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Related Concept Videos

The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

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Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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Inhibitors of Viral Protein Synthesis01:30

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Protein synthesis is indispensable for viral replication, as viruses lack the cellular machinery required for this process and must hijack the host's translational apparatus. In response, host cells deploy a critical innate immune defense involving interferons, specialized cytokines that play a central role in inhibiting viral propagation.Upon viral detection, infected cells release interferons that bind to receptors on adjacent uninfected cells, activating the JAK-STAT signaling pathway and...
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The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
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Selective JAK inhibitors.

Brian W Dymock1, Eugene Guorong Yang, Yuyi Chu-Farseeva

  • 1Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543.

Future Medicinal Chemistry
|October 21, 2014
PubMed
Summary
This summary is machine-generated.

Selective Janus kinase (JAK) inhibitors are crucial for treating immune and inflammatory diseases. Recent advancements show promising clinical applications for these targeted therapies in oncology and autoimmune conditions.

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Area of Science:

  • Pharmacology
  • Immunology
  • Oncology

Background:

  • Janus kinases (JAKs), comprising JAK1, JAK2, JAK3, and TYK2, are key targets for managing proliferative and immune-inflammatory disorders.
  • The development of selective inhibitors for each JAK isoform represents a significant advancement in targeted therapy.

Purpose of the Study:

  • To summarize the current landscape of selective JAK inhibitors.
  • To discuss recent discoveries and clinical progress in JAK inhibitor development.

Main Methods:

  • Review of recently described selective JAK inhibitor compounds.
  • Analysis of X-ray co-crystal structures to understand biochemical selectivity.
  • Evaluation of clinical trial data and therapeutic indications.

Main Results:

  • Significant progress has been made in discovering selective inhibitors for all four JAK isoforms.
  • X-ray crystallography provides molecular insights into the basis of observed selectivity.
  • Increased clinical trial activity and a diversity of indications for JAK inhibitors are evident.

Conclusions:

  • Selective JAK inhibitors demonstrate considerable promise as monotherapies or combination treatments.
  • These targeted agents are poised for significant roles in treating oncology, immune, and inflammatory diseases.