Achieving high-yielding, robust, and reproducible chemistry is a prerequisite for the (18)F-labeling of peptides for quantitative receptor imaging using positron emission tomography (PET). In this study, we extend the toolbox of oxime chemistry to include the novel prosthetic groups [(18)F]-(2-{2-[2-(2-fluoroethoxy)ethoxy]ethoxy}ethoxy)acetaldehyde, [(18)F]5, and [(18)F]-4-(3-fluoropropoxy)benzaldehyde, [(18)F]9, in addition to the widely used 4-[(18)F]fluorobenzaldehyde, [(18)F]12. The three (18)F-aldehydes were conjugated to the same aminooxy-bearing RGD peptide and the effect of the prosthetic group on biodistribution and tumor uptake studied in mice. The peptide conjugate [(18)F]7 was found to possess superior in vivo pharmacokinetics with higher tumor to blood, tumor to liver, tumor to muscle, and tumor to lung ratios than either [(18)F]10 or [(18)F]13. The radioactivity from the [(18)F]7 conjugate excreted more extensively through the kidney route with 79%id passing through the urine and bladder at the 2 h time point compared to around 55%id for the more hydrophobic conjugates [(18)F]10 and [(18)F]13. The chemical nature of a prosthetic group can be employed to tailor the overall biodistribution profile of the radiotracer. In this example, the hydrophilic nature of the ethylene glycol containing prosthetic group [(18)F]5 clearly influences the overall excretion pattern for the RGD peptide conjugate.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/bc700472w | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Background: There has been an increase in both primary anatomic (aTSA) and reverse total shoulder arthroplasty (rTSA) over the last decade, with rates peaking for patients aged 75 years and older. Despite aTSA being the mainstay of treatment for patients with glenohumeral arthritis in the absence of rotator cuff insufficiency, there has been an upward trend of rTSA utilization in the elderly due to concerns about rotator cuff integrity, regardless of deformity. The purpose of this study is to evaluate outcomes including pain, function, range of motion, satisfaction, and complications in patients 80 years or older following primary anatomic and reverse total shoulder arthroplasty for osteoarthritis without full thickness rotator cuff tears.
View Article and Find Full Text PDFMicrobial Adhesion and Cytotoxicity of Heat-Polymerized and 3D-Printed Denture Base Materials when Modified with Dimethylaminohexadecyl Methacrylate and/or 2-Methacryloyloxyethyl Phosphorylcholine as Antimicrobial and Protein-Repellent Materials.
Polymers (Basel)
January 2025
Department of Advanced Oral Sciences and Therapeutics, University of Maryland School of Dentistry, Baltimore, MD 21201, USA.
Background: Polymethyl methacrylate (PMMA) is ideal for denture bases but is prone to biofilm accumulation, leading to denture stomatitis (DS), often involving . Dimethylaminohexadecyl methacrylate (DMAHDM) and 2-methacryloyloxyethyl phosphorylcholine (MPC) are introduced into dental materials for their antimicrobial and protein-repellent properties. This study investigates the effects of incorporating dimethylaminohexadecyl methacrylate (DMAHDM) and 2-methacryloyloxyethyl phosphorylcholine (MPC) into heat-polymerized (HP) and 3D-printed (3DP) denture base resins on microbial adhesion and cytotoxicity.
View Article and Find Full Text PDFFully Automated Production of ((()-1-Carboxy-5-(6-([F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic Acid ([F]JK-PSMA-7).
Pharmaceuticals (Basel)
January 2025
Forschungszentrum Jülich GmbH, Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Wilhelm-Johnen-Str., 52428 Jülich, Germany.
The radiotracer [F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an F-labeled active ester as a prosthetic group, which had to be isolated and purified before it could be linked to the pharmacologically active Lys-urea-Glu motif. Although this procedure could be automated on two-reactor modules like the GE TRACERLab FX2N (FXN) to afford the tracer in modest radiochemical yields (RCY) of 18-25%, it is unsuitable for cassette-based systems with a single reactor. To simplify implementation on an automated synthesis module, the radiosynthesis of [F]JK-PSMA-7 was devised as a one-pot, two-step reaction.
View Article and Find Full Text PDFDental Rehabilitation After Microvascular Reconstruction of Segmental Jaw Defects: A Ten-Year Follow-Up.
J Clin Med
January 2025
Department of Oral and Maxillofacial Surgery, University Hospital of Salzburg, Paracelsus Medical University, 5020 Salzburg, Austria.
: Defects in maxillary and mandibular continuity are common in maxillofacial practice. They can occur after trauma, osteonecrosis, congenital jaw deformities, or surgical resection of benign or malignant tumours. Reconstruction with microvascular bone flaps and subsequent prosthetic rehabilitation is considered the contemporary first line treatment.
View Article and Find Full Text PDFNational Trends in Racial and Ethnic Disparities in Mortality from Mechanical Complications of Cardiac Valves and Grafts (1999-2020).
J Clin Med
January 2025
Division of Cardiothoracic Surgery, Department of Surgery, Pauley Heart Center, Virginia Commonwealth University School of Medicine, Richmond, VA 23298, USA.
: The volume of cardiac valve and coronary artery revascularization procedures is rising in the United States. This cross-sectional study explores ethnic disparities in mortality in cardiac surgery attributed to mechanical failures of implantable heart valves and coronary artery grafts. : We used the CDC Wide-Ranging Online Data for Epidemiologic Research Multiple Causes of Death database to identify patients whose single cause of death was categorized by complications of cardiovascular prosthetic devices, implants, and grafts (ICD-10 code T82) between 1999 and 2020.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!