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
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
Chronic hepatitis B is a critical cause of many serious liver diseases such as hepatocellular carcinoma (HCC). The main challenges in hepatitis B treatment include the rebound of hepatitis B virus (HBV)-related antigen levels after drug withdrawal and ...
Yan Mu +6 more
doaj +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 +3 more sources
Background: Hepatocellular carcinoma (HCC) is a highly malignant disease with poor prognosis. It is urgent to find effective biomarkers. Eukaryotic Translation Initiation Factor 2 Subunit Beta (EIF2S2) is a subunit of heterotrimeric G protein EIF2, and ...
Jing Liu +12 more
doaj +1 more source
Development and validation of a luminescence-based, medium-throughput assay for drug screening in Schistosoma mansoni [PDF]
Schistosomiasis, one of the world's greatest neglected tropical diseases, is responsible for over 280,000 human deaths per annum. Praziquantel, developed in the 1970s, has high efficacy, excellent tolerability, few and transient side effects, simple ...
Altamura, Sergio +5 more
core +3 more sources
Role of matrix metalloproteinases in diabetic foot ulcers: Potential therapeutic targets
Diabetic foot ulcers (DFUs) are pathological states of tissue destruction of the foot or lower extremity in diabetic patients and are one of the serious chronic complications of diabetes mellitus.
Kang Fu +11 more
doaj +1 more source
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
Animal testing for drug discovery is expensive and the decision to test a compound in an in vivo model should be carefully considered. In addition, the FDA Modernization Act has resulted in the allowance of alternatives to animal models for testing the ...
N. Miranda Nebane +7 more
doaj +1 more source
Multi-Behavioral Endpoint Testing Of An 87-Chemical Compound Library In Freshwater Planarians [PDF]
There is an increased recognition in the field of toxicology of the value of medium-to-high-throughput screening methods using in vitro and alternative animal models.
Collins, Eva-Maria S. +4 more
core +3 more sources

