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Self-assembled natural triterpenoids for the delivery of cyclin-dependent kinase 4/6 inhibitors to enhance cancer chemoimmunotherapy.
J Control Release
December 2024
Key Laboratory of Natural Medicine Innovation and Transformation, Henan University, Kaifeng 475000, PR China; State Key Laboratory of Antiviral Drugs, Henan University, Kaifeng 475000, PR China; Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, PR China. Electronic address:
Immunogenic cell death (ICD) has recently emerged as a promising strategy in reinforcing anti-PD-L1 blockade immunotherapy of triple-negative breast cancer (TNBC). The CDK4/6 inhibitor palbociclib (PAL), as a clinical star medicine targeting the cell cycle machinery, is an ideal candidate for fabricating a highly efficient ICD inducer for TNBC chemoimmunotherapy. However, the frequently observed chemoresistance and clinical adverse effects, as well as significant antagonistic effects when co-administered with certain chemotherapeutics, have seriously restricted the efficiency of PAL and the feasibility of combination strategies.
View Article and Find Full Text PDFDiscovery of a novel CDK4/6 and HDAC dual-targeting agent for the treatment of hepatocellular carcinoma.
Bioorg Chem
December 2024
The State Key Laboratory of Chemical Oncogenomics, Tsinghua Shenzhen International Graduate School, Tsinghua University, Shenzhen 518055, China; Institute of Biomedical Health Technology and Engineering, Shenzhen Bay Laboratory, Shenzhen, 518132, China; School of Pharmaceutical Sciences, Tsinghua University, Beijing, 100084, China.
The down-regulation of p21 after long-term CDK4/6 inhibition represents a key mechanism causing resistance to CDK4/6 inhibitors in some tumor cells, while the HDAC inhibitor could upregulate the level of p21. Herein, a series of novel CDK4/6 and HDAC dual-targeting inhibitors based on the moiety of palbociclib were designed and synthesized. Among them, compound N14 potently inhibited CDK4/6 and HDAC1/6 at nanomolar levels and induced cell apoptosis and G/G phase arrest through HDAC-p21-CDK signaling pathway in HuH-7 cell line.
View Article and Find Full Text PDFContinuation of CDK4/6 Inhibition and Switching of Hormonal Therapy After Progression on Prior CDK4/6 Inhibitors in HR+/HER2- Breast Cancer: A Systematic Review and Meta-Analysis.
Cureus
November 2024
Department of Pharmacy, Hospital San Juan de Dios, Caja Costarricense de Seguro Social, San José, CRI.
This study aims to determine the efficacy of maintaining cyclin-dependent kinase 4/6 (CDK4/6) inhibition and switching endocrine therapy (ET) versus ET alone after progression on prior CDK4/6 inhibitors (CDK4/6i) in patients with hormone-receptor-positive, human epidermal growth factor receptor-2-negative breast cancer. We identified phase II and III comparative randomized clinical trials through a systematic search across relevant clinical databases. A random effects model was used to determine the pooled hazard ratio (HR) for progression-free survival (PFS) according to the inverse-variance method.
View Article and Find Full Text PDFDesigning a Time-Dependent Therapeutic Strategy using CDK4/6 Inhibitors in an Intracranial ATRT Model.
Neuro Oncol
December 2024
Department of Neurological Surgery, Weill Cornell Medicine, New York, NY 10065, USA.
Background: Inhibitors targeting cyclin-dependent kinases 4 and 6 (CDK4/6), crucial for cell cycle regulation, have shown promise in early-stage studies for treating central nervous system (CNS) tumors. However, challenges such as limited CNS penetration, optimal treatment duration, and systemic side effects have impeded their clinical translation for pediatric brain tumors (PBTs).
Methods: We evaluated the potency of CDK4/6 inhibitors across various PBTs cell lines, focusing particularly on palbociclib against atypical teratoid rhabdoid tumor (ATRT) with cell viability assays and gene expression analysis.
Palbociclib plus letrozole in estrogen receptor-positive advanced/recurrent endometrial cancer: Double-blind placebo-controlled randomized phase II ENGOT-EN3/PALEO trial.
Gynecol Oncol
December 2024
Department of Gynecology with Center of Oncological Surgery, Universitätsklinik Charité, Campus Virchow Klinikum, Berlin, Germany.
Purpose: The CDK4/6 inhibitor palbociclib inhibits cyclin A, which is overexpressed in endometrial cancer. Combining palbociclib with endocrine therapy improves efficacy in hormone receptor-positive breast cancer. We investigated palbociclib combined with endocrine therapy for estrogen receptor-positive advanced/recurrent endometrial cancer.
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