1-[4-(Bromomethyl)phenyl]-1,2,2-triphenylethene (2) was synthesized and evaluated for specific fluorescent prestaining of proteins containing cysteine (Cys) in SDS-PAGE. The molecule showed classic aggregation-induced emission (AIE) property in protein labeling and its quantum efficiency was further enhanced upon reacting with Cys. The parameters of reaction such as labeling time and concentration of dye and reducing reagent-tris(2-carboxyethyl)phosphine (TCEP) were examined to obtain the optimal labeling condition. In addition to its specific labeling effect, molecule 2 also showed its advantage over traditional self-quenching dyes through labeling Cys containing BSA with different dye/Cys ratios.
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http://dx.doi.org/10.1021/am401486h | DOI Listing |
MAGMA
January 2025
Medical Physics Group, Institute of Diagnostic and Interventional Radiology, Jena University Hospital, Friedrich Schiller University Jena, Jena, Germany.
Objective: To establish an arterial spin labeling (ASL) protocol for rat livers that improves data reliability and reproducibility for perfusion quantification.
Methods: This study used respiratory-gated, single-slice, FAIR-based ASL imaging with multiple inversion times (TI) in rat livers. Quality assurance measures included: (1) introduction of mechanical ventilation to ensure consistent respiratory cycles by controlling the respiratory rate (45 bpm), tidal volume (10 ml/kg), and inspiration: expiration ratio (I:E ratio, 1:2), (2) optimization of the trigger window for consistent trigger points, and (3) use of fit residual map and coefficient of variance as metrics to assess data quality.
Cancer Chemother Pharmacol
January 2025
Clinical Pharmacology and Translational Sciences, Pfizer Worldwide R&D, 10555 Science Center Drive, San Diego, CA, 92121, USA.
As development of new oncology small molecule therapies is focused mainly on molecularly targeted agents, the dose selection paradigm has shifted from the maximum tolerated dose (MTD)-based approach traditionally utilized with cytotoxic drugs towards determining an optimal dose with long-term tolerability while maintaining efficacy. To assess overall tolerability in recently approved oncology small molecules, we surveyed 54 compounds approved by the FDA since March 2017 with respect to dose intensity, dose modifications, and treatment emergent adverse events (TEAEs). Of the 54 new molecular entities surveyed, only 15 were approved at a label dose equal to the MTD (Label Dose = MTD).
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Respiratory and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-Related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, State Key Laboratory of Respiratory Health and Multimorbidity, West China Hospital of Sichuan University, Chengdu 610041, China.
Radiolabeled peptides are vital for positron emission tomography (PET) imaging, yet the F-labeling peptides remain challenging due to harsh conditions and time-consuming premodification requirements. Herein, we developed a novel vinyltetrazine-mediated bioorthogonal approach for highly efficient F-radiolabeling of a native peptide under mild conditions. This approach enabled radiosynthesis of various tumor-targeting PET tracers, including targeting the neurofibromin receptor (), the integrin αβ (), and the platelet-derived growth factor receptor β (), with a radiochemical yield exceeding 90%.
View Article and Find Full Text PDFInt J Stroke
January 2025
Department of Neurosurgery and Interventional Neuroradiology, Xuanwu Hospital, China International Neuroscience Institute, Capital Medical University, National Center for Neurological Disorders, 45 Changchun St, Beijing 100053, China.
Rationale: The Chemical Optimization of Cerebral Embolectomy (CHOICE) trial suggested that the administration of intra-arterial alteplase after successful endovascular thrombectomy (EVT) may improve neurological outcomes in patients with acute ischemic stroke due to large vessel occlusion (AIS-LVO) in the anterior circulation. However, the use of adjunctive intra-arterial alteplase following successful EVT in acute posterior circulation stroke remains unexplored.
Aims: This study aims to investigate the efficacy and safety of intra-arterial alteplase after successful EVT for AIS-LVO in the posterior circulation.
Asia Pac J Public Health
January 2025
Department of Dental Hygiene, College of Software and Digital Healthcare Convergence, Yonsei University, Wonju, South Korea.
This study evaluates the influence of smoking cessation policies and COVID-19 on the prevalence of smoking among Korean adolescents from 2011 to 2020. Based on the Korea Youth Risk Behavior Web-based Survey, trends in adolescent smoking behaviors were examined, including the impact of cigarette price increases, Pictorial Warning Labels (PWLs), and the onset of COVID-19. We used joinpoint regression analysis to discern annual changes in the prevalence of adolescent smokers.
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