Results 1 to 10 of about 346 (65)
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 ...
Laurence H Arnold +2 more
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Frontiers in Molecular Biosciences, 2022 Knowing that the drug candidate binds to its intended target is a vital part of drug discovery. Thus, several labeled and label-free methods have been developed to study target engagement.
Tuomas Aleksi Tolvanen +1 more
exaly +3 more sources
Cell ReportsSummary: Cellular phenotypes of apoptosis, as well as the activation of apoptosis caspase cascades, are well described. However, sequences and locations of early biochemical effector events after apoptosis initiation are still only partly understood ...
Anderson Daniel Ramos +15 more
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PlateletsSmall molecule drugs play a major role in the study of human platelets. Effective action of a drug requires it to bind to one or more targets within the platelet (target engagement). However, although in vitro assays with isolated proteins can be used to
Matthew Thomas Harper
exaly +3 more sources
Cost-Efficient Task Scheduling Algorithm for Reducing Energy Consumption and Makespan of Cloud Computing [PDF]
Computer and Knowledge Engineering, 2022 In cloud computing, task scheduling is one of the most important issues that need to be considered for enhancing system performance and user satisfaction.
najme mansouri, Reyhane ghafari
doaj +1 more source
STAR Protocols, 2022 Summary: Pharmacologic inhibition of the protein-protein interaction (PPI) interface of the Keap1:Nrf2 complex, which leads to Nrf2 activation and cytoprotective gene expression, offers a promising strategy for disease prevention and treatment.
Sharadha Dayalan Naidu +3 more
doaj +1 more source
A high content, high throughput cellular thermal stability assay for measuring drug-target engagement in living cells. [PDF]
PLoS ONE, 2018 Determining and understanding drug target engagement is critical for drug discovery. This can be challenging within living cells as selective readouts are often unavailable.
Andrew J Massey
doaj +1 more source
Pharmaceuticals, 2022 Metastasis, in which cancer cells migrate to other tissues and form new tumors, is a major cause of both cancer death and treatment failure. In a previous study, benproperine (Benp) was identified as a cancer cell migration inhibitor and an inhibitor of ...
Hyun-Jin Jang +9 more
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Military Medical Research, 2022 Background Malaria is a devastating infectious disease that disproportionally threatens hundreds of millions of people in developing countries. In the history of anti-malaria campaign, chloroquine (CQ) has played an indispensable role, however, its ...
Peng Gao +19 more
doaj +1 more source
Biomedicines, 2021 Tetradecyl 2,3-dihydroxybenzoate (ABG-001) is a lead compound derived from gentisides with a remarkable neuritogenic activity. However, the target of ABG-001 is yet to be defined to date.
Lihong Cheng +3 more
doaj +1 more source