Kenji Mishiro
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View article: Development of theranostic agents combined with nuclear medicine imaging and boron neutron capture therapy (BNCT) for bone metastases of cancer
Development of theranostic agents combined with nuclear medicine imaging and boron neutron capture therapy (BNCT) for bone metastases of cancer Open
View article: Comparison of Technetium-99m-Labeled Pentapeptides as Bone Imaging Agents: Influence of Different Types of Acidic Amino Acids
Comparison of Technetium-99m-Labeled Pentapeptides as Bone Imaging Agents: Influence of Different Types of Acidic Amino Acids Open
Bone-seeking radiopharmaceuticals are essential for the early detection of bone metastases. In this study, we developed three Technetium-99m (99mTc)-labeled oligopeptides composed of acidic amino acids and evaluated their bone-t…
View article: Evaluation of an 211At-labeled RGD peptide in an orthotopic glioblastoma model by targeted alpha therapy
Evaluation of an 211At-labeled RGD peptide in an orthotopic glioblastoma model by targeted alpha therapy Open
[211At]1 is a promising candidate for targeted alpha therapy in glioblastoma.
View article: Development of a Theranostic Agent for Bone Metastases: Integration of Nuclear Medicine Imaging and Boron Neutron Capture Therapy (BNCT)
Development of a Theranostic Agent for Bone Metastases: Integration of Nuclear Medicine Imaging and Boron Neutron Capture Therapy (BNCT) Open
Boron neutron capture therapy (BNCT) is one of the promising cancer treatment methods with 10B-labeled compounds and neutron irradiation. The 10B(n,α)7Li reaction produces a 7Li nucleus and an α-…
View article: Combination therapy of an 211At-labeled RGD peptide and immune checkpoint blockade to enhance antitumor efficacy
Combination therapy of an 211At-labeled RGD peptide and immune checkpoint blockade to enhance antitumor efficacy Open
View article: Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics
Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics Open
The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated that 4-(p-astatophenyl)butyric acid (APBA), an albumin-binding moiety (ABM) labeled with astati…
View article: Light‐Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions
Light‐Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions Open
Phosphate and sulfate groups play an important role in controlling the physical properties of biomolecules and artificial materials. However, despite their significance, the incorporation of phosphate or sulfate groups into aqueous organic…
View article: Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions
Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions Open
Phosphate and sulfate groups play an important role in controlling the physical properties of biomolecules and artificial materials. However, despite their significance, the incorporation of phosphate or sulfate groups into aqueous organic…
View article: Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions
Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions Open
Phosphate and sulfate groups play an important role in controlling the physical properties of biomolecules and artificial materials. However, despite their significance, the incorporation of phosphate or sulfate groups into aqueous organic…
View article: Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions
Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions Open
Phosphate and sulfate groups play an important role in controlling the physical properties of biomolecules and artificial materials. However, despite their significance, the incorporation of phosphate or sulfate groups into aqueous organic…
View article: Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions
Light-Induced Conjugation of Inorganic Phosphate and Sulfate with Aminocyclobutenediones under Aqueous Conditions Open
Phosphate and sulfate groups play an important role in controlling the physical properties of biomolecules and artificial materials. However, despite their significance, the incorporation of phosphate or sulfate groups into aqueous organic…
View article: Differences in the Renal Accumulation of Radiogallium-Labeled (Glu)14 Peptides Containing Different Optical Isomers of Glutamic Acid
Differences in the Renal Accumulation of Radiogallium-Labeled (Glu)14 Peptides Containing Different Optical Isomers of Glutamic Acid Open
