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In Vitro Ubiquitination Platform Identifies Methyl Ellipticiniums as Ubiquitin Ligase Inhibitors

期刊: SLAS DISCOVERY, 2021; 26 (7)

The transfer of the small protein ubiquitin to a target protein is an intricately orchestrated process called ubiquitination that results in modulatio......

Development and Validation of High-Content Analysis for Screening HDAC6-Selective Inhibitors

期刊: SLAS DISCOVERY, ; ()

Throughout recent decades, histone deacetylase (HDAC) inhibitors have shown encouraging potential in cancer treatment, and several pan-HDAC inhibitors......

Selecting Approaches for Hit Identification and Increasing Options by Building the Efficient Discovery of Actionable Chemical Matter from DNA-Encoded Libraries

期刊: SLAS DISCOVERY, 2021; 26 (2)

Over the past 20 years, the toolbox for discovering small-molecule therapeutic starting points has expanded considerably. Pharmaceutical researchers c......

Identification of Novel Compounds Enhancing SR-BI mRNA Stability through High-Throughput Screening

期刊: SLAS DISCOVERY, 0; ()

Atherosclerosis is the pathological basis of most cardiovascular diseases. Reverse cholesterol transport (RCT) is a main mechanism of cholesterol home......

Exploring the Lower Limit of Individual DNA-Encoded Library Molecules in Selection

期刊: SLAS DISCOVERY, 0; ()

DNA-encoded library (DEL) technology has been used as an ultra-high-throughput screening approach for hit identification of drug targets. This process......

Generation of a Monoclonal Antibody against D-Dimer Using HTS-Based LiCA

期刊: SLAS DISCOVERY, 0; ()

D-dimer is an essential diagnostic index of thrombotic diseases. Since the existing anti-D-dimer antibodies vary in quality and specificity, a search ......

Development of a Bacterial Macroarray for the Rapid Screening of Targeted Antibody-Secreted Hybridomas

期刊: SLAS DISCOVERY, 2019; 24 (2)

Hybridoma screening is a key step for the successful generation of high-affinity analyte-specific monoclonal antibodies (MAbs). This work presents an ......

JIF:2.19

Addition of Optimized Bovine Serum Albumin Level in a High-Throughput Caco-2 Assay Enabled Accurate Permeability Assessment for Lipophilic Compounds

期刊: SLAS DISCOVERY, 2019; 24 (7)

The Caco-2 permeability assay is a well-accepted in vitro model to evaluate compounds' potential for oral absorption at early discovery. However, for ......

JIF:2.19

Amoxapine Demonstrates Incomplete Inhibition of beta-Glucuronidase Activity from Human Gut Microbiota

期刊: SLAS DISCOVERY, 2018; 23 (1)

Amoxapine has been demonstrated to be a potent inhibitor of Escherichia coli beta-glucuronidase. This study aims to explore the factors causing unsati......

JIF:2.19

The Development of a Biotinylated NAD(+)-Applied Human Poly(ADP-Ribose) Polymerase 3 (PARP3) Enzymatic Assay

期刊: SLAS DISCOVERY, 2018; 23 (6)

Poly(ADP-ribose) polymerase 3 (PARP3) is an important member of the PARP family and shares high structural similarities with both PARP1 and PARP2. The......

JIF:2.19

Quantitative Algorithm-Based Paired Imaging Measurement for Antibody-Triggered Endocytosis in Cultured Cells

期刊: SLAS DISCOVERY, 2018; 23 (8)

Antibody-triggered endocytosis (ATE) is a biological mechanism on which many therapeutic strategies are grounded, such as delivery of antibody-drug co......

JIF:2.19

Discovery of SARS-CoV-2 main protease covalent inhibitors from a DNA-encoded library selection

期刊: SLAS DISCOVERY, 2022; 27 (2)

Covalent inhibitors targeting the main protease (M-pro, or 3CLpro) of SARS-CoV-2 have shown promise in preclinical investigations. Herein, we report t......

DeepTI: A deep learning-based framework decoding tumor-immune interactions for precision immunotherapy in oncology

期刊: SLAS DISCOVERY, 2022; 27 (2)

Background: Increasing evidence suggests the immunomodulatory potential of genes in oncology. But the identification of immune attributes of genes is ......

Adipocyte-based high throughput screening for anti-obesity drug discovery: Current status and future perspectives

期刊: SLAS DISCOVERY, 2022; 27 (7)

Drug discovery for obesity treatment, particularly bodily slimming, is a topic of timely importance that requires continued investigation, as the curr......

Development of a biotin-streptavidin-enhanced enzyme-linked immunosorbent assay (BA-ELISA) for high-throughput screening of KRAS(G12C) inhibitors

期刊: SLAS DISCOVERY, 2022; 27 (2)

KRAS, the most frequently mutated oncogene in human cancers, was considered undruggable until the identification of small molecules that bind irrevers......

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