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Inside Perspective of the Synthetic and Computational Toolbox of JAK Inhibitors: Recent Updates

Adriana Coricello1, Francesco Mesiti1,2, Antonio Lupia2

  • 1Dipartimento di Scienze della Salute, Università "Magna Græcia" di Catanzaro, Viale Europa, 88100 Catanzaro, Italy.

Molecules (Basel, Switzerland)
|July 26, 2020
PubMed

Insights

Janus kinase (JAK) inhibition shows promise for treating inflammatory diseases and cancer. Recent advancements in JAK inhibitors, including structural insights and improved synthesis, support drug repurposing and multitarget strategies.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Inflammation and cancer share complex signaling pathways, with Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway dysregulation implicated in chronic inflammation, autoimmune diseases, and cancer.
  • The JAK/STAT pathway is a critical mediator in these conditions, making it a significant therapeutic target.

Purpose of the Study:

  • To review recent advancements in Janus kinase (JAK) inhibition for therapeutic applications.
  • To highlight innovations in JAK inhibitor development, including structural biology and synthetic strategies.
  • To explore the potential of JAK inhibitors in drug repurposing and multitarget therapeutic approaches.

Main Methods:

  • Literature review of recent progress in JAK inhibition.
  • Analysis of innovations stemming from JAK crystal structure elucidation.
  • Assessment of improved synthetic strategies for industrial scale-up.

Main Results:

  • Five JAK inhibitors are currently FDA-approved for various diseases, demonstrating clinical efficacy.
  • Advances in understanding JAK structures and synthetic methodologies are facilitating inhibitor development.
  • JAK inhibitors present opportunities for drug repurposing and multitargeting due to their role in multiple disorders.

Conclusions:

  • JAK inhibition is a validated therapeutic strategy for inflammatory and cancerous conditions.
  • Ongoing innovations in JAK inhibitor design and synthesis are expanding their clinical utility.
  • The repurposing of JAK inhibitors and the development of multitarget strategies hold significant therapeutic potential.
Keywords:
Janus kinase (JAK)cancerinflammationmultitargetruxolitinibsynthetic strategiestofacitinib

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