Acidic amino acid peptides have a high affinity for bone. Previously, we demonstrated that radiogallium complex-conjugated oligo-acidic amino acids possess promising properties as bone-seeking radiopharmaceuticals. Here, to elucidate the e…
View article: Optimizing the pharmacokinetics of an 211At-labeled RGD peptide with an albumin-binding moiety via the administration of an albumin-binding inhibitor
Optimizing the pharmacokinetics of an 211At-labeled RGD peptide with an albumin-binding moiety via the administration of an albumin-binding inhibitor Open
Purpose A probe for targeted alpha therapy (TAT) using the RGD peptide (Ga-DOTA-K([ 211 At]APBA)-c(RGDfK) ([ 211 At] 1 )) with albumin-binding moiety (ABM) was recently developed. [ 211 At] 1 highly accumulated in tumors and significantly …
View article: Synthesis and evaluation of a rociletinib analog as prospective imaging double mutation L858R/T790M in non-small cell lung cancer
Synthesis and evaluation of a rociletinib analog as prospective imaging double mutation L858R/T790M in non-small cell lung cancer Open
Context: Imaging the mutation status of non-small cell lung cancer (NSCLC) using radiolabeled tyrosine kinase inhibitor (TKI) analogs has garnered interest due to their unique interactions with the target epidermal growth factor receptor (…
View article: Phototriggered Butenolide Formation from a Cyclobutenedione and an Acidic Nucleophile
Phototriggered Butenolide Formation from a Cyclobutenedione and an Acidic Nucleophile Open
A phototriggered conjugation reaction of an aminocyclobutenedione and a nucleophile was discovered. Upon irradiation of the materials with a blue LED, a butenolide derivative with substituents derived from the aminocyclobutenedione and the…
View article: Synthesis and initial <i>in vitro</i> evaluation of olmutinib derivatives as prospective imaging probe for non-small cell lung cancer
Synthesis and initial <i>in vitro</i> evaluation of olmutinib derivatives as prospective imaging probe for non-small cell lung cancer Open
Introduction: Imaging a non-small cell lung cancer (NSCLC) using radiolabeled tyrosine kinase inhibitors (TKIs) has attracted attention due to their unique interaction with the target epidermal growth factor receptor (EGFR). Olmutinib (OTB…
View article: Epitope-Based Specific Antibody Modification
Epitope-Based Specific Antibody Modification Open
Modified antibodies play essential roles in various fields, such as analysis, diagnosis, and therapy, which require modified antibodies with optimal physical and biological properties. To this aim, the development of methods for site-selec…
View article: Preparation and Evaluation of Thermosensitive Liposomes Encapsulating I-125-Labeled Doxorubicin Derivatives for Auger Electron Therapy
Preparation and Evaluation of Thermosensitive Liposomes Encapsulating I-125-Labeled Doxorubicin Derivatives for Auger Electron Therapy Open
Auger electrons (AEs) are very low-energy electrons emitted by radionuclides such as I-125 (125I). This energy is deposited across a small distance (<0.5 μm), resulting in high linear energy transfer that is potent for causing lethal damag…
View article: Discovery of a Novel Aminocyclopropenone Compound That Inhibits BRD4-Driven Nucleoporin NUP210 Expression and Attenuates Colorectal Cancer Growth
Discovery of a Novel Aminocyclopropenone Compound That Inhibits BRD4-Driven Nucleoporin NUP210 Expression and Attenuates Colorectal Cancer Growth Open
Epigenetic deregulation plays an essential role in colorectal cancer progression. Bromodomains are epigenetic “readers” of histone acetylation. Bromodomain-containing protein 4 (BRD4) plays a pivotal role in transcriptional regulation and …
View article: Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics Open
[ 125 I]15 and [ 125 I]17 exhibited high uptake in the tumor and low uptake in non-target tissues, indicating that [ 123/131 I]15 and [ 123/131 I]17 are promising compounds to be used as imaging and therapeutic probes for sigma receptor-po…
View article: Synthesis and evaluation of radiolabeled porphyrin derivatives for cancer diagnoses and their nonradioactive counterparts for photodynamic therapy
Synthesis and evaluation of radiolabeled porphyrin derivatives for cancer diagnoses and their nonradioactive counterparts for photodynamic therapy Open
The prepared radiolabeled porphyrin derivatives showed high accumulation in tumor tissues and good phototoxicities indicating their potential for cancer theranostics.
