Results 21 to 30 of about 37,916 (265)

Discovery of a pyrrole-pyridinimidazole derivative as novel SIRT6 inhibitor for sensitizing pancreatic cancer to gemcitabine

Cell Death and Disease, 2023
Pancreatic cancer is a highly aggressive cancer, and is primarily treated with gemcitabine, with increasing resistance. SIRT6 as a member of sirtuin family plays important roles in lifespan and diverse diseases, such as cancer, diabetes, inflammation and
Nannan Song, Xian Guan, Siqi Zhang, Yanqing Wang, Xuekai Wang, Zhongxia Lu, Daochen Chong, Jennifer Yiyang Wang, Rilei Yu, Wengong Yu, Tao Jiang, Yuchao Gu   +11 more
doaj   +1 more source

A high-throughput drug combination screen identifies an anti-glioma synergism between TH588 and PI3K inhibitors

Cancer Cell International, 2020
Background Glioblastoma multiforme (GBM) is the most common and lethal type of primary brain tumor. More than half of GBMs contain mutation(s) of PTEN/PI3K/AKT, making inhibitors targeting the PI3K pathway very attractive for clinical investigation ...
Zhen Chen, Chao Chen, Tingting Zhou, Chao Duan, Qianqian Wang, Xiaohui Zhou, Xia Zhang, Fangrong Wu, Yunfen Hua, Fan Lin   +9 more
doaj   +1 more source

The New Antitumor Drug ABTL0812 Inhibits the Akt/mTORC1 Axis by Upregulating Tribbles-3 Pseudokinase [PDF]

, 2016
Purpose: ABTL0812 is a novel first-in-class, small molecule which showed antiproliferative effect on tumor cells in phenotypic assays. Here we describe the mechanism of action of this antitumor drug, which is currently in clinical development ...
Fuster, Gemma, Lizcano, Jose, Gomez-Ferreria, Mariana, Erazo, Tatiana, Munoz-Guardiola, Pau, García-Martínez, Jose, Salazar Roa, María, Lopez-Plana, Anna, Espadaler, Jordi, Fernandez-Nogueira, Patricia, Gascon, Pedro, Bragado Domingo, Paloma, Lorente Pérez, María Del Mar, Alfon, Jose, Domenech, Carles, Bayascas, Jose Ramon, Cortal, Marc, Velasco Díez, Guillermo, Vidal, Laura, Hernandez-Losa, Javier   +19 more
core   +4 more sources

CRISPR/Cas9 screening identifies a kinetochore‐microtubule dependent mechanism for Aurora‐A inhibitor resistance in breast cancer

Cancer Communications, 2021
Background Overexpression of Aurora‐A (AURKA) is a feature of breast cancer and associates with adverse prognosis. The selective Aurora‐A inhibitor alisertib (MLN8237) has recently demonstrated promising antitumor responses as a single agent in various ...
Ailin Chen, Shijun Wen, Fang Liu, Zijian Zhang, Meiling Liu, Yuanzhong Wu, Bin He, Min Yan, Tiebang Kang, Eric W‐F Lam, Zifeng Wang, Quentin Liu   +11 more
doaj   +1 more source

Early ADMET profiling of anti-inflammatory alkaloids using validated LC-MS/MS methods [PDF]

, 2016
Natural products provide an important and unique source of new lead compounds for drug discovery. Approximately 50% of all new chemical entities are inspired by nature.
Jähne, Evelyn
core   +1 more source

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry [PDF]

, 2014
Deubiquitylases (DUBs) are key regulators of the ubiquitin system which cleave ubiquitin moieties from proteins and polyubiquitin chains. Several DUBs have been implicated in various diseases and are attractive drug targets. We have developed a sensitive
Virdee, Satpal; id_orcid, Gray, Nathanael, Trost, Matthias, Ritorto, Maria Stella, Gray, Nathanael S., Alessi, Dario R., Perez-Oliva, Ana B., Wood, Nicola T., Alessi, Dario R.; id_orcid, Knebel, Axel, Buhrlage, Sara J., Ewan, Richard, Wightman, Melanie, Morrice, Nicholas A., Virdee, Satpal, Kelly, Sharon M.   +15 more
core   +1 more source

Deep learning-assisted high-content screening identifies isoliquiritigenin as an inhibitor of DNA double-strand breaks for preventing doxorubicin-induced cardiotoxicity

Biology Direct, 2023
Background Anthracyclines including doxorubicin are essential components of many cancer chemotherapy regimens, but their cardiotoxicity severely limits their use.
Xuechun Chen, Changtong Liu, Hong Zhao, Yigang Zhong, Yizhou Xu, Yi Wang   +5 more
doaj   +1 more source

Rapid fluorescence-based reporter-gene assays to evaluate the cytotoxicity and antitumor drug potential of platinum complexes [PDF]

, 1999
BackgroundThe need for new platinum antitumor drugs is underscored by the usefulness of cisplatin and carboplatin in chemotherapy and the resistance of many tumors to these compounds.
Lippard, Stephen J, Gregor Zlokarnik, Karen E Sandman, Sudhakar S Marla, Zlokarnik, Gregor, Marla, Sudhakar S, Sandman, Karen E, Stephen J Lippard   +7 more
core   +1 more source

A low-molecular-weight compound exerts anticancer activity against breast and lung cancers by disrupting EGFR/Eps8 complex formation

Journal of Experimental & Clinical Cancer Research, 2019
Background Epidermal growth factor receptor (EGFR) and epidermal growth factor receptor pathway substrate 8 (Eps8) have been widely reported to be expressed in various tumors.
Meifang Li, Jilong Yang, Lenghe Zhang, Sanfang Tu, Xuan Zhou, Ze Tan, Weijun Zhou, Yanjie He, Yuhua Li   +8 more
doaj   +1 more source

On the discovery of a potential survivin inhibitor combining computational tools and cytotoxicity studies

Heliyon, 2019
Survivin protein is a metalloprotein member of the inhibitors of apoptosis proteins family, involved in the regulation of programmed cell death. Due to the recent development of antitumor therapies having survivin as molecular target, several strategies ...
Patricia A. Quispe, Martin J. Lavecchia, Ignacio E. León   +2 more
doaj   +1 more source