Journey through basic biology reveals a way to treat chromosomally unstable cancers.
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A novel ROR1-targeting antibody-PROTAC conjugate promotes BRD4 degradation for solid tumor treatment.
Theranostics
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Engineering Research Center of Cell & Therapeutic Antibody, Ministry of Education, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China.
Proteolysis Targeting Chimeras (PROTACs) are bifunctional compounds that have been extensively studied for their role in targeted protein degradation (TPD). The capacity to degrade validated or undruggable targets provides PROTACs with significant potency in cancer therapy. However, the clinical application of PROTACs is limited by their poor potency and unfavorable pharmacokinetic properties.
View Article and Find Full Text PDFPROTACs in the treatment of viral diseases.
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Department of Pharmacognosy, Goa College of Pharmacy, Goa University, Panaji, India.
Mass Spectrometry Analysis of Chemically and Collisionally Dissociated Molecular Glue- and PROTAC-Mediated Protein Complexes Informs on Disassembly Pathways.
J Am Soc Mass Spectrom
January 2025
Technical University of Darmstadt, Clemens-Schöpf Institute of Organic Chemistry and Biochemistry, Department of Chemistry, Peter-Grünberg-Straße 4, 64287 Darmstadt, Germany.
Molecular glues (MGs) and proteolysis-targeting chimeras (PROTACs) are used to modulate protein-protein interactions (PPIs), via induced proximity between compounds that have little or no affinity for each other naturally. They promote either reversible inhibition or selective degradation of a target protein, including ones deemed undruggable by traditional therapeutics. Though native MS (nMS) is capable of analyzing multiprotein complexes, the behavior of these artificially induced compounds in the gas phase is still not fully understood, and the number of publications over the past few years is still rather limited.
View Article and Find Full Text PDFCorydalis decumbens and tetrahydropalmatrubin inhibit macrophages inflammation to relieve rheumatoid arthritis by targeting Fosl2.
J Ethnopharmacol
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State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China. Electronic address:
Ethnopharmacological Relevance: Corydalisdecumbens (Thunb.) (CD) is a traditional Chinese medicine and as a single herb or formula has been used to treat RA for decades. Rheumatoid arthritis (RA) is a persistent, systemic autoimmune inflammatory disease.
View Article and Find Full Text PDFCurrent Strategies and Future Dimensions in the Development of KRAS Inhibitors for Targeted Anticancer Therapy.
Drug Dev Res
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South University School of Pharmacy, Savannah, Giorgia, USA.
KRAS is a proto-oncogene that is found to be mutated in 15% of all metastatic cancers with high prevalence in pancreatic, lung, and colorectal cancers. Additionally, patients harboring KRAS mutations respond poorly to standard cancer therapy. As a result, KRAS is seen as an attractive target for targeted anticancer therapy.
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