A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells [PDF]
Hypoxia inducible factor-1 (HIF-1) is a heterodimeric transcription factor that acts as the master regulator of cellular response to reduced oxygen levels, thus playing a key role in the adaptation, survival and progression of tumors.
Court, William+11 more
core +1 more source
Quantitative Cell-based Protein Degradation Assays to Identify and Classify Drugs That Target the Ubiquitin-Proteasome System [PDF]
We have generated a set of dual-reporter human cell lines and devised a chase protocol to quantify proteasomal degradation of a ubiquitin fusion degradation (UFD) substrate, a ubiquitin ligase CRL2^(VHL) substrate, and a ubiquitin-independent substrate ...
Aghajan+50 more
core +3 more sources
Visual and computational analysis of structure-activity relationships in high-throughput screening data [PDF]
Novel analytic methods are required to assimilate the large volumes of structural and bioassay data generated by combinatorial chemistry and high-throughput screening programmes in the pharmaceutical and agrochemical industries. This paper reviews recent
Agrafiotis+75 more
core +1 more source
A high-throughput screening method for determining the substrate scope of nitrilases [PDF]
Nitrile compounds are intermediates in the synthesis of pharmaceuticals such as atorvastatin. We have developed a chromogenic reagent to screen for nitrilase activity as an alternative to Nessler's reagent. It produces a semi-quantifiable blue colour and
Black, Gary+5 more
core +1 more source
New compound sets identified from high throughput phenotypic screening against three kinetoplastid parasites:an open resource [PDF]
Using whole-cell phenotypic assays, the GlaxoSmithKline high-throughput screening (HTS) diversity set of 1.8 million compounds was screened against the three kinetoplastids most relevant to human disease, i.e.
Alonso-Padilla, Julio+20 more
core +2 more sources
Iterative focused screening with biological fingerprints identifies selective Asc-1 inhibitors distinct from traditional high throughput screening [PDF]
N-methyl-d-aspartate receptors (NMDARs) mediate glutamatergic signaling that is critical to cognitive processes in the central nervous system, and NMDAR hypofunction is thought to contribute to cognitive impairment observed in both schizophrenia and ...
Amoss, Adam+18 more
core +2 more sources
Microfluidic Platform for Adherent Single Cell High-Throughput Screening [PDF]
This paper was presented at the 4th Micro and Nano Flows Conference (MNF2014), which was held at University College, London, UK. The conference was organised by Brunel University and supported by the Italian Union of Thermofluiddynamics, IPEM, the ...
4th Micro and Nano Flows Conference (MNF2014)+7 more
core
In-silico Predictive Mutagenicity Model Generation Using Supervised Learning Approaches [PDF]
With the advent of High Throughput Screening techniques, it is feasible to filter possible leads from a mammoth chemical space that can act against a particular target and inhibit its action.
Abhik Seal+4 more
core +2 more sources
Optimization of Protein-Protein Interaction Measurements for Drug Discovery Using AFM Force Spectroscopy [PDF]
Increasingly targeted in drug discovery, protein-protein interactions challenge current high throughput screening technologies in the pharmaceutical industry.
Basson, Marc D.+11 more
core +1 more source
Enabling Solar Fuels Technology With High Throughput Experimentation [PDF]
The High Throughput Experimentation (HTE) project of the Joint Center for Artificial Photosynthesis (JCAP, http://solarfuelshub.org/) performs accelerated discovery of new earth-abundant photoabsorbers and electrocatalysts.
Becerra, N.+13 more
core +1 more source