Publications by authors named "Bettina Quade"

Protein ubiquitination plays an important role in the regulation of almost every aspect of eukaryotic cellular function; therefore, its destabilization is often observed in most human diseases and cancers. Consequently, developing inhibitors of the ubiquitination system for the treatment of cancer has been a recent area of interest. Currently, only a few classes of compounds have been discovered to inhibit the ubiquitin-activating enzyme (E1) and only one class is relatively selective in E1 inhibition in cells.

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Unique chemical methodology enables the synthesis of innovative and diverse scaffolds and chemotypes and allows access to previously unexplored "chemical space." Compound collections based on such new synthetic methods can provide small-molecule probes of proteins and/or pathways whose functions are not fully understood. We describe the identification, characterization, and evolution of two such probes.

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Article Synopsis
  • The kidneys regulate fluid balance, maintain acid-base and electrolyte levels, and excrete metabolic waste, highlighting their essential functions in the body.
  • The study investigated the human uric acid transporter 1 (hURAT1) using Xenopus oocytes to test new compounds that inhibit uric acid uptake, which is linked to conditions like gout.
  • Results showed that certain modified benzofuran compounds exhibited strong inhibitory activity on hURAT1, with some achieving submicromolar effectiveness, indicating potential for developing treatments targeting uric acid secretion.
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