Results 61 to 70 of about 25,087 (209)

DualPG‐DTA: A Large Language Model‐Powered Graph Neural Network Framework for Enhanced Drug‐Target Affinity Prediction and Discovery of Novel CDK9 Inhibitors Exhibiting in Vivo Anti‐Leukemia Activity

Advanced Science, EarlyView.
This study introduces DualPG‐DTA, a framework integrating two pre‐trained models to generate molecular and protein representations. It constructs dual graphs processed by specialized neural networks with dynamic attention for feature fusion, achieving superior benchmark performance.
Yihao Chen, Jindi Huang, Cong Liu, Shipeng Zhang, Xinze Li, Zhang Zhang, Tie‐Gen Chen, Ling Wang   +7 more
wiley   +1 more source

Interindividual variability in CYP3A‐mediated venetoclax metabolism in vitro and in vivo in patients with chronic lymphocytic leukemia

Clinical and Translational Science
Venetoclax is a first‐in‐class orally administered B‐cell lymphoma‐2 inhibitor used to treat chronic lymphocytic leukemia (CLL). Venetoclax is primarily metabolized in the liver by cytochrome P450 (CYP) 3A4 to its major metabolite M27, via M5, and M2, M3,
Jonghwa Lee, Jessica L. Beers, Isabel Cheng, Vivian Truong, Zachary Brown, Benyam Muluneh, Catherine C. Coombs, Klarissa D. Jackson   +7 more
doaj   +1 more source

Treatment of Central Nervous System Relapse in Acute Promyelocytic Leukemia by Venetoclax: A Case Report

Frontiers in Oncology, 2021
Extramedullary relapse of acute promyelocytic leukemia is a rare phenomenon and is associated with a poor prognosis, with the central nervous system being the most common site of relapse. The current treatments are still limited.
Xuzhao Zhang, Jinliang Chen, Weiqin Wang, Xian Li, Yanbin Tan, Xiaohong Zhang, Wenbin Qian   +6 more
doaj   +1 more source

Clinical Pharmacology & Therapeutics: Past, Present, and Future. [PDF]

, 2017
Clinical Pharmacology & Therapeutics (CPT), the definitive and timely source for advances in human therapeutics, transcends the drug discovery, development, regulation, and utilization continuum to catalyze, evolve, and disseminate discipline ...
Terzic, Andre, Waldman, Scott A.
core   +2 more sources

IL4I1⁺ Macrophages and TDO2⁺ Myofibroblasts Drive AhR‐Mediated Immunosuppression and Ferroptosis Resistance in Solid Predominant Lung Adenocarcinoma

Advanced Science, EarlyView.
Solid predominant lung adenocarcinoma exhibits an immune‐excluded, ferroptosis‐resistant niche enriched with IL4I1⁺ TAMs and TDO2⁺ myCAFs. Spatial and multi‐omics analyses reveal AhR‐driven crosstalk that promotes T cell exhaustion and therapy resistance. Blocking AhR with CH‐223191 restores ferroptosis sensitivity, and its combination with ferroptosis
Zhaoxuan Wang, Weijiao Xu, Lei Zhao, Lin Zhong, Wendan Yu, Shengmin Wang, Lu Sun, Tao Guo, Fengzhou Li, Zhuoshi Li, Lei Fang, Shiqing Wang, Guohui Zhang, Guoqing Xue, Wei Guo, Shilei Zhao, Chundong Gu   +16 more
wiley   +1 more source

Targeting METTL3 mitigates venetoclax resistance via proteasome-mediated modulation of MCL1 in acute myeloid leukemia

Cell Death and Disease
Venetoclax, a selective BCL2 inhibitor, is extensively utilized in clinical settings for the treatment of acute myeloid leukemia (AML). However, its efficacy is often compromised by the development of drug resistance.
Chang-qing Jiao, Chen Hu, Meng-hua Sun, Yan Li, Chao Wu, Fei Xu, Lei Zhang, Fu-rong Huang, Jun-jie Zhou, Ji-fei Dai, Min Ruan, Wen-chao Wang, Qing-song Liu, Jian Ge   +13 more
doaj   +1 more source

Cirmtuzumab inhibits Wnt5a-induced Rac1 activation in chronic lymphocytic leukemia treated with ibrutinib. [PDF]

, 2016
Signaling via the B cell receptor (BCR) plays an important role in the pathogenesis and progression of chronic lymphocytic leukemia (CLL). This is underscored by the clinical effectiveness of ibrutinib, an inhibitor of Bruton's tyrosine kinase (BTK) that
Chen, L, Chen, Y, Choi, MY, Cui, B, Kipps, TJ, Rassenti, LZ, Widhopf Ii, GF, Wu, Christina, Yu, J, Zhang, L   +9 more
core   +1 more source

Pirin Transcriptionally Regulates PLA2G4A To Inhibit Ferroptosis in Colorectal Cancer via Lipid Profile Remodeling

Advanced Science, EarlyView.
This study identifies Pirin (PIR), an iron‐binding protein, as a critical ferroptosis suppressor in colorectal cancer through lipid membrane remodeling. PIR, induced by NRF2 during ferroptotic stress, transcriptionally regulates PLA2G4A to shift cellular lipid composition away from ferroptosis‐permissive polyunsaturated phospholipids.
Wei Shi, Yue Qi Ong, Prativa Majee, Esther SM Wong, Amhed Missael Vargas Velazquez, Kerem Fidan, Pierce Kah‐Hoe Chow, Wai Leong Tam, Ker Kan Tan, Iain Beehuat Tan, Vinay Tergaonkar   +10 more
wiley   +1 more source

Concurrent ibrutinib plus venetoclax in relapsed/refractory mantle cell lymphoma: the safety run-in of the phase 3 SYMPATICO study

Journal of Hematology & Oncology, 2021
Ibrutinib plus venetoclax, given with an ibrutinib lead-in, has shown encouraging clinical activity in early phase studies in mantle cell lymphoma (MCL).
Michael Wang, Radhakrishnan Ramchandren, Robert Chen, Lionel Karlin, Geoffrey Chong, Wojciech Jurczak, Ka Lung Wu, Mark Bishton, Graham P. Collins, Paul Eliadis, Frédéric Peyrade, Yihua Lee, Karl Eckert, Jutta K. Neuenburg, Constantine S. Tam   +14 more
doaj   +1 more source

DRP-1 is required for BH3 mimetic-mediated mitochondrial fragmentation and apoptosis [PDF]

, 2017
The concept of using BH3 mimetics as anticancer agents has been substantiated by the efficacy of selective drugs, such as Navitoclax and Venetoclax, in treating BCL-2-dependent haematological malignancies.
Butterworth, Michael, Byrne, Dominic P, Cohen, Gerald M, Eyers, Patrick A, Greaves, Georgia, Milani, Mateus, Varadarajan, Shankar   +6 more
core   +2 more sources