Browse
Submit Data
Databases
API
Help

Dataset Information

0 Views

0 Connections

0 Citations

0 Reanalyses

0 Downloads

Omics score: 0

A Gadolinium DO3A Amide m-Phenyl Boronic Acid MRI Probe for Targeted Imaging of Sialated Solid Tumors.

ABSTRACT: We developed a new probe, Gd-DO3A-Am-PBA, for imaging tumors. Our results showed active targeting of Gd-DO3A-Am-PBA to sialic acid (SA) moieties, with increased cellular labeling in vitro and enhanced tumor accumulation and retention in vivo, compared to the commercial Gadovist. The effectiveness of our newly synthesized probe lies in its adequate retention phase, which is expected to provide a suitable time window for tumor diagnosis and a faster renal clearance, which will reduce toxicity risks when translated to clinics. Hence, this study can be extended to other tumor types that express SA on their surface. Targeting and MR imaging of any type of tumors can also be achieved by conjugating the newly synthesized contrast agent with specific antibodies. This study thus opens new avenues for drug delivery and tumor diagnosis via imaging.

SUBMITTER: Rajan C

PROVIDER: S-EPMC8533322 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature

ACCESS DATA

Json Xml

Publications

A Gadolinium DO3A Amide <i>m</i>-Phenyl Boronic Acid MRI Probe for Targeted Imaging of Sialated Solid Tumors.

Rajan Christu C Seema Jaya J Chen Yu-Wen YW Chen Tsai-Chen TC Lin Ming-Huang MH Lin Chia-Huei CH Hwang Dennis Wen-Han DW

Biomedicines 20211013 10

We developed a new probe, Gd-DO3A-Am-PBA, for imaging tumors. Our results showed active targeting of Gd-DO3A-Am-PBA to sialic acid (SA) moieties, with increased cellular labeling in vitro and enhanced tumor accumulation and retention in vivo, compared to the commercial Gadovist. The effectiveness of our newly synthesized probe lies in its adequate retention phase, which is expected to provide a suitable time window for tumor diagnosis and a faster renal clearance, which will reduce toxicity risk ...[more]

PMID: 34680576

Similar Datasets

Imaging of Dysfunctional Elastogenesis in Atherosclerosis Using an Improved Gadolinium-Based Tetrameric MRI Probe Targeted to Tropoelastin.

Project description:Dysfunctional elastin turnover plays a major role in the progression of atherosclerotic plaques. Failure of tropoelastin cross-linking into mature elastin leads to the accumulation of tropoelastin within the growing plaque, increasing its instability. Here we present Gd4-TESMA, an MRI contrast agent specifically designed for molecular imaging of tropoelastin within plaques. Gd4-TESMA is a tetrameric probe composed of a tropoelastin-binding peptide (the VVGS-peptide) conjugated with four Gd(III)-DOTA-monoamide chelates. It shows a relaxivity per molecule of 34.0 ± 0.8 mM-1 s-1 (20 MHz, 298 K, pH 7.2), a good binding affinity to tropoelastin (KD = 41 ± 12 μM), and a serum half-life longer than 2 h. Gd4-TESMA accumulates specifically in atherosclerotic plaques in the ApoE-/- murine model of plaque progression, with 2 h persistence of contrast enhancement. As compared to the monomeric counterpart (Gd-TESMA), the tetrameric Gd4-TESMA probe shows a clear advantage regarding both sensitivity and imaging time window, allowing for a better characterization of atherosclerotic plaques.

| S-EPMC8558862 | biostudies-literature

Targeted immunotherapy for pediatric solid tumors.

Project description:Metastatic and refractory pediatric solid tumor malignancies continue to have a poor outcome despite the > 80% cure rates appreciated in many pediatric cancers. Targeted immunotherapy is impacting treatment and survival in these aggressive tumors. We review current promising immunotherapeutic approaches in the pediatric oncology solid tumor setting.

| S-EPMC4839383 | biostudies-literature

Optimization of ZD2 Peptide Targeted Gd(HP-DO3A) for Detection and Risk-Stratification of Prostate Cancer with MRI.

