and Integrin αVβ3-Targeting Peptides as Potential Radiometal-Labeled Radiopharmaceuticals for Cancer Theranostics

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Product

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Development of a Novel Peptide-Based PET Tracer [⁶⁸Ga]Ga-DOTA-BP1 for BCMA Detection in Multiple Myeloma