Results 261 to 270 of about 112,008 (305)

Identification of Novel CD39 Inhibitors Based on Virtual Screening and Enzymatic Assays

Journal of Chemical Information and Modeling, 2021
The accumulation of adenosine in the tumor microenvironment mediates immunosuppression and promotes tumor growth and proliferation. Intervention of the adenosine pathway is an important direction of antitumor immunity research.
Yunshuo Zhao, Xiaotong Chen, Zhe Ding, Chuanjie He, Guan-Lun Gao, Sifan Lyu, Yanfeng Gao, Jiangfeng Du   +7 more
semanticscholar   +1 more source

Rapid screening of multi-target antitumor drugs by nonimmobilized tumor cells/tissues capillary electrophoresis.

Analytica Chimica Acta, 2019
As there are more target categories on tumor cells/tissues than on receptor-overexpressing cells, and tumor tissues can better simulate TME, we established a new method of screening multi-target antitumor drugs by nonimmobilized tumor cells/tissues ...
Ruijun Wu, Chen Li, Cong Li, Jinyu Ren, Xiaozhi Sun, Sufang Zhang, Juncheng Zou, Xiaomei Ling   +7 more
semanticscholar   +1 more source

Drug-like molecules targeting androgen receptor's allosteric binding sites selected by augmented AI and high-throughput screening as antitumor agents against prostate cancer.

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Despite therapeutic advancements, metastatic and nonmetastatic castration-resistant prostate cancer (mCRPC and nmCRPC) remain incurable due to drug resistance, partly due to Androgen receptor (AR) gene abnormalities and splice variants.
F. Bruzzese, Federica Iannelli, M. Roca, L. Addi, Laura Grumetti, Mostafa Ahmed, Alfredo Budillon, N. Gumede   +7 more
semanticscholar   +1 more source

High-throughput in vitro drug screening and in vivo studies identify fenretinide as a brain-penetrant DMG therapeutic

Neuro-Oncology
Background Diffuse midline glioma, characterized by H3K27 alteration (DMG), is the predominant high-grade glioma in children. It commonly originates in the brainstem, yet effective treatments for these patients remain elusive.
D. Upton, Jie Liu, S. George, Santosh Valvi, Caitlin Ung, Benjamin S. Rayner, A. Gopalakrishnan, Ruby Pandher, Aaminah Khan, Pooja Venkat, C. Mayoh, Holly Holliday, N. Yeung, Hieu Nguyen, Laura Franshaw, A. Ehteda, Han Shen, Giovanna Farruggia, I. Orienti, Patrick Reynolds, M. Tsoli, †. DavidS.Ziegler, Alma Mater   +22 more
semanticscholar   +1 more source

Exploration into the Antitumor Potential of Chiral Oligopeptides: a Comprehensive Study Encompassing Design, Synthesis, In Silico Target Screening and Experimental Validation

Journal of Chemical Information and Modeling
Peptides are assuming an increasingly critical role in the fields of medicine and cosmetics. Artificial intelligence-assisted drug screening has significantly improved the efficiency and economic feasibility of drug development.
Yang Lv, Hongyu Xu, Yue Lei, Zeyan Jiang, Tong Li, Rui Yan, Xiaodan Wu, Yingxue Jin, Limin Zhang, Zhiqiang Wang   +9 more
semanticscholar   +1 more source

Green gold of the Pacific: unlocking compounds from terrestrial flora for antitumor and immunomodulatory drug discovery.

Natural product reports (Print)
Covering up to 2025Natural products (NPs) from the terrestrial biodiversity play a key role in oncology drug discovery. While historically identified through bioactivity-guided fractionation, recent advances in high-content screening (HCS) assays ...
P. Huchedé, Vincent Dumontet, Mariko Matsui   +2 more
semanticscholar   +1 more source

Abstract 1670: The SHMT inhibitor SHIN1 augments the antitumor efficacy of 5-Fuin preclinical models of gastric cancer

Cancer Research
Advanced gastric cancer (GC) is a malignant tumor with poor prognosis, which requires in-depth exploration of its malignant progression mechanism and the development of efficient therapeutic protocols.
Huan Deng, Ya-jie Wang, Lin Xiao, Yisheng Pan   +3 more
semanticscholar   +1 more source

Comparative Assay of 2D and 3D Cell Culture Models: Proliferation, Gene Expression and Anticancer Drug Response.

Current pharmaceutical design, 2018
BACKGROUND In vitro tests allow establishing experimental variables. However, in vitro results cannot be extrapolated to in vivo tests. Considering that three-dimensional (3D) culture has been one of the best ways to portray the in vivo system of most ...
Aline G Souza, I. B. Silva, Esther Campos-Fernández, Letícia S. Barcelos, J. B. Souza, Karina Marangoni, L. Goulart, V. Alonso-Goulart   +7 more
semanticscholar   +1 more source

Structure-based drug design of DNA minor groove binders and evaluation of their antibacterial and anticancer properties.

European journal of medicinal chemistry
Antimicrobial and chemotherapy resistance are escalating medical problem of paramount importance. Yet, research for novel antimicrobial and anticancer agents remains lagging behind. With their reported medical applications, DNA minor groove binders (MGBs)
Hasan Y. Alniss, Hadeel M. Al-Jubeh, Yousef A. Msallam, R. Siddiqui, Zinb Makhlouf, Anil Ravi, Rania Hamdy, Sameh S. M. Soliman, N. A. Khan   +8 more
semanticscholar   +1 more source

Virtual Screening, Molecular Dynamics Simulation, and Bioactivity Assessment Validate T13074 as a Dual-Target EGFR/c-Met Inhibitor.

Current Medicinal Chemistry
OBJECTIVES The objective of this study is to identify dual-target inhibitors against EGFR/c-Met through virtual screening, dynamic simulation, and biological activity evaluation.
Dang Fan, Haifeng Dong, Anqi Li, Yuying Zhang, Shiyu Wang, Y. Tu, Linxiao Wang   +6 more
semanticscholar   +1 more source