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Design, synthesis and antiviral evaluation of triazole-linked 7-hydroxycoumarin-monoterpene conjugates as inhibitors of RSV replication.
RSC Med Chem
December 2024
Department of Medicinal Chemistry, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry 9, Akademika Lavrentieva Ave. 630090 Novosibirsk Russia
Respiratory syncytial virus (RSV) is the leading cause of acute lower respiratory infections in babies across the world. Irrespective of progress in the development of RSV vaccines, effective small molecule drugs are still not available on the market. Based on our previous data we designed and synthesized triazole-linked coumarin-monoterpene hybrids and showed that they are indeed effective in inhibiting the RSV replication.
View Article and Find Full Text PDFRecent advances of antibody-drug conjugates in treating breast cancer with different HER2 status.
Ther Adv Med Oncol
January 2025
Department of General Surgery, The First Affiliated Hospital of Soochow University, No. 899, Pinghai Road, Suzhou, Jiangsu 215006, China.
Despite the availability of multiple treatment options for breast cancer, challenges such as adverse events, drug resistance, and disease progression persist for patients. The identification of human epidermal growth factor receptor 2 (HER2) as an oncogenic driver in a subset of breast cancers, alongside the development of HER2-targeted therapies, has significantly improved the prognosis of HER2-amplified breast cancers. However, therapeutic options remain limited for HER2-overexpressing or HER2-negative breast cancers.
View Article and Find Full Text PDFOn-site biosignal amplification using a single high-spin conjugated polymer.
Nat Commun
January 2025
National Key Laboratory of Advanced Micro and Nano Manufacture Technology, School of Materials Science and Engineering, Peking University, Beijing, China.
On-site or in-sensor biosignal transduction and amplification can offer several benefits such as improved signal quality, reduced redundant data transmission, and enhanced system integration. Ambipolar organic electrochemical transistors (OECTs) are promising for this purpose due to their high transconductance, low operating voltage, biocompatibility, and suitability for miniaturized amplifier design. However, limitations in material performance and stability have hindered their application in biosignal amplification.
View Article and Find Full Text PDFResults of a patient-level pooled analysis of three studies of trastuzumab deruxtecan in HER2-positive breast cancer with active brain metastasis.
ESMO Open
January 2025
Dana-Farber Cancer Institute, Boston. Electronic address:
Background: Brain metastases (BMs) are common in human epidermal growth factor receptor 2 (HER2)-positive advanced breast cancer, increasing morbidity and mortality. Systemic therapy for BMs can be effective, with the triple combination of trastuzumab, capecitabine, and tucatinib being a potential standard. More recently, intracranial activity of antibody-drug conjugates has been reported, but the size of individual studies has been small.
View Article and Find Full Text PDFThe Nonclinical Safety Assessment of a Novel Anti-CEACAM5 Antibody Exatecan Conjugate Predicts a Low Risk for Interstitial Lung Disease (ILD) in Patients-The Putative Mechanism Behind ILD.
Int J Toxicol
January 2025
Chemical and Preclinical Safety Department, Global Chemical and Preclinical Safety, Merck KGaA, Darmstadt, Germany.
The therapeutic window of antibody drug-conjugates (ADC) remains challenging due to safety issues such as interstitial lung disease (ILD) observed with specific deruxtecan-based ADCs. To avoid ILD, we designed M9140 by conjugating the maleimide-containing hydrophilic β-glucuronide linker to exatecan and our anti-CEACAM5 (CarcinoEmbryonic Antigen-related Cell Adhesion Molecule 5) specific antibody. Following repeated iv-infusion at 3 to 30 mg/kg of M9140 every 3 weeks, the pathological findings obtained in cynomolgus monkeys were confined to gastrointestinal and hematolymphoid tissues and resembled the toxicity of exatecan.
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