Positron emission tomography (PET) imaging of Colony Stimulating Factor 1 Receptor (CSF1R) is a new strategy for quantifying both neuroinflammation and inflammation in the periphery since CSF1R is expressed on microglia and macrophages. AZ683 has high affinity for CSF1R (K = 8 nM; IC = 6 nM) and >250-fold selectivity over 95 other kinases. In this paper, we report the radiosynthesis of [C]AZ683 and initial evaluation of its use in CSF1R PET. [C]AZ683 was synthesized by C-methylation of the desmethyl precursor with [C]MeOTf in 3.0% non-corrected activity yield (based upon [C]MeOTf), >99% radiochemical purity and high molar activity. Preliminary PET imaging with [C]AZ683 revealed low brain uptake in rodents and nonhuman primates, suggesting that imaging neuroinflammation could be challenging but that the radiopharmaceutical could still be useful for peripheral imaging of inflammation.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316681 | PMC |
| http://dx.doi.org/10.3390/ph11040136 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Naringenin, a Food Bioactive Compound, Reduces Oncostatin M Through Blockade of PI3K/Akt/NF-κB Signal Pathway in Neutrophil-like Differentiated HL-60 Cells.
Foods
January 2025
Center for Converging Humanities, Kyung Hee University, Seoul 02447, Republic of Korea.
Oncostatin M (OSM) plays a crucial role in diverse inflammatory reactions. Although the food bioactive compound naringenin (NAR) exerts various useful effects, including antitussive, anti-inflammatory, hepatoprotective, renoprotective, antiarthritic, antitumor, antioxidant, neuroprotective, antidepressant, antinociceptive, antiatherosclerotic, and antidiabetic effects, the modulatory mechanism of NAR on OSM expression in neutrophils has not been specifically reported. In the current work, we studied whether NAR modulates OSM release in neutrophil-like differentiated (d)HL-60 cells.
View Article and Find Full Text PDFEngineered GM-CSF polarizes protumorigenic tumor-associated macrophages to an antitumorigenic phenotype and potently synergizes with IL-12 immunotherapy.
J Immunother Cancer
December 2024
Pritzker School of Molecular Engineering, The University of Chicago, Chicago, Illinois, USA
Background: The use of immune checkpoint inhibitors (CPIs) has become a dominant regimen in modern cancer therapy, however immune resistance induced by tumor-associated macrophages (TAMs) with immune suppressive and evasion properties limits responses. Therefore, the rational design of immune modulators that can control the immune suppressive properties of TAMs and polarize them, as well as dendritic cells (DCs), toward a more proinflammatory phenotype is a principal objective in cancer immunotherapy.
Methods: Here, using a protein engineering approach to enhance cytokine residence in the tumor microenvironment, we examined combined stimulation of the myeloid compartment via tumor stroma-binding granulocyte-macrophage colony-stimulating factor (GM-CSF) to enhance responses in both DCs and T cells via stroma-binding interleukin-12 (IL-12).
Neutropenic event incidence in women with early-stage breast cancer receiving neoadjuvant or adjuvant chemotherapy: a retrospective study.
BMJ Support Palliat Care
January 2025
Department of Oncology, County Hospital Ryhov, Jönköping, Jonkoping County, Sweden
Neutropenia is a common chemotherapy-induced symptom that can lead to febrile neutropenia (FN) and infection. The aim of this study was to assess the incidence of neutropenia, FN, documented infection with neutropenia and fever associated with early-stage breast cancer (BC) in a real-life setting. This retrospective study includes 88 women with early-stage BC who received a first dose of epirubicin plus cyclophosphamide with or without 5-fluorouracil.
View Article and Find Full Text PDFSpontaneous Remission of Pneumocystis jirovecii Pneumonia Followed by Severe Pulmonary Nocardiosis in a Patient with HIV Infection: A Case Report.
J Infect Chemother
January 2025
Department of Respiratory Medicine, Hamamatsu Medical Center, Hamamatsu, Japan.
We describe a rare case of spontaneous remission of Pneumocystis jirovecii pneumonia (PCP) in a 42-year-old patient with human immunodeficiency virus (HIV) infection, followed by severe pulmonary nocardiosis. To our knowledge, this is the first report of spontaneous remission of PCP in a completely untreated patient with HIV infection. The patient, a bisexual Japanese man, presented with fever and anorexia and had a history of non-compliance with antiretroviral therapy (ART) for 13 years.
View Article and Find Full Text PDFDevelopmental delay and its associated factors among children of 9 months and of 18 months attending primary health facilities in an urban resettlement area of East Delhi.
J Family Med Prim Care
December 2024
Department of Pediatrics, University College of Medical Sciences and Guru Teg Bahadur Hospital, New Delhi, India.
Background: Early identification of developmental delay in children can help in making early intervention for its management. Routine developmental screening is not being practised in India due to lack of trained field workers, lack of awareness among parents and lack of feasible assessment screening tool. There is lack of studies that focuses on home environment provided to the children as it is associated with developmental delay.
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!