Project description:The aim of this work is to optimize a peptide targeted macrocyclic MRI contrast agent for detection and risk-stratification of aggressive prostate cancer. The optimized agent was prepared using click chemistry in the presence of CuSO4 and ascorbate at room temperature. The T1 and T2 relaxivities of ZD2-N3-Gd(HP-DO3A) are 5.44 and 7.10 mM-1 s-1 at 1.4 T, and 5.53 and 7.81 mM-1 s-1 at 7 T, respectively, higher than the previously reported ZD2-Gd(HP-DO3A). The specific tumor enhancement of the agent was investigated in male nude mice bearing aggressive PC3 human prostate cancer xenografts and slow-growing LNCaP tumor xenografts. Contrast enhanced MR images were acquired using a 2D spin-echo sequence and a 3D FLASH sequence with a 7 T small animal scanner. ZD2-N3-Gd(HP-DO3A) produced robust contrast enhancement in aggressive PC3 tumors and little enhancement in slow-growing LNCaP tumors. It produced 400% and 100% CNR increases in the T1-weighted 2D spin-echo MR images and 3D FLASH images of PC3 tumors, respectively, for at least 30 min at a dose of 0.1 mmol/kg. In contrast, less than 20% CNR increase was observed in the LNCaP tumors with both sequences. The optimized targeted contrast agent has higher relaxivities and are effective to detect aggressive PC3 tumors and differentiate the aggressive cancer from the slow-growing LNCaP prostate cancer in contrast enhanced MRI. ZD2-N3-Gd(HP-DO3A) has the promise for accurate detection and risk-stratification of aggressive prostate cancer.

| S-EPMC6047029 | biostudies-literature

2,4-Dibutoxy-phenyl-boronic acid.

Project description:In the crystal of the title compound, C(14)H(23)BO(4), centrosymmetric dimers linked by pairs of O-H⋯O hydrogen bonds occur. The dimers are linked via C-H⋯O contacts, generating a two-dimensional array parallel to (12). These are inter-connected by weak O-H⋯O hydrogen bonds, as well as C-H⋯π inter-actions.

| S-EPMC2969364 | biostudies-literature

2,4-Difluoro-phenyl-boronic acid.

Project description:The mol-ecular structure of the title compound, C(6)H(5)BF(2)O(2), is essentially planar (mean deviation = 0.019 Å), indicating electronic delocalization between the dihydroxy-boryl group and the aromatic ring. In the crystal structure, inversion dimers linked by two O-H⋯O hydrogen bonds arise. An intra-molecular O-H⋯F hydrogen bond reinforces the conformation and the same H atom is also involved in an inter-molecular O-H⋯F link, leading to mol-ecular sheets in the crystal.

| S-EPMC2967960 | biostudies-literature

Mesothelin-Targeted Recombinant Immunotoxins for Solid Tumors.

Project description:Mesothelin (MSLN) is a cell surface glycoprotein normally expressed only on serosal surfaces, and not found in the parenchyma of vital organs. Many solid tumors also express MSLN, including mesothelioma and pancreatic adenocarcinoma. Due to this favorable expression profile, MSLN represents a viable target for directed anti-neoplastic therapies, such as recombinant immunotoxins (iToxs). Pre-clinical testing of MSLN-targeted iTox's has yielded a strong body of evidence for activity against a number of solid tumors. This has led to multiple clinical trials, testing the safety and efficacy of the clinical leads SS1P and LMB-100. While promising clinical results have been observed, neutralizing anti-drug antibody (ADA) formation presents a major challenge to overcome in the therapeutic development process. Additionally, on-target, off-tumor toxicity from serositis and non-specific capillary leak syndrome (CLS) also limits the dose, and therefore, impact anti-tumor activity. This review summarizes existing pre-clinical and clinical data on MSLN-targeted iTox's. In addition, we address the potential future directions of research to enhance the activity of these anti-tumor agents.

| S-EPMC7408136 | biostudies-literature

3-Amino-phenyl-boronic acid monohydrate.

