Results 281 to 290 of about 120,380 (317)

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, Vivian Alonso-Goulart   +7 more
semanticscholar   +1 more source

Discovery of 2H-Indazole-3-carboxamide Derivatives as Novel Potent Prostanoid EP4 Receptor Antagonists for Colorectal Cancer Immunotherapy.

Journal of Medicinal Chemistry, 2023
Nowadays, small-molecule drugs have become an indispensable part of tumor immunotherapy. Accumulating evidence has indicated that specifically blocking PGE2/EP4 signaling to induce robust antitumor immune response represents an attractive immunotherapy ...
Zhiyuan Cheng, Yijie Wang, Yao Zhang, Chan Zhang, Mengru Wang, Wei Wang, Jiacheng He, Yang Wang, Hankun Zhang, Qiansen Zhang, Chunyong Ding, Deyan Wu, Linlin Yang, Mingyao Liu, Weiqiang Lu   +14 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

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

Application of molecular dynamics-based pharmacophore and machine learning approaches to identify novel Mcl1 inhibitors through drug repurposing and mechanics research.

Physical Chemistry, Chemical Physics - PCCP
Myeloid cell leukemia 1 (Mcl1), a critical protein that regulates apoptosis, has been considered as a promising target for antitumor drugs. The conventional pharmacophore screening approach has limitations in conformation sampling and data mining.
Han-xun Wang, Zhuo Qi, Wenxiong Lian, Lanyan Ma, Shizun Wang, Haihan Liu, Yu Jin, Hua-Li Yang, Jian Wang, Maosheng Cheng   +9 more
semanticscholar   +1 more source

In vitro assays for anticancer drug discovery--a novel approach based on engineered mammalian cell lines.

Anti-Cancer Drugs, 2005
Despite decisive progress in understanding the molecular biology of cancer development, cytotoxic anticancer drugs continue to be the cornerstone of modern antitumor therapies.
V. Gonzalez‐Nicolini, M. Fussenegger
semanticscholar   +1 more source

Identification and Characterization of Strychnine-Binding Peptides Using Phage-Display Screening.

Protein Peptide Letters, 2017
BACKGROUND In drug development, phage display is a high-throughput method for identifying the specific cellular targets of drugs. However, insoluble small chemicals remain intractable to this technique because of the difficulty of presenting molecules to
Fang Zhang, Min Wang, Zheng Qiu, Xiao-Meng Wang, Chunlei Xu, Xia Zhang   +5 more
semanticscholar   +1 more source

Abstract 1944: High-throughput fluorescence-based assay for screening of Arginase I inhibitors for cancer immunotherapy

Experimental and Molecular Therapeutics, 2018
Arginase I (ArgI) is an important small molecule drug target in cancer immunotherapy. Arg1 converts L-arginine into L-ornithine and urea. Recruitment of ArgI-expressing myeloid-derived suppressor cells (MSDCs) at a tumor site results in the depletion of ...
Y. Grobben, J. Uitdehaag, N. Willemsen-Seegers, W. Tabak, Martine B. W. Prinsen, Suzanne J.C. van Gerwen, J. V. Groningen, J. Friesen, Helma Rutjes, J. Man, R. Buijsman, G. Zaman   +11 more
semanticscholar   +1 more source

Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.

Journal of Medicinal Chemistry, 2009
An aberrant activity of the epidermal growth factor receptor (EGFR) has been shown to be related to many human cancers, such as breast and liver cancers, thus making EGFR an attractive target for antitumor drug discovery.
C. La Motta, S. Sartini, T. Tuccinardi, E. Nerini, F. Da Settimo, A. Martinelli   +5 more
semanticscholar   +1 more source

Discovery of New E‐Selectin Inhibitors by Virtual Screening, Fluorescence Binding Assays, and STD NMR Experiments

ChemMedChem, 2016
Pabla A. Barra, V. Jiménez, J. Gavín, A. Daranas, J. Alderete   +4 more
semanticscholar   +1 more source