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September 18, 2025ChemMedChemOpen Access

Development of a Partial Proteolysis Targeting Chimera Library Based on Achiral Cereblon E3 Ligase Ligands and its Application for Bruton's Tyrosine Kinase Degraders

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Authors

CAChelsi M. Almodóvar‐RiveraITIra TandonRMRamesh Mudududdla

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Overview

This research demonstrates improved PROTACs targeting Bruton's tyrosine kinase using novel achiral ligands, highlighting their potential for efficient drug development.

Key Points

  • Nine hits capable of significant BTK degradation were identified, with compound B1 as the most potent.
  • The novel achiral ligands enhance stability and eliminate racemization challenges, promising better therapeutic options.
  • Utilizing a partial PROTAC library allowed for rapid generation and screening of effective BTK degraders.
  • Mechanistic studies confirmed BTK degradation occurs via the ubiquitin–proteasome system, indicating effective targeting.

Cite This Study

Almodóvar‐Rivera et al. (2025) studied this question.

synapsesocial.com/papers/68d435cf713b0b5dfea74df6https://doi.org/10.1002/cmdc.202500209
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions2025
  2. 2Proteolysis-targeting chimera (PROTAC) targeting bruton tyrosine kinase (BTK) degradation for cancer therapy in mantle cell lymphoma2025
  3. 3Synthesis and Application of BRD4‐Targeting ByeTACs (Bypassing E‐Ligase Targeting Chimeras)2025
  4. 4Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs2025
  5. 5Discovery of a CNS active GSK3 degrader using orthogonally reactive linker screening2025