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Targeting RBM39 suppresses tumor growth and sensitizes osteosarcoma cells to cisplatin.
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Guangdong Provincial Key Laboratory of Digestive Cancer Research, Center of Digestive Diseases, Scientific Research Center, The Seventh Affiliated Hospital, Sun Yat-sen University, Shenzhen, China.
Osteosarcoma is one of the most common malignant primary bone tumors and lacks effective therapeutic targets. Recent studies have reported that RNA binding proteins (RBPs) could serve as promising therapeutic targets for cancers, as their critical roles in transcriptional regulation and RNA splicing. Nevertheless, the potential of pharmacologically inhibiting RBPs as a therapeutic strategy for patients with osteosarcoma remains unclear.
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Department of Medicine; Leukemia Service, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
Targeted Protein Degradation and Regulation with Molecular Glue: Past and Recent Discoveries.
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Institute of Pharmacology and Toxicology, Zhejiang Province Key Laboratory of Anti-Cancer, Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
The evolution in research and clinical settings of targeted therapies has been inspired by the progress of cancer chemotherapy to use small molecules and monoclonal antibodies for targeting specific disease-associated genes and proteins for noninfectious chronic diseases. In addition to conventional protein inhibition and activation strategies as drug discovery modalities, new methods of targeted protein degradation and regulation using molecular glues have become an attractive approach for drug discovery. Mechanistically, molecular glues trigger interactions between the proteins that originally did not interact by forming ternary complexes as protein-protein interaction (PPI) modulators.
View Article and Find Full Text PDFSmall molecule integrin antagonists in cancer therapy.
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Dipartimento di Farmacologia Sperimentale ed Applicata, Università di Pavia, Italy.
Integrins are a large family of dimeric receptors composed by alpha and beta subunits that, once bound to extra-cellular matrix (ECM) proteins, regulate a variety of cellular processes such as cell motility, migration, and proliferation. The integrins transduce signals from inside-out and outside-in the cell, thus representing the cellular link to the external environment. For these properties, integrin activation has been involved in pathological processes like tumor growth and metastasis formation.
View Article and Find Full Text PDFApplication of population pharmacokinetic modeling in early clinical development of the anticancer agent E7820.
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Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute/Slotervaart Hospital, Louwesweg 6, 1066 EC, Amsterdam, The Netherlands.
The aim of this study was to assess the population pharmacokinetics (PopPK) of the novel oral anti-cancer agent E7820. Both a non-linear mixed effects modeling analysis and a non-compartmental analysis (NCA) were performed and results were compared. Data were obtained from a phase I dose escalation study in patients with malignant solid tumors or lymphomas.
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