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Drug Design: An 18F‐labeled caspase‐3‐sensitive nanoaggregation positron emission tomography tracer was prepared and evaluated for imaging the caspase‐3 activity in doxorubicin‐treated tumor xenografts. Enhanced retention of the 18F activity in apoptotic tumors is achieved through intramolecular macrocyclization and in situ aggregation upon caspase‐3 activation (see picture). [ABSTRACT FROM AUTHOR]

Wirkstoff ‐ Design: Ein 18F ‐ markiertes Nanoaggregat ‐ bildendes Capase ‐ 3 ‐ empfindliches Radiopharmakum für die Positronenemissionstomographie wurde hergestellt und die Abbildung der Caspase ‐ 3 ‐ Aktivität in Doxorubizin ‐ behandelten Tumorxenotransplantaten bewertet. Eine verstärkte Retention der 18F ‐ Aktivität in apoptotischen Tumoren wird durch intramolekulare Makrocyclisierung und In ‐ situ ‐ Aggregation nach der Caspase ‐ 3 ‐ Aktivierung erhalten (siehe Bild). [ABSTRACT FROM AUTHOR]

The caspase‐3 activity in doxorubicin‐treated tumor xenografts is studied by positron emission tomography (PET) using a novel 18F‐labeled caspase‐3‐sensitive nanoaggregation tracer. In their Communication on page 10511 ff., J. Rao, F. T. Chin, et al. show that the enzyme‐activatable tracer improves the PET imaging of apoptotic tumors by intramolecular macrocyclization and in situ aggregation of the cyclized tracer upon caspase‐3 activation. (Picture: Jim Strommer and Lydia‐Marie Joubert.) [ABSTRACT FROM AUTHOR]

Die Caspase ‐ 3 ‐ Aktivität in mit Doxorubicin behandelten Tumorxenotransplantaten wird unter Verwendung eines 18F ‐ markierten, für Caspase ‐ 3 empfindlichen Nanoaggregat ‐ bildenden Tracers mit Positronenemissionstomographie (PET) untersucht. In der Zuschrift auf S. 10705 ff. zeigen J. Rao, F. T. Chin et al., dass der Enzym ‐ aktivierbare Tracer durch intramolekulare Makrocyclisierung und In ‐ situ ‐ Aggregatbildung des cyclisierten Tracers nach Caspase ‐ 3 ‐ Aktivierung verfeinerte PET ‐ Bilder von apoptotischen Tumoren liefert. Bild: Jim Strommer und Lydia ‐ Marie Joubert. [ABSTRACT FROM AUTHOR]

Exposure to diesel particulate matter (DPM) is associated with several adverse health effects, including severe respiratory diseases. Quantitative analysis of DPM in vivo can provide important information on the behavior of harmful chemicals, as well as their toxicological impacts in living subjects. This study presents whole-body images and tissue distributions of DPM in animal models, using molecular imaging and radiolabeling techniques. The self-assembly of the 89Zr-labeled pyrene analog with a suspension of DPM efficiently produced 89Zr-incorporated DPM (89Zr-DPM). Positron emission tomography images were obtained for mice exposed to 89Zr-DPM via three administration routes: intratracheal, oral, and intravenous injection. DPM was largely distributed in the lungs and only slowly cleared after 7 days in mice exposed via the intratracheal route. In addition, a portion of 89Zr-DPM was translocated to other organs, such as the heart, spleen, and liver. Uptake values in these organs were also noticeable following exposure via the intravenous route. In contrast, most of the orally administered DPM was excreted quickly within a day. These results suggest that continuous inhalation exposure to DPM causes serious lung damage and may cause toxic effects in the extrapulmonary organs. [Display omitted] • A89Zr-labeling method was used for tracing diesel particulate matter (DPM) in mice. • 89Zr-incorporated DPM was administered in mice via three different routes. • When exposed via the intratracheal route, DPM was highly distributed in the lungs and excreted slowly. • Uptake in some organs such as spleen and heart were evident following intravenous exposure. • Most of the orally administered diesel particulates were cleared quickly in a day. [ABSTRACT FROM AUTHOR]