Kinase signaling plays an important role in acquired epilepsy, but only a small percentage of the total kinome has been investigated in this context. A major roadblock that prevents the systematic investigation of the contributions of kinase signaling networks is the slow speed of experiments designed to test the chronic effects of target inhibition in epilepsy models. We developed a novel in vitro screening platform based on microwire recordings from an organotypic hippocampal culture model of acquired epilepsy. This platform enables the direct, parallel determination of the effects of compounds on spontaneous epileptiform activity. The platform also enables repeated recordings from the same culture over two-week long experiments. We screened 45 kinase inhibitors and quantified their effects on seizure duration, the frequency of paroxysmal activity, and electrographic load. We identified several inhibitors with previously unknown antiepileptic properties. We also used kinase inhibition profile cross-referencing to identify kinases that are inhibited by seizure-suppressing compounds, but not by compounds that had no effect on seizures.
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http://dx.doi.org/10.3390/ijms20102502 | DOI Listing |
Cancer Metastasis Rev
January 2025
Département de Radiothérapie et de Physique Médicale, Centre Henri Becquerel Rouen QuantiF, LITIS EA4108 Université Rouen, Rouen, France.
The management of bone metastases (BoM) requires a multidisciplinary approach to prevent complications, necessitating updated knowledge in light of the rapid advancements in systemic treatments and surgical, interventional radiology or radiation techniques. This review aims to discuss efficacy of new systemic treatments on BoM, the benefits of radiotherapy adjunction, and the optimal methods for combining them. Preliminary evidence suggesting reduced efficacy of immune checkpoint inhibitors (ICI), and several multi-kinase inhibitors regarding BoM may encourage early use of radiotherapy (RT).
View Article and Find Full Text PDFCommun Biol
January 2025
Department of Oncology, NHC Key Laboratory of Cancer Proteomics & State Local Joint Engineering Laboratory for Anticancer Drugs, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, China.
Hyperactive c-Met signaling pathway caused by altered MET is a common mechanism underlying gastric cancer and represents an attractive target for the treatment of gastric cancer with MET alterations. However, no c-Met kinase inhibitors are currently approved specifically for the treatment of c-Met-amplified gastric cancer. Recently, bozitinib, a highly selective c-Met kinase inhibitor, has shown remarkable potency in selectively inhibiting MET-altered non-small cell lung cancer and secondary glioblastoma.
View Article and Find Full Text PDFCell Death Discov
January 2025
Laboratory of Genome Stress Signaling, National Cancer Center Research Institute, Chuo-ku, Tokyo, 104-0045, Japan.
DNA replication stress (RS), a prevalent feature of various malignancies, arises from both genetic mutations and genotoxic exposure. Elevated RS levels increase the vulnerability of cancer cells to ataxia telangiectasia and Rad3-related kinase inhibitors (ATRis). Here, we screened for DNA damage response inhibitors that enhance ATRi-induced cytotoxicity using SWI/SNF complex-deficient cells and identified a potent synergy between ATRi and poly(ADP-ribose) polymerase inhibitor (PARPi), particularly in SMARCA4-deficient cells.
View Article and Find Full Text PDFClin Lymphoma Myeloma Leuk
January 2025
Department of Haematology, the First Affiliated Hospital of Sun Yat-sen University, Guangzhou, China. Electronic address:
Objective: To analyze the impact of tyrosine kinase inhibitor (TKI) maintenance therapy following allogeneic hematopoietic stem cell transplantation (HSCT) in patients with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL) on recurrence rates and prognosis for the 2 transcripts, p190 and p210.
Methods: We conducted a retrospective analysis of clinical data from 58 patients diagnosed with Ph + ALL who underwent HSCT. All patients received TKI maintenance therapy following hematopoietic reconstruction post-transplantation.
Cell Rep Med
January 2025
Severance Biomedical Science Institute, Yonsei University College of Medicine, Seoul, Republic of Korea; Yonsei New ΙΙ Han Institute for Integrative Lung Cancer Research, Yonsei University of Medicine, Seoul, Republic of Korea. Electronic address:
Uncommon epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer (NSCLC) pose therapeutic challenge due to limited response to EGFR tyrosine kinase inhibitors (TKIs). This study presents preclinical evidence and mechanistic insights into the combination of lazertinib, a third-generation EGFR-TKI; and amivantamab, an EGFR-MET bispecific antibody, for treating NSCLC with uncommon EGFR mutations. The lazertinib-amivantamab combination demonstrates significant antitumor activity in patient-derived models with uncommon EGFR mutations either before treatment or after progressing on EGFR-TKIs.
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