from preclinical tool compounds to the highly specific medicines approved to treat patients with cancer. Herein we discuss current paradigms for PI3K inhibitors in cancer therapy, focusing on clinical data and mechanisms of action. We also discuss current limitations in the use of PI3K inhibitors, in...
[7] Liu N, Rowley BR, Bull CO, etal. BAY80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013Nov;12(11):2...
[3] PI3K inhibitors: review and new strategies. [4]Umbralisib, a Dual PI3Kδ/CK1ε Inhibitor in Patients With Relapsed or Refractory Indolent Lymphoma. [5] Targeting PI3K in cancer: mechanisms and advances in clinical trials. [6] 特异性PI3K亚型抑制剂抗肿瘤作用研究进展. [7] PI3K 选择性抑制...
Selectide-18 is a novel PI3K inhibitor that targets PI3K's catalytic subunit p110β, resulting in reduced viability of cancer cells. The p110β subunit is the most prominent PI3K subunit in many chemoresistant tumors. Previous research has revealed a unique 18-residue long motif within the C2...
4.化疗耐药:PAM信号通路通过KEAP1-Nrf2轴和核转录因子NF-κB通路促进乳腺癌耐药蛋白(breast cancer resistance protein, BCRP)抑制剂的转录,并诱导P-糖蛋白(P-glycoprotein, P-gp)的表达,其机制尚不明确。BCRP和P-gp可增强化疗药物的外...
Although progress has been hampered by issues such as poor drug tolerance and drug resistance, several PI3K inhibitors have now received regulatory approval — the PI3Kα isoform-selective inhibitor alpelisib for the treatment of breast cancer and inhibitors mainly aimed at the leukocyte-enriched PI3K...
Fruman DA, Rommel C. PI3K and cancer: lessons, challenges and opportunities. Nat Rev Drug Discov. 2014;13(2):140-156. Edgar K, Hong R, Song K, et al. GDC-0077 is a selective PI3K alpha inhibitor with robust efficacy in PIK3CA mutant hormone-positive breast cancer models. Cancer Res....
[7] Liu N, Rowley BR, Bull CO, etal. BAY80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013Nov;12(11):2319-30. [8] S. Christenson, J. A. Wala, R. Parkinson,etal.Phase...
Leary A, Estévez-García P, Sabatier R, et al. ENDOLUNG trial. A phase 1/2 study of the Akt/mTOR inhibitor and autophagy inducer ibrilatazar (ABTL0812) in combination with paclitaxel/carboplatin in patients with advanced/recurrent endometrial cancer. BMC Cancer. 2024;24(1):876. doi:10.11...
1. Christine Fritsch, etc. Characterization of the Novel and Specific PI3Ka Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials.Small Molecule Therapeutics, 2014, 13.2. Setiawan V. W., etc. Breast cancer risk factors defined by estrogen and progesterone ...