Theranostic iRGD peptide containing cisplatin prodrug: Dual-cargo tumor penetration for improved imaging and therapy

Cho, Hong Jun; Park, Sung Jun; Lee, Yoon Sik; Kim, Sehoon

doi:10.1016/j.jconrel.2019.02.043

Cited by 34 publications

(22 citation statements)

References 40 publications

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“…Previous reports demonstrated that iRGD improves the tumor homing and vascular/tissue penetration of NPs. [ 25–27 ] We optimized various aspects of particles and their use (size, dose, and dosing scheme) using 4T1 mouse breast tumor model. Two different sizes of iRGD‐liposomes were tested and their ASO EE% was listed in Table 1.…”

Section: Resultsmentioning

confidence: 99%

iRGD‐Liposomes Enhance Tumor Delivery and Therapeutic Efficacy of Antisense Oligonucleotide Drugs against Primary Prostate Cancer and Bone Metastasis

Guan

Guo

Tang

et al. 2021

Adv Funct Materials

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Nucleotide‐based drugs, such as antisense oligonucleotides (ASOs), have unique advantages in treating human diseases as they provide virtually unlimited ability to target any gene. However, their clinical translation faces many challenges, one of which is poor delivery to the target tissue in vivo. This problem is particularly evident in solid tumors. Here, liposomes are functionalized with a tumor‐homing and ‐penetrating peptide, iRGD, as a carrier of an ASO against androgen receptor (AR) for prostate cancer treatment. The iRGD‐liposomes exhibit a high loading efficiency of AR‐ASO, and an efficient knockdown of AR gene products is achieved in vitro, including AR splice variants. In vivo, iRGD‐liposomes significantly increase AR‐ASO accumulation in the tumor tissue and decrease AR expression relative to free ASOs in prostate tumors established as subcutaneous xenografts. Similar results are obtained with intra‐tibial xenografts modeling metastasis to bones, the predominant site of metastasis for prostate cancer. In treatment studies, iRGD‐liposomes markedly improve the AR‐ASO efficacy in suppressing the growth of both subcutaneous xenografts and intra‐tibial xenografts. The inhibitory effect on tumor growth is also significantly prolonged by the delivery of the AR‐ASO in the iRGD‐liposomes. Meanwhile, iRGD‐liposomes does not increase ASO accumulation or toxicity in healthy organs. Overall, a delivery system that can significantly increase ASO accumulation and efficacy in solid tumors is provided here. These benefits are achieved without significant side effects, providing a way to increase the antitumor efficacy of ASOs.

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Section: Resultsmentioning

confidence: 99%

iRGD‐Liposomes Enhance Tumor Delivery and Therapeutic Efficacy of Antisense Oligonucleotide Drugs against Primary Prostate Cancer and Bone Metastasis

Guan

Guo

Tang

et al. 2021

Adv Funct Materials

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“…Examples of RGD ligands and cytotoxic drug complexes can be found in two recent reviews [152,153] . Recent advances in the field included dual‐functional complexes that incorporate one fluorophore on one side for imaging and a cytotoxic pro‐drug on the other side [154] . But currently intense efforts are mainly directed towards nanocarriers functionalized with RGD ligands.…”

Section: Current Applications Of Rgd Ligandsmentioning

confidence: 99%

Biological Relevance of RGD‐Integrin Subtype‐Specific Ligands in Cancer

et al. 2020

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Integrins are heterodimeric transmembrane proteins able to connect cells with the micro‐environment. They represent a family of receptors involved in almost all the hallmarks of cancer. Integrins recognizing the Arg‐Gly‐Asp (RGD) peptide in their natural extracellular matrix ligands have been particularly investigated as tumoral therapeutic targets. In the last 30 years, intense research has been dedicated to designing specific RGD‐like ligands able to discriminate selectively the different RGD‐recognizing integrins. Chemists′ efforts have led to the proposition of modified peptide or peptidomimetic libraries to be used for tumor targeting and/or tumor imaging. Here we review, from the biological point of view, the rationale underlying the need to clearly delineate each RGD‐integrin subtype by selective tools. We describe the complex roles of RGD‐integrins (mainly the most studied αvβ3 and α5β1 integrins) in tumors, the steps towards selective ligands and the current usefulness of such ligands. Although the impact of integrins in cancer is well acknowledged, the biological characteristics of each integrin subtype in a specific tumor are far from being completely resolved. Selective ligands might help us to reconsider integrins as therapeutic targets in specific clinical settings.

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“…In comparison to a control peptide having a non‐iRGD sequence, such probe displayed better tumor imaging contrast. [ 71 ] More recently, efforts have been devoted to design RGD cyclopeptides to selectively image other relatively unexplored integrin receptors, such as αvβ8, with promising results. [ 72 ]…”

Section: Chemical Synthesis Of Fluorescent Cyclic Peptidesmentioning

confidence: 99%

Fluorescent cyclic peptides for cell imaging

2020

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Fluorescent cyclic peptides are excellent chemical scaffolds to build optical agents for molecular imaging. In addition to their favorable physicochemical properties, they can be modified with multiple organic fluorophores and generate useful probes for biological assays targeting specific proteins, namely receptors or enzymes. In this article, we review recent advances in the synthetic approaches for the preparation of fluorescent cyclic peptides as well as some of their applications in biological imaging, from in vitro live‐cell imaging studies to in vivo characterization of preclinical models.

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Theranostic iRGD peptide containing cisplatin prodrug: Dual-cargo tumor penetration for improved imaging and therapy

Cited by 34 publications

References 40 publications

iRGD‐Liposomes Enhance Tumor Delivery and Therapeutic Efficacy of Antisense Oligonucleotide Drugs against Primary Prostate Cancer and Bone Metastasis

iRGD‐Liposomes Enhance Tumor Delivery and Therapeutic Efficacy of Antisense Oligonucleotide Drugs against Primary Prostate Cancer and Bone Metastasis

Biological Relevance of RGD‐Integrin Subtype‐Specific Ligands in Cancer

Fluorescent cyclic peptides for cell imaging

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