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April 10, 2026Journal of Medicinal ChemistryOpen Access

Leveraging Kinase Drugs for Neurosciences: Discovery of Selective, CNS-Penetrant Reversible Bruton’s Tyrosine Kinase Inhibitors as Therapeutics for Neuroinflammation

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Authors

BHBrian T. HopkinsIMIsaac E. MarxHVHarlod George Vandeveer

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Overview

This discovery reveals reversible BTK inhibitors effective against neuroinflammation, suggesting new therapeutic avenues.

Key Points

  • The aim is to discover a selective, CNS-penetrant reversible BTK inhibitor for treating neuroinflammation.
  • Designed a reversible BTK inhibitor targeting the phosphorylation site Tyr-551.
  • Evaluated safety at doses inhibiting peripheral B-cell activity.
  • Assessed CNS exposure and its effects on microglia.
  • The inhibitor effectively blocked BCR signaling through BTK inhibition.
  • Excellent safety profile was observed at doses effective in the periphery.
  • Increased CNS exposure raised concerns of off-target toxicity or microglial BTK inhibition consequences.

Cite This Study

Hopkins et al. (2026) studied this question.

synapsesocial.com/papers/69d8948f6c1944d70ce058abhttps://doi.org/10.1021/acs.jmedchem.5c02648
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Also Consider

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

  1. 1Bruton's Tyrosine Kinase: Pathophysiological Roles and Inhibitor‐Based Therapeutic Advances2026
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  4. 4Targeting Bruton’s Tyrosine Kinase in CLL: Selectivity, Resistance Mechanisms, and Emerging Therapeutic Strategies2026
  5. 5Bruton’s tyrosine kinase (BTK) inhibitors: an updated patent review (2019-2024)2025