Project description:In the title compound, C(6)H(8)BNO(2)·H(2)O, the almost planar boronic acid mol-ecules (r.m.s. deviation = 0.044 Å) form inversion dimers, linked by pairs of O-H⋯O hydrogen bonds. The water mol-ecules link these dimers into [100] chains by way of O-H⋯O hydrogen bonds, and N-H⋯O links generate (100) sheets.

| S-EPMC2979464 | biostudies-literature

Targeted Therapies in Older Adults With Solid Tumors.

Project description: Not available

| S-EPMC8260907 | biostudies-literature

Immunotherapies for Pediatric Solid Tumors: A Targeted Update.

Project description:There are encouraging signs in our collective progress to leverage the immune system to treat pediatric cancers. Here, we summarize interim successes in cancer immunotherapy and opportunities to translate from the adult world to pediatrics, and highlight challenges that could benefit from additional development, focusing on solid tumors. Just a decade ago, other than antibodies targeting disialoganglioside (GD2) in neuroblastoma, pediatric cancer immunotherapy was mostly relegated to obscure preclinical studies in a few academic labs. Today there are numerous clinical trials of a variety of antibody, cellular, gene, and viral therapies and vaccines designed to either promote antitumor immunity or specifically attack validated immunotherapy targets. Understanding those targets and their pediatric relevance is paramount. While much work is underway to evaluate the utility of numerous immunologic targets, the lack of regulatory approvals is emblematic of the challenges that remain. Herein we focus our review on the most promising targeted immunotherapies in clinical trials for children.

| S-EPMC8613512 | biostudies-literature

Amide Proton Transfer-weighted MRI in the Diagnosis of Major Salivary Gland Tumors.

Project description:Amide proton transfer-weighted magnetic resonance imaging (APTw-MRI), which is effective in tumor characterization, has expanded its role in the head and neck. We aimed to evaluate the diagnostic ability of APTw-MRI in differentiating malignant from benign major salivary gland tumors compared with diffusion-weighted imaging (DWI) and dynamic contrast-enhanced (DCE)-MRI. Between December 2017 and November 2018, 38 subjects, who were diagnosed with major salivary gland tumors and who underwent preoperative 3 T MRI, including APTw-MRI, DWI, and DCE-MRI, were included in this retrospective study. Twenty-three subjects had benign tumors, and fifteen had malignancies. APTw-signals of the tumors were measured and compared according to the histopathological diagnosis. Using receiver operating characteristic curve analysis, diagnostic performance of APTw-MRI was evaluated and compared with DWI and DCE-MRI using DeLong test. The maximum, mean, and median APTw-signals were significantly higher in malignant than in benign tumors (P < 0.001). The mean and maximum APTw-signals showed excellent area under the curve for predicting malignant tumors (0.948 and 0.939), which were significantly higher than the combining use of DWI and DCE-MRI (0.780) (P = 0.021 and 0.028). Therefore, APTw-MRI could be a useful tool for differentiating malignant from benign major salivary gland tumors, and can be applicable in the clinical setting.

| S-EPMC6554276 | biostudies-literature

OmicsDI is part of the ELIXIR infrastructure

OmicsDI is an Elixir interoperability service. Learn more ›

Tweets

OmicsDI Databases

PRIDE
PeptideAtlas
MassIVE
JPOST Repository
Physiome Model Repository

EGA
EVA
ENA
LINCS
PAXDB
Cell Collective

MetaboLights
Metabolomics Workbench
MetabolomeExpress
GNPS
BioModels
FAIRDOMHub

ArrayExpress
dbGaP
ExpressionAtlas
GEO
NODE

Information

Databases
Help
API
Contact us
Code on GitHub
Terms of use
Submit Data