View article: Synthesis and evaluation of radiogallium-labeled long-chain fatty acid derivatives as myocardial metabolic imaging agents
Synthesis and evaluation of radiogallium-labeled long-chain fatty acid derivatives as myocardial metabolic imaging agents Open
Since long-chain fatty acids work as the primary energy source for the myocardium, radiolabeled long-chain fatty acids play an important role as imaging agents to diagnose metabolic heart dysfunction and heart diseases. With the aim of dev…
View article: Synthesis and Evaluation of a Dimeric RGD Peptide as a Preliminary Study for Radiotheranostics with Radiohalogens
Synthesis and Evaluation of a Dimeric RGD Peptide as a Preliminary Study for Radiotheranostics with Radiohalogens Open
We recently developed 125I- and 211At-labeled monomer RGD peptides using a novel radiolabeling method. Both labeled peptides showed high accumulation in the tumor and exhibited similar biodistribution, demonstrating their usefulness for ra…
View article: A Radiobrominated Tyrosine Kinase Inhibitor for EGFR with L858R/T790M Mutations in Lung Carcinoma
A Radiobrominated Tyrosine Kinase Inhibitor for EGFR with L858R/T790M Mutations in Lung Carcinoma Open
Activating double mutations L858R/T790M in the epidermal growth factor receptor (EGFR) region are often observed as the cause of resistance to tyrosine kinase inhibitors (TKIs). Third-generation EGFR-TKIs, such as osimertinib and rociletin…
View article: Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor Receptor β (PDGFRβ) Imaging: Influence of Different Linkers
Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor Receptor β (PDGFRβ) Imaging: Influence of Different Linkers Open
The purpose of this study is to develop peptide-based platelet-derived growth factor receptor β (PDGFRβ) imaging probes and examine the effects of several linkers, namely un-natural amino acids (D-alanine and β-alanine) and ethylene-glycol…
View article: Decreasing undesirable absorbed radiation to the intestine after administration of radium-223 dichloride for treatment of bone metastases
Decreasing undesirable absorbed radiation to the intestine after administration of radium-223 dichloride for treatment of bone metastases Open
View article: Synthesis and Fundamental Evaluation of Radioiodinated Rociletinib (CO-1686) as a Probe to Lung Cancer with L858R/T790M Mutations of Epidermal Growth Factor Receptor (EGFR)
Synthesis and Fundamental Evaluation of Radioiodinated Rociletinib (CO-1686) as a Probe to Lung Cancer with L858R/T790M Mutations of Epidermal Growth Factor Receptor (EGFR) Open
Rociletinib (CO-1686), a 2,4-diaminopyrimidine derivative, is a highly potent tyrosine kinase inhibitor (TKI) that acts on epidermal growth factor receptor (EGFR) with L858R/T790M mutations. We supposed radioiodinated CO-1686 would functio…
View article: Phototriggered Functionalization of a Carboxy Group Using a Tetrazole
Phototriggered Functionalization of a Carboxy Group Using a Tetrazole Open
A phototriggered functionalization reaction of a carboxy group using a tetrazole was recently reinvestigated as a useful method for functionalization of proteins and polymer materials in aqueous media. Irradiation of a tetrazole generates …
View article: Radiotheranostics Coupled between an At-211-Labeled RGD Peptide and the Corresponding Radioiodine-Labeled RGD Peptide
Radiotheranostics Coupled between an At-211-Labeled RGD Peptide and the Corresponding Radioiodine-Labeled RGD Peptide Open
Alpha particle-emitting radionuclides have gained considerable attention for radionuclide therapy. Astatine-211 (211At) is a promising alpha particle-emitting radionuclide. 211At is a halogen that has similar chemical properties to iodine …
View article: Radiobrominated benzimidazole-quinoline derivatives as Platelet-derived growth factor receptor beta (PDGFRβ) imaging probes
Radiobrominated benzimidazole-quinoline derivatives as Platelet-derived growth factor receptor beta (PDGFRβ) imaging probes Open