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We note some areas for improvement, including increasing the rate of deacetylation and improving selectivity for a single HDAC isoform, which may be accomplished through future structural modifications.
Structure-based methods were used to design β-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13.
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The spectroelectrochemical sensor combines in a single device electrochemistry, spectroscopy, and selective partitioning into a film, giving improved selectivity for applications that involve complex samples.
Several different conditions can be varied to improve selectivity for reversed-phase chromatography (RPC).
Compound 6 showed improved selectivity for JAK1 compared to that of tofacitinib (IC50 11, 2.4 × 102, 2.8 × 103, and 1.1 × 102 nM for JAK1, JAK2, JAK3, and TYK2, respectively).
We further describe design strategies that utilize the ponatinib scaffold to develop two classes of inhibitors (CS and PN series), each with greatly improved selectivity for RIPK1.
We recently reported the design and synthesis of conformationally restricted analogs (e.g., 2) with improved selectivity for inhibiting invasion versus acute cytotoxicity.
X-ray crystallography and structure-based drug design were used to improve selectivity for RARγ by targeting residue differences in the ligand binding pockets of these receptors.
Members of this series were designed to improve selectivity for MC4R versus the other melanocortin receptors, and to reduce the flexibility of the side chains.
These reactors offer improved selectivity for some classes of complex reactions under non-isothermal conditions or when composition modulation is employed.
Catalyst-enabled reduction of the working potential under CPA was found to improve selectivity for NO over high potential interferents, regardless of MPc.
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