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http://dx.doi.org/10.1016/j.molcel.2023.10.013 | DOI Listing |
Endocr Oncol
January 2025
Cancer Cell Signalling Lab, University of Udine, Udine, Italy.
Background: Gastrointestinal neuroendocrine tumors (GI-NETs) are rare neoplasms with limited therapeutic options and increasing clinical incidence. Focal adhesion kinase (FAK) has been implicated in oncogenic processes across various tumor types; however, its specific role in GI-NET biology remains inadequately characterized. This study investigates the impact of FAK inhibition on GI-NET cell survival, invasive potential, and gene regulation, with the aim of evaluating FAK as a therapeutic target.
View Article and Find Full Text PDFJ Exp Clin Cancer Res
August 2025
Department of Gastroenterology, Shanghai Ninth People's Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
Background: Aurora kinase B (AURKB), a key regulator of mitosis, is frequently upregulated in various malignancies, including colorectal cancer (CRC), and is associated with poor prognosis. However, the limited clinical efficacy of AURKB inhibitors suggests the existence of previously unrecognized oncogenic mechanisms that merit further investigation.
Methods: AURKB was prioritized through bioinformatic analysis, and its elevated expression in CRC was validated via single-cell RNA sequencing (scRNA-seq) and western blot.
Eur J Med Chem
November 2025
Department of Medicinal and Organic Chemistry and Excellence Research Unit of Chemistry Applied to Biomedicine and the Environment, Faculty of Pharmacy, University of Granada, Campus Cartuja s/n, 18071, Granada, Spain; Instituto de Investigación Biosanitaria ibs.GRANADA, 18012, Granada, Spain. Elec
CD44, a cell surface glycoprotein, plays a crucial role in cancer progression by enhancing cell proliferation and resistance to apoptosis. Targeting CD44 with small molecules is a promising cancer therapy strategy. Building on our previous work with the tetrahydroisoquinoline (THIQ) derivative SRT1, we designed and synthesized a series of analogues (SRT2-SRT10) to explore their anticancer potential.
View Article and Find Full Text PDFJ Med Chem
August 2025
Department of Emergency Medicine and Laboratory of Emergency Medicine, State Key Laboratory of Biotherapy and Collaborative Innovation Center of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, China.
Focal adhesion kinase (FAK) has emerged as a promising therapeutic target since its pivotal involvement in tumorigenesis. However, FAK inhibitors exhibit limited efficacy in suppressing FAK's noncatalytic functions, potentially compromising their therapeutic outcomes. Herein, we developed a series of FAK PROTACs derived from our previously characterized FAK inhibitor .
View Article and Find Full Text PDFCell Death Dis
July 2025
Structural Biology and Bioinformatics Division, CSIR-Indian Institute of Chemical Biology, IICB TRUE Campus, CN-6, Sector 5, Kolkata, 700091, India.
ER and mitochondrial stress are often interconnected and considered major contributors to aging as well as neurodegeneration. Coordinated induction of ER and mito has been observed in diabetes and pulmonary disorders. However, in the context of aging and neurodegeneration, regulation of this intra-organellar crosstalk has remained relatively elusive.
View Article and Find Full Text PDF