Publications by authors named "M Entzeroth"

Background: Implementation of goal-directed fluid therapy (GDFT) protocols remains low. Protocol compliance among anesthesiologists tends to be suboptimal owing to the high workload and the attention required for implementation. The assisted fluid management (AFM) system is a novel decision support tool designed to help clinicians apply GDFT protocols.

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Article Synopsis
  • Apoptosis is often impaired in cancer cells due to overexpression of prosurvival Bcl-2 proteins, so BH3 mimetics—drugs designed to mimic natural apoptosis triggers—could help tackle chemoresistance.
  • Small molecule inhibitors targeting Bcl-X(L) have been developed using drug design and screening methods, but many have weaker affinities compared to natural BH3-only proteins.
  • The study suggests that using differential scanning fluorimetry (DSF) to validate these inhibitors uncovered varying selectivities; interactions with tagged versus untagged Bcl-X(L) indicate that the protein's conformation can influence drug selectivity, highlighting the need for more careful screening protocols.
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High-throughput screening (HTS) is a key process used in drug discovery to identify hits from compound libraries that may become leads for medicinal chemistry optimization. This updated overview discusses the utilization of compound libraries, compounds derived from combinatorial and parallel synthesis campaigns and natural product sources; creation of mother and daughter plates; and compound storage, handling, and bar coding in HTS. The unit also presents an overview of established and emerging assay technologies (i.

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A series of N-hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides were designed and synthesized as novel HDAC inhibitors. General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays.

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High throughput screening has significantly contributed to advances in drug discovery. The great increase in the number of samples screened has been accompanied by increases in costs and in the data required for the investigated compounds. High throughput profiling addresses the issues of compound selectivity and specificity.

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