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The utilization and impact of parallel synthesis on lead exploration around initial hit oxindole (1) are described. The emergent SAR, analogue design and functional impact will also be detailed.
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http://dx.doi.org/10.1016/s0960-894x(03)00657-7 | DOI Listing |
Front Immunol
September 2025
Department of Thoracic Surgery, Shenzhen People's Hospital (The First Affiliated Hospital, Southern University of Science and Technology; The Second Clinical Medical College, Jinan University), Shenzhen, Guangdong, China.
Background: Lung cancer remains the leading cause of cancer-related mortality globally, primarily due to late-stage diagnosis, molecular heterogeneity, and therapy resistance. Key biomarkers such as EGFR, ALK, KRAS, and PD-1 have revolutionized precision oncology; however, comprehensive structural and clinical validation of these targets is crucial to enhance therapeutic efficacy.
Methods: Protein sequences for EGFR, ALK, KRAS, and PD-1 were retrieved from UniProt and modeled using SWISS-MODEL to generate high-confidence 3D structures.
Top Magn Reson Imaging
October 2025
BIOSPACE LAB, Nesles-la-Vallée, France.
Aims: Cardiac tumors are aggressive and asymptomatic in early stages, causing late diagnosis and locoregional metastasis. Currently, the standard of care uses gadolinium-based contrast agents for MRI, and the associated hypersensitivity reactions are a significant concern, such as gadolinium deposition disease. In addition, the proximity of cardiac lesions closer to vital structures complicates surgical interventions.
View Article and Find Full Text PDFZhong Nan Da Xue Xue Bao Yi Xue Ban
May 2025
Department of Rheumatology and Immunology, Xiangya Hospital, Central South University, Changsha 410008.
Objectives: Patients with connective tissue diseases (CTD) have a high incidence of cardiac involvement, which often presents insidiously and can progress rapidly, making it one of the leading causes of death. Multiparametric cardiovascular magnetic resonance (CMR) provides a comprehensive quantitative evaluation of myocardial injury and is emerging as a valuable tool for detecting cardiac involvement in CTD. This study aims to investigate the correlations between CMR features and serological biomarkers in CTD patients, assess their potential clinical value, and further explore the impact of pre-CMR immunotherapy intensity on CMR-specific parameters, thereby evaluating the role of CMR in the early diagnosis of CTD-related cardiac involvement.
View Article and Find Full Text PDFCold Spring Harb Perspect Med
September 2025
Departments of Pathology, Genetics, and Biology, Stanford University, Stanford, California 94305-5324, USA
Dysregulation of cell growth and metabolic changes are a feature of tumorigenesis. Studies over the past 50 years have mapped the pathways that control cell growth and metabolism and revealed how these are altered in cancer. In this excerpt from his forthcoming book on the history of cancer research, Joe Lipsick looks at how we got here-from early work on insulin and growth factor receptor signaling to the discovery of phosphatidyl inositol 3-kinase (PI 3-kinase), the identification of mTOR as the target of rapamycin, and the unexpected finding that tumors can produce novel "oncometabolites.
View Article and Find Full Text PDFAims: Ribociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that was approved by the US Food and Drug Administration (FDA) in 2017 for the treatment of advanced hormone receptor-positive (HR+) breast cancer. The presented study aimed to evaluate the ribociclib-associated adverse events (AEs) through data mining of the US Food and Drug Administration Adverse Event Reporting System (FAERS).
Methods: Data were collected from the FAERS database covering the period from the first quarter of 2017 to the first quarter of 2023.