Results 11 to 20 of about 241,105 (256)

A perspective on the discovery of enzyme activators

SLAS Discovery, 2022
Enzyme activation remains a largely under-represented and poorly exploited area of drug discovery despite some key literature examples of the successful application of enzyme activators by various mechanisms and their importance in a wide range of ...
Antonia Turberville, Hannah Semple, Gareth Davies, Delyan Ivanov, Geoffrey A. Holdgate   +4 more
doaj   +1 more source

High throughput screening of 0.5 million compounds against CRAF using Alpha CETSAⓇ

SLAS Discovery, 2023
The cellular thermal shift assay (CETSA®) has increasingly been used in early drug discovery to provide a measure of cellular target engagement. Traditionally, CETSA has been employed for bespoke questions with small to medium throughput and has ...
Hannah Rowlands, Kirsten Tschapalda, Carolyn Blackett, Delyan Ivanov, Darren Plant, Joseph Shaw, Andrew Thomas, Martin Packer, Laurence Arnold, Geoffrey A. Holdgate   +9 more
doaj   +1 more source

A Novel Approach To Identify Inhibitors of Iron Acquisition Systems of Pseudomonas aeruginosa

Microbiology Spectrum, 2022
Pseudomonas aeruginosa is an opportunistic pathogen that has been declared by the World Health Organization as a “priority 1 critical pathogen” needing immediate new strategies for chemotherapy. During infection, P.
Mamie Kannon, N. Miranda Nebane, Pedro Ruiz, Sara McKellip, Paige N. Vinson, Avishek Mitra   +5 more
doaj   +1 more source

EndoBind detects endogenous protein-protein interactions in real time

Communications Biology, 2021
Bill et al describe two high-throughput methods to detect protein-protein interactions in cells in real-time using the split-NanoLuciferase-complementation system.
Anke Bill, Sheryll Espinola, Daniel Guthy, Jacob R. Haling, Mylene Lanter, Min Lu, Anthony Marelli, Angelica Mendiola, Loren Miraglia, Brandon L. Taylor, Leonardo Vargas, Anthony P. Orth, Frederick J. King   +12 more
doaj   +1 more source

Utilising acoustic mist ionisation mass spectrometry to identify redox cycling compounds in high throughput screening outputs

SLAS Discovery, 2022
Rapid triage of compounds acting via undesired mechanisms is a crucial stage in a high-throughput screening (HTS) cascade to ensure time and resource is efficiently assigned to the most propitious hits.
Rachel Moore, Corinne Molyneux, Ian Sinclair, Geoffrey A. Holdgate, Jarrod Walsh   +4 more
doaj   +1 more source

High-throughput detection of metal contamination in HTS outputs

SLAS Discovery, 2022
Large compound libraries utilised for HTS often include metal contaminated compounds which can interfere with assay signal or target biology, and therefore appear as hits.
Corinne Molyneux, Ian Sinclair, Helen L. Lightfoot, Jarrod Walsh, Geoffrey A. Holdgate, Rachel Moore   +5 more
doaj   +1 more source

Interplay between transforming growth factor-β and Nur77 in dual regulations of inhibitor of differentiation 1 for colonic tumorigenesis

Nature Communications, 2021
Inhibitor of Differentiation 1 (ID1) is an oncogene for colorectal cancer. Here, the authors show a complex interplay between nuclear receptor Nur77 and Transforming Growth Factor-β (TGFβ) to regulate ID1 expression at both transcriptional and post ...
Boning Niu, Jie Liu, Ben Lv, Jiacheng Lin, Xin Li, Chunxiao Wu, Xiaohua Jiang, Zhiping Zeng, Xiao-kun Zhang, Hu Zhou   +9 more
doaj   +1 more source

Extracellular matrix stiffness mediates radiosensitivity in a 3D nasopharyngeal carcinoma model

Cancer Cell International, 2022
Purpose Radiotherapy is one of the essential treatment modalities for nasopharyngeal carcinoma (NPC), however, radioresistance still poses challenges.
Yanhua Fang, Shanshan Liang, Jianong Gao, Zhe Wang, Cheng Li, Ruoyu Wang, Weiting Yu   +6 more
doaj   +1 more source

Glc7/PP1 dephosphorylates histone H3T11 to regulate autophagy and telomere silencing in response to nutrient availability

Cell Discovery, 2023
How cells adapt their gene expression to nutritional changes remains poorly understood. Histone H3T11 is phosphorylated by pyruvate kinase to repress gene transcription.
Xinyu Zhang, Qi Yu, Yinsheng Wu, Yuan Zhang, Yi He, Rongsha Wang, Xilan Yu, Shanshan Li   +7 more
doaj   +1 more source

The Future of High-Throughput Screening

SLAS Discovery, 2008
High-throughput screening (HTS) is a well-established process in lead discovery for pharma and biotech companies and is now also being set up for basic and applied research in academia and some research hospitals. Since its first advent in the early to mid-1990s, the field of HTS has seen not only a continuous change in technology and processes but ...
Lorenz M, Mayr, Peter, Fuerst
openaire   +2 more sources