A series of bifunctional compounds have been discovered for their dual functionality as MER/AXL inhibitors and immune modulators. The furanopyrimidine scaffold, renowned for its suitability in kinase inhibitor discovery, offers at least three distinct pharmacophore access points. Insights from molecular modeling studies guided hit-to-lead optimization, which revealed that the 1,3-diketone side chain hybridized with furanopyrimidine scaffold that respectively combined amino-type substituent and 1-pyrazol-4-yl substituent on the top and bottom of the aryl regions to produce and , exhibiting potent antitumor activities in various syngeneic and xenograft models.
View Article and Find Full Text PDFIncarceration of the appendix within a femoral hernia is a rare condition of abdominal wall hernia about 0.1 to 0.5% in reported femoral hernia [1].
View Article and Find Full Text PDFEnergy shortage has become a global issue in the twenty-firt century, as energy consumption grows at an alarming rate as the fossil fuel supply exhausts. Perovskite solar cells (PSCs) are a promising photovoltaic technology that has grown quickly in recent years. Its power conversion efficiency (PCE) is comparable to that of traditional silicon-based solar cells, and scale-up costs can be substantially reduced due to its utilization of solution-processable fabrication.
View Article and Find Full Text PDFObjectives: Trauma is one of the leading causes of death and its incidence increases annually. The "weekend effect" and "holiday season effect" on traumatic injury mortality remain controversial, whereby traumatic injury patients admitted during weekends and/or holiday season have a higher risk of in-hospital death. The present study is aimed to explore the association between "weekend effect" and "holiday season effect" and mortality in traumatic injury population.
View Article and Find Full Text PDFPurpose: Metformin is a biguanide derivative that is commonly used for the treatment of diabetes mellitus (DM). It demonstrates antioxidative, anti-inflammatory, and antiangiogenic activity within the ocular tissue and thus may be implicated in the treatment of age-related macular degeneration (AMD). However, epidemiological studies have shown conflicting results.
View Article and Find Full Text PDFObjectives: Early identification of traumatic brain injury (TBI) patients at a high risk of mortality is very important. This study aimed to compare the predictive accuracy of four scoring systems in TBI, including shock index (SI), modified shock index (MSI), age-adjusted shock index (ASI), and reverse shock index multiplied by the Glasgow Coma Scale (rSIG).
Patients And Methods: This is a retrospective analysis of a registry from the Taipei Tzu Chi trauma database.
Diagnostics (Basel)
September 2022
Background: Early trauma team activation (TTA) may improve clinical outcomes through early diagnosis and timely intervention by a dedicated multidisciplinary team. Controversy seems to exist about the effect of establishing trauma team systems in traumatic injury populations. Our aim was to identify factors that may be associated with clinical outcomes in trauma injury and to investigate the effect of trauma team activation.
View Article and Find Full Text PDFThe pulmonary artery catheter (PAC)-despite its invasiveness-remains the gold standard for cardiac output (CO) monitoring. The FloTrac system, a less invasive hemodynamic monitor has been developed, which estimates CO using arterial pressure waveform analysis without external calibration. Recently, an upgraded version of FloTrac system with improved algorithm to follow changes in vascular resistance was introduced into the market.
View Article and Find Full Text PDFIntraocular pressure (IOP) is crucial to the well-being of eyes. During anesthesia, the administration of succinylcholine and endotracheal intubation are associated with an increase in IOP, which may be attenuated by short-acting opioids. However, the drug of choice among the commonly used short-acting opioids is unclear.
View Article and Find Full Text PDFAcute low-tone hearing loss (ALHL) is a common clinical disease and was first proposed by Abe in 1981 as sensorineural hearing loss confined to low frequencies. The best strategy for initiating medication is still unclear, as the superiority of steroids and diuretics is still debated, and combination therapy might yield additional benefits. However, no study regarding combination therapy has been published.
View Article and Find Full Text PDFObjective: Blood pressure in patients with traumatic brain injury (TBI) is associated with clinical outcome. However, evidence of blood pressure (BP) range is scarce and the association between BP and clinical outcome is mostly controversial. We aimed to investigate the association between blood pressure and clinical outcome in TBI.
View Article and Find Full Text PDFTraditional otoscopy has some limitations, including poor visualization and inadequate time for evaluation in suboptimal environments. Smartphone-enabled otoscopy may improve examination quality and serve as a potential diagnostic tool for middle ear diseases using a telemedicine approach. The main objectives are to compare the correctness of smartphone-enabled otoscopy and traditional otoscopy and to evaluate the diagnostic confidence of the examiner via meta-analysis.
View Article and Find Full Text PDFCleft palate is the most common congenital facial deformity and may result in multiple sequelae and disabilities. One common comorbidity is refractory otitis media with effusion (OME), as patients with cleft palate have impaired eustachian tube function with alteration of the nearby muscular structures. Ventilation tube insertion (VTI) is regarded as an effective mean to address OME in addition to palatal repair surgery.
View Article and Find Full Text PDFEvidence regarding the effect of a face-down posture (FDP) for large idiopathic macular hole (IMH) is inconsistent. We conducted a systematic review and meta-analysis to determine whether a postoperative FDP is required for the treatment of large IMH. Eligible randomized controlled trials published before September 2021 were retrieved from the Medline, Embase, and Cochrane Library databases.
View Article and Find Full Text PDFColony-stimulating factor-1 receptor (CSF1R) is implicated in tumor-associated macrophage (TAM) repolarization and has emerged as a promising target for cancer immunotherapy. Herein, we describe the discovery of orally active and selective CSF1R inhibitors by property-driven optimization of BPR1K871 (), our clinical multitargeting kinase inhibitor. Molecular docking revealed an additional nonclassical hydrogen-bonding (NCHB) interaction between the unique 7-aminoquinazoline scaffold and the CSF1R hinge region, contributing to CSF1R potency enhancement.
View Article and Find Full Text PDFBackground: Hearing loss is one of the most common disabilities worldwide and affects both individual and public health. Pure tone audiometry (PTA) is the gold standard for hearing assessment, but it is often not available in many settings, given its high cost and demand for human resources. Smartphone-based audiometry may be equally effective and can improve access to adequate hearing evaluations.
View Article and Find Full Text PDFImportance: Platinum-induced ototoxic effects are a significant issue because platinum-based chemotherapy is one of the most commonly used therapeutic medications. Sodium thiosulfate (STS) is considered a potential otoprotectant for the prevention of platinum-induced ototoxic effects that functions by binding the platinum-based agent, but its administration raises concerns regarding the substantial attenuation of the antineoplastic outcome associated with platinum.
Objective: To evaluate the association between concurrent STS and reduced risk of ototoxic effects among patients undergoing platinum-based chemotherapy and to evaluate outcomes, including event-free survival, overall survival, and adverse outcomes.