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Novel Hyperpolarized Agents for Metabolic Imaging of Cancer

用于癌症代谢成像的新型超极化剂

基本信息

批准号：
8854604
负责人：
Kelvin L Billingsley
金额：
$ 15.4万
依托单位：
SAN FRANCISCO STATE UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2015
资助国家：
美国
起止时间：
2015-07-07 至 2018-06-30
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8854604
关键词：
Acids Animal Model Biology Biomedical Research Cancerous Carbon Carboxylic Acids Cell Survival Cell membrane Cell model Cells Characteristics Chemicals Chemistry Citric Acid Cycle Clinical Clinical Trials Drug Formulations Elements Energy Metabolism Environment Enzymes Evaluation Exhibits Foundations Fumarates Funding Glycolysis Goals Human Hydrolysis Hypoxia Image Individual Investigation LNCaP Label Magnetic Resonance Spectroscopy Malignant - descriptor Malignant Neoplasms Malignant neoplasm of prostate Mediating Medical Imaging Medicine Metabolic Metabolism Methods Mitochondria Modification Molecular Probes Molecular Structure Monitor NMR Spectroscopy New Agents Noise Nuclear Oxidative Phosphorylation PC3 cell line Partition Coefficient Permeability Pharmaceutical Chemistry Process Production Property Pyruvate Relaxation Research Sampling San Francisco Series Signal Transduction Students Succinates Technology Time Tissues Toxic effect Transmembrane Transport Tricarboxylic Acids Universities Warburg Effect analog base cancer cell cancer imaging chemical property chemical synthesis clinical application design esterase functional group imaging agent imaging probe in vivo innovation insight interest molecular imaging mouse model novel physical property preclinical evaluation programs prostate cancer cell line prostate cancer model public health relevance research study transgenic adenocarcinoma of mouse prostate tumor tumor metabolism underrepresented minority student uptake

项目摘要

DESCRIPTION (provided by applicant): We aim to develop molecular imaging agents for hyperpolarized 13C magnetic resonance spectroscopy (MRS) that effectively access the intracellular environment of malignant tissue and provide insight into the metabolic profile of tumors. A series of 13C-labeled analogs of tricarboxylic cycle intermediates, which exhibit enhanced cell permeability and are effectively metabolized, will be explored. Through chemical synthesis, systematic modification of carboxylic acid functional groups will yield the corresponding biologically cleavable carboxyl moieties and provide probes with the desired properties. These agents will be assessed to determine ideal candidates and subsequently be employed in hyperpolarized 13C MRS studies of tricarboxylic acid cycle metabolism in cellular and animal models of prostate cancer. New strategies for molecular probe delivery in hyperpolarized 13C MR spectroscopy will offer unique opportunities for targeting specific aspects of tumor metabolism, which will be of broad importance to medicinal chemistry, chemical biology, and medical imaging.

描述（由申请人提供）：我们的目标是开发用于超极化13 C磁共振波谱（MRS）的分子成像剂，其有效地进入恶性组织的细胞内环境，并提供对肿瘤代谢谱的洞察。将探索一系列13 C标记的三羧酸循环中间体类似物，它们表现出增强的细胞渗透性并被有效代谢。通过化学合成，羧酸官能团的系统修饰将产生相应的生物可裂解的羧基部分，并提供具有所需性质的探针。这些药物将进行评估，以确定理想的候选人，并随后在超极化13 C MRS研究的三羧酸循环代谢的细胞和动物模型的前列腺癌。在超极化13 C MR波谱中分子探针递送的新策略将为靶向肿瘤代谢的特定方面提供独特的机会，这将对药物化学、化学生物学和医学成像具有广泛的重要性。