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Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations.
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December 2024
Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Rearranged during transfection (RET) kinase is a validated therapeutic target for various cancers characterized by RET alterations. Although two selective RET inhibitors, selpercatinib and pralsetinib, have been approved by the FDA, acquired resistance through solvent-front mutations has been identified rapidly. Developing proteolysis targeting chimera (PROTAC) targeting RET mutations offers a promising strategy to combat drug resistance.
View Article and Find Full Text PDFChemoprevention of natural product against oral cancer: A comprehensive review.
Malays J Pathol
December 2024
Universiti Sains Malaysia, School of Dental Sciences, Health Campus, Kubang Kerian, Kelantan, Malaysia.
Introduction: Oral cancer is considered the sixth most common form of cancer worldwide. It causes significant morbidity and mortality, especially in low socioeconomic status groups. However, Cancer chemoprevention encompasses the use of specific compounds to suppress the growth of tumours or inhibit carcinogenesis.
View Article and Find Full Text PDFFrom Random Perturbation to Precise Targeting: A Comprehensive Review of Methods for Studying Gene Function in Species.
J Fungi (Basel)
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College of Food Science and Technology, Huazhong Agricultural University, Wuhan 430070, China.
, a genus of fungi known for its fermentation capability and production of bioactive compounds, such as azaphilone pigments and Monacolin K, have received considerable attention because of their potential in biotechnological applications. Understanding the genetic basis of these metabolic pathways is crucial for optimizing the fermentation and enhancing the yield and quality of these products. However, spp.
View Article and Find Full Text PDFMicrostructural and Surface Texture Evaluation of Orthodontic Microimplants Covered with Bioactive Layers Enriched with Silver Nanoparticles.
J Funct Biomater
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Department of Maxillofacial Orthopaedics and Orthodontics, Pomeranian Medical University in Szczecin, Al. Powst. Wlkp. 72, 70111 Szczecin, Poland.
Bacterial infections are a common cause of clinical complications associated with the use of orthodontic microimplants. Biofilm formation on their surfaces and subsequent infection of peri-implant tissues can result in either exfoliation or surgical removal of these medical devices. In order to improve the properties of microimplants, hybrid coatings enriched with silver nanoparticles, calcium, and phosphorus were investigated.
View Article and Find Full Text PDFAsteroid Saponins: A Review of Their Bioactivity and Selective Cytotoxicity.
Mar Drugs
December 2024
Centre for Bioinnovation, University of the Sunshine Coast, Maroochydore BC, QLD 4558, Australia.
Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e.
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