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SLAS Discovery
Scopus
ISSN 2472-5552 · Elsevier · 283 artikel di indeks
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Artikel Jurnal
MICRO-TAG enzyme complementation enables quantification of cellular drug-target engagement in temperature series
Drug discovery for challenging drug targets necessitates the proteomic complexities of the cellular milieu for contextual target folding and function. Conventional biophysical methods for assessing drug interaction with a target are often not sufficiently suited for drug discovery as they impose…
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Artikel Jurnal
Binder2030: a quantitative membrane proteome binding dataset enabling AI-driven drug discovery
Membrane proteins represent more than half of therapeutic targets but remain underrepresented in quantitative ligand-binding datasets. Here we report Binder2030, a curated affinity selection–mass spectrometry (ASMS) dataset comprising 3384 small-molecule ligands across approximately 400…
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Artikel Jurnal
Application of a MALDI mass spectrometry assay to identify covalent fragments targeting the methyl-lysine reader protein MPP8
In recent decades, the development of targeted covalent inhibitors (TCIs) has significantly advanced, as evidenced by the increasing number of FDA approved drugs with covalent mechanisms of action. This study focuses on the application of a robust and efficient screening platform to identify…
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AI-based analysis of label-free live cell imaging of T-cell mediated tumor killing assay enables competitive and robust hit calling
For the discovery and optimization of personalized cancer treatments using immune cell therapeutics, such as T-cell receptor (TCR-T) therapy and bispecific antibodies (BsAbs), robust functional activity of candidates must be confirmed in immune-mediated killing assays. In these assays, co-cultures…
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Artikel Jurnal
An MRC-5 cell based high-throughput, high-content imaging assay to identify hits against Trypanosoma cruzi intracellular parasites
The discovery of effective therapies for Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease, remains one of the most pressing challenges in parasitology and global health. Despite the significant burden posed by Chagas disease, especially in Latin America, only two drugs…
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Artikel Jurnal
MitoLatentProfiler: ROI-constrained deep learning for mitochondrial phenotyping in human myotubes
Mitochondrial network organization in skeletal muscle reflects metabolic health and is disrupted in primary mitochondrial myopathies, type 2 diabetes/insulin resistance, and age-related functional decline. Studying these disruptions in vitro using mature human myotubes is, however, complicated by…
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Artikel Jurnal
High-content imaging workflow for single-cell drug response profiling of acute myeloid leukemia subtypes
Acute myeloid leukemia (AML) exhibits pronounced cellular heterogeneity, which contributes to variable therapeutic responses and limits the predictive power of conventional functional assays. While bulk viability measurements provide aggregated readouts, they fail to resolve phenotypic diversity…
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Artikel Jurnal
From phenotypic screening to target and compound prioritization for autosomal dominant polycystic kidney disease
Autosomal Dominant Polycystic Kidney Disease (ADPKD) is a progressive kidney disorder with limited therapeutic options, highlighting an urgent need for safer, long-term treatments. This study presents a multi-step computational and experimental approach to identify and assess target-based…
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Artikel Jurnal
Probing and painting to get the full picture of macrophage polarisation
Macrophages play central roles in tissue repair and remodelling, host defence and immunopathology. Their ability to rapidly reprogram key functions in response to local cues makes them attractive targets for drug discovery. While this plasticity creates therapeutic opportunities, it also…
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Artikel Jurnal
Hit selection using SSMD-based machine learning performance metrics in high-throughput screening assays
High-throughput screening (HTS) assays are central to early-stage drug discovery but are often limited by extreme data sparsity, as primary screens typically use only a single replicate per test substance. This sparsity makes conventional machine-learning performance metrics, such as sensitivity…
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Artikel Jurnal
ADCs for colorectal carcinoma: decoding clinical evidence for molecular design innovation
Antibody-drug conjugate (ADC) is a novel type of targeted systemic therapy that is changing the current landscape of tumor treatment. By integrating the specificity of antibodies with the cytotoxic effects of their payloads, ADCs facilitate precise tumor killing. In solid tumors such as breast…
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Artikel Jurnal
CellVision: A deep learning based image analysis platform to accelerate immuno-plaque assay data processing for dengue vaccine development
Accurately detecting patterns of interest across a large number of images presents a significant challenge in data analysis for high-throughput analytical assays. In many cases, manual image review to some degree is necessary, deviating from a fully automated workflow desired in high-throughput…
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Artikel Jurnal
Forecasting a clear vision: How QSAR modeling catalyzes small molecule discovery in the field of corneal endothelial regeneration
The corneal endothelium executes its crucial role in the maintenance of corneal transparency by regulating the corneal hydration levels. Dysfunction of the endothelial layer leads to corneal edema, i.e. bullous keratopathy, for which an endothelial transplantation is currently the only available…
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Development of diversified HTS cell-based assays for solute carrier drug discovery
Solute carrier (SLC) transporters comprise a family of >450 membrane-bound proteins that facilitate the transport of a wide array of substrates across biological membranes. They play a fundamental role in controlling the transport of molecules, such as ions and metabolites, across the cell…
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Artikel Jurnal
Acoustic ejection native mass spectrometry for high-throughput protein-ligand screening
Native mass spectrometry (nMS) enables direct analysis of non-covalent protein-ligand interactions, providing information on binding, stoichiometry, and protein oligomeric state. In drug discovery, nMS is widely used for mechanistic protein-ligand characterization and for confirming hits identified…
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Artikel Jurnal
Application of dual-view oblique plane microscopy to small-molecule compound screening across 3D glioblastoma stem cell spheroids with single-cell resolution
Recent advances and increasing adoption of 3-dimensional (3D) model systems, such as tumour spheroids and organoids, attempt to more faithfully recapitulate the pathophysiology and heterogeneity observed in patients’ tumours, with the goal of reducing high attrition rates observed in late stage…
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Artikel Jurnal
AI-driven identification of Zika virus inhibitors
Research engaged with AI has dramatically increased due to a huge improvement of technologies in terms of cost and time-effectiveness as well as decreasing use of animals. High throughput screening (HTS) is a frequently used method in drug discovery. Here, we combined two powerful tools for…
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Modern therapies: Nanotechnology promises new approaches for rare breast cancer brain metastases
Brain metastasis originating from breast cancer is an uncommon but clinically significant complication that poses substantial therapeutic challenges and is associated with poor patient prognosis. Traditional treatment modalities—including surgical resection, whole-brain radiation therapy…
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A high throughput screening platform for label-free identification and characterization of GPCR ligands using impedance-based real-time cellular analysis
Real-time cell analysis (RTCA) is a biosensor technology that enables kinetic monitoring of cellular activities via electrical impedance. Among its multiple applications, this label-free method offers a holistic approach to monitoring the activity of G protein-coupled receptors (GPCRs) by capturing…
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Artikel Jurnal
Three high throughput compatible cell-based assays for identifying small molecule JAG1 upregulators for Alagille syndrome
Haploinsufficiency disorders arise when loss of function mutations in one allele of a gene reduce gene dosage below the level required for normal physiology. Pharmacologic upregulation of the remaining functional allele represents a promising therapeutic strategy but requires screening assays…