Synthesis and Evaluation of a Dimeric RGD Peptide as a Preliminary Study for Radiotheranostics with Radiohalogens

Echigo, Hiroaki; Mishiro, Kenji; Fuchigami, Takeshi; Shiba, Kazuhiro; Kinuya, Seigo; Ogawa, Kenji

doi:10.3390/molecules26206107

Cited by 7 publications

(3 citation statements)

References 26 publications

(41 reference statements)

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“…The affinity of deltic c(RGDyK) ( 1 ), c(deltic RGDyK) ( 3 ), and c(KGDyK) ( 8 ) for α v β 3 integrin was evaluated through a competitive binding assay between the peptides and [ 125 I]c[RGDy(3-I)V] using U-87 MG cells, which overexpress α v β 3 integrin, as previously reported. 17,18 Fig. 3 shows the representative results of the assay.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

et al. 2023

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Section: Resultsmentioning

confidence: 99%

Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

et al. 2023

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“…42 Cyclic RGD pentapeptide (Arg-Gly-Asp-Phe-Lys) (RGDfK) has high metabolic stability and selectively binds with ανβ3 integrin that is overexpressed in angiogenic vessels and certain cancer cells with high affinity. [43][44][45][46][47][48] Liu et al successfully induced the conventional surface modification of liposomes using RGDfK cyclic peptide for the targeted delivery. 21,39 Therefore, RGDfK was selected as the targeting group of NV, depicting active targeting characteristics.…”

Section: Introductionmentioning

confidence: 99%

Engineered Polymeric Nanovector for Intracellular Peptide Delivery in Antitumor Therapy

Zhang,

Huang

et al. 2023

IJN

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This study aimed to deliver a polypeptide from the Bax-BH3 domain (BHP) through the synthesis of self-assembled amphiphile nanovectors (NVs) and to assess their potential for cancer therapeutic applications and biological safety in vitro and in vivo. These findings provide valuable options for cancer intervention and a novel approach for the rational design of therapeutics. Methods: We studied the antitumor activity of BHP by preparing RGDfK-PHPMA-b-Poly (MMA-alt-(Rhob-MA)) (RPPMMRA) and encapsulating it in BHP-NV. We also performed a series of characterizations and property analyses of RPPMMRA, including its size, stability, and drug-carrying capacity. The biocompatibility of RPPMMRA was evaluated in terms of cytotoxicity and hemolytic effects. The pro-apoptotic capacity of BHP was evaluated in vitro using mitochondrial membrane potential, flow cytometry, and apoptosis visualization techniques. The potential therapeutic effects of BHP on tumors were explored using reverse molecular docking. We also investigated the in vivo proapoptotic effect of BHP-NV in a nude mouse tumor model. Results: NVs were successfully prepared with hydrated particle sizes ranging from 189.6 nm to 256.6 nm, spherical overall, and were able to remain stable in different media for 72 h with drug loading up to 15.2%. The NVs were be successfully internalized within 6 h with good biocompatibility. Neither BHP nor NV showed significant toxicity when administered alone, however, BHP-NV demonstrated significant side effects in vitro and in vivo. The apoptosis rate increased significantly from 14.13% to 66.34%. Experiments in vivo showed that BHP-NV exhibited significant apoptotic and tumor-suppressive effects. Conclusion: A targeted fluorescent NV with high drug delivery efficiency and sustained release protected the active center of BHP, constituting BHP-NV for targeted delivery. RPPMMRA demonstrated excellent biocompatibility, stability, and drug loading ability, whereas and BHP-NV demonstrated potent antitumor effects in vivo and in vitro.

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“…Cyclic pentapeptides that contain an RGD sequence are typical ligands with high affinity for α v β 3 integrin as it is highly expressed on endothelial cells during neovascularization and on some cancer cells . Therefore, many radiolabeled RGD peptides were investigated for tumor imaging and therapy in nuclear medicine, − and RGD peptides were used as carriers for anticancer drugs . Thus, this study used c(RGDfK) as a carrier molecule for cancer therapeutics.…”

Section: Introductionmentioning

confidence: 99%

RGD Peptide-Conjugated Dodecaborate with the Ga-DOTA Complex: A Preliminary Study for the Development of Theranostic Agents for Boron Neutron Capture Therapy and Its Companion Diagnostics

et al. 2022

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A boron neutron capture therapy (BNCT) system, using boron-10-introduced agents coupled with companion diagnostics, is anticipated as a promising cancer theranostic. Thus, this study aimed to synthesize and evaluate a probe closo-dodecaborate-(Ga-DOTA)-c(RGDfK) (16) [Ga = gallium, DOTA =1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, and c(RGDfK) = cyclo(arginine-glycine-aspartate-d-phenylalanine-lysine] containing closo-dodecaborate ([B12H12]2–) as a boron cluster, a [67Ga]Ga-DOTA derivative for nuclear medicine imaging, and an RGD peptide for tumor targeting. Moreover, we prepared a radioiodinated probe [125I]17 in which I-125 is introduced into a closo-dodecaborate moiety of 16. [67Ga]16 and [125I]17 showed high stability and high uptake in cancer cells in vitro. Biodistribution experiments in tumor-bearing mice revealed similar biodistribution patterns between [67Ga]16 and [125I]17, such as a high uptake in the tumor and a low uptake in other non-target tissues. Meanwhile, [125I]17 exhibited higher accumulation in most tissues, including the tumor, than [67Ga]16, probably because of higher albumin binding. The higher the [125I]17 accumulation in the tumor, the more desirable it is for BNCT, with the possibility that the iodo-closo-dodecaborate site may work as an albumin binder.

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Synthesis and Evaluation of a Dimeric RGD Peptide as a Preliminary Study for Radiotheranostics with Radiohalogens

Cited by 7 publications

References 26 publications

Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

Engineered Polymeric Nanovector for Intracellular Peptide Delivery in Antitumor Therapy

RGD Peptide-Conjugated Dodecaborate with the Ga-DOTA Complex: A Preliminary Study for the Development of Theranostic Agents for Boron Neutron Capture Therapy and Its Companion Diagnostics

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