Publications by authors named "A Kreamer"
Article Synopsis
- - Inhibiting Arginase 1 (ARG1), which breaks down l-arginine in the body, shows potential for boosting immune responses against various cancers in immuno-oncology treatments.
- - Most current ARG1 inhibitors are based on boronic acid; this research focuses on discovering new, non-boronic acid inhibitors through virtual screening methods.
- - The study utilized biophysical and biochemical techniques to analyze the promising candidates, with X-ray crystallography revealing a new class of trisubstituted pyrrolidine derivatives for potential cancer therapy development.
High-throughput phenotypic screening is a key driver for the identification of novel chemical matter in drug discovery for challenging targets, especially for those with an unclear mechanism of pathology. For toxic or gain-of-function proteins, small-molecule suppressors are a targeting/therapeutic strategy that has been successfully applied. As with other high-throughput screens, the screening strategy and proper assays are critical for successfully identifying selective suppressors of the target of interest.
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- * To streamline this process, researchers can start with a smaller subset of compounds and use virtual screening methods to prioritize which additional compounds to test, combining multiple screening techniques for better results.
- * A new method of combining these prioritizations was tested and showed to retrieve significantly more active compounds compared to using a single approach, improving the efficiency of drug discovery and guiding future screening strategies.
High-throughput siRNA screens are now widely used for identifying novel drug targets and mapping disease pathways. Despite their popularity, there remain challenges related to data variability, primarily due to measurement errors, biological variance, uneven transfection efficiency, the efficacy of siRNA sequences, or off-target effects, and consequent high false discovery rates. Data variability can be reduced if siRNA screens are performed in replicate.
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