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Rational Design, Synthesis, and Biological Evaluation of Novel c-Met Degraders for Lung Cancer Therapy.
J Med Chem
January 2025
Center for Molecular Oncology, Frontiers Science Center for Disease-Related Molecular Network, State Key Laboratory of Biotherapy and Cancer Center, State Key Laboratory of Respiratory Health and Multimorbidity, West China Hospital, Sichuan University, 610064 Chengdu, China.
Cellular-mesenchymal epithelial transition factor (c-Met) is an attractive target for treating multiple cancers. Despite plentiful c-Met inhibitors have been developed, some issues, including the acquired drug resistance to c-Met inhibitors, have emerged to hamper their application in clinical treatment. Degradation of c-Met offers an opportunity to solve these issues.
View Article and Find Full Text PDFHow (not) to define 'assisted dying'.
J Med Ethics
January 2025
Anscombe Bioethics Centre, Oxford, UK
In the last 20 years 'assisted dying' (and/or its variants 'assisted death', 'assistance in dying', 'aid in dying') has become increasingly prevalent as a term to denote the intentional ending of the life of a patient by or with the assistance of a doctor. However, there is no agreed definition. This paper focuses on the debate over the definition of this term in the UK.
View Article and Find Full Text PDFDesign, synthesis, and antiviral activity of fragmented-lapatinib aminoquinazoline analogs towards SARS-CoV-2 inhibition.
Eur J Med Chem
January 2025
Center of Excellence in Natural Products, Department of Chemistry, Faculty of Science, Chulalongkorn University, Pathumwan, Bangkok, 10330, Thailand. Electronic address:
The severe impact of COVID-19 on global health and economies highlights the critical need for innovative treatments. Recently, lapatinib, a drug initially used for breast cancer, has been identified as a potential inhibitor of the main protease (Mpro) of SARS-CoV-2, meriting further investigation. Utilizing rational design strategies and guided by MD simulations, we developed novel aminoquinazoline analogs based on fragmented lapatinib's structure.
View Article and Find Full Text PDFSilk-based biomaterials for tissue engineering.
Adv Colloid Interface Sci
January 2025
Institute of Smart Biomedical Materials, School of Materials Science and Engineering, Zhejiang Sci-Tech University, Hangzhou 310018, China; Zhejiang-Mauritius Joint Research Center for Biomaterials and Tissue Engineering, Zhejiang Sci-Tech University, Hangzhou 310018, PR China. Electronic address:
Tissue engineering (TE) involves repairing, replacing, regeneration, or improving the function of tissues and organs by combining cells, growth factors and scaffold materials. Among these, scaffold materials play a crucial role. Silk fibroin (SF), a natural biopolymer, has been widely used in the TE field due to its good biodegradability, biocompatibility, and mechanical properties attributed to its chemical composition and structure.
View Article and Find Full Text PDFRationally manipulating molecular planarity to improve molar absorptivity, NIR-II brightness, and photothermal effect for tumor phototheranostics.
Biomaterials
January 2025
Lab of Molecular Imaging and Translational Medicine (MITM), Engineering Research Center of Molecular and Neuro Imaging, Ministry of Education, School of Life Science and Technology, Xidian University & International Joint Research Center for Advanced Medical Imaging and Intelligent Diagnosis and Treatment, Xi'an, Shaanxi, 710126, China. Electronic address:
The secondary near-infrared region (NIR-II) fluorescence imaging-guided photothermal therapy (PTT) offers a noninvasive and light-controllable treatment option for deep-seated cancers. However, the development of NIR-II photothermal agents (NIR-II PTAs) that possess the desired properties of high molar absorption coefficient (ε), fluorescence quantum yield (QY), and photothermal conversion efficiency (PCE) remain a challenge due to the contradiction between radiative and nonradiative processes. Herein, we propose a novel side-chain heteroatom substitution engineering strategy to simultaneously enhance ε, QY, and PCE by modifying the molecular planarity.
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