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Janus Kinase JAK Inhibitors - Biotech, Pharma and Life Science Channel

22:13 EDT 24th May 2013 | BioPortfolio

As cytokines play pivotal roles in immunity and inflammation, targeting of cytokines and their receptors represents an effective means of treating such diseases. Janus kinases (JAK) are a small family of receptor-associated kinases, that together with signal transducers and activators of transcription (STAT), provide a rapid signalling pathway for cytokines. Four JAKs have been identified: JAK1, JAK2, JAK3 and tyrosine kinase 2 (Tyk2). JAK3 has attracted much attention as an anti-inflammatory drug target because of its restricted hematopoietic tissue expression and because of its specific association with the common gamma chain of the interleukin-2 (IL-2) receptor which is shared by the receptors for IL-4, IL-7, IL-9, IL-15 and IL-21. Quite a number of companies are developing selective JAK3 inhibitors as JAK3 appears not to have functions outside of hematopoetic cells. Pfizer leads the field with evaluation of JAK3 inhibition in a number of inflammatory diseases including rheumatoid arthritis, ulcerative colitis, Crohn's disease and psoriasis. JAK2 gain-of-function mutations (JAK2V617F) underlie a subset of disorders collectively referred to as myeloproliferative disorders. The most advanced JAK2 inhibitors are also being evaluated in phase II trials for myelofibrosis, polycythemia vera and essential thrombocythemia.

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Medical and Biotech [MESH] Definitions

Taxodium

A plant genus of the family TAXODIACEAE. Members contain taxodione and taxodone, which are diterpenoid quinone methide tumor inhibitors.

Huperzia

A plant genus of the family LYCOPODIACEAE. Members contain huperzine, one of the CHOLINESTERASE INHIBITORS.

Receptor, Ephb6

An eph family receptor found primarily in BRAIN and THYMUS. The EphB6 receptor is unusual in that its tyrosine kinase domain shares little homology with other members of this class. The unusual tyrosine kinase domain of this receptor appears to result in its lack of tyrosine kinase activity.

Glycogen Synthase Kinase 3

A glycogen synthase kinase that was originally described as a key enzyme involved in glycogen metabolism. It regulates a diverse array of functions such as CELL DIVISION, microtubule function and APOPTOSIS.

Ribosomal Protein S6 Kinases, 90-kda

A family of ribosomal protein S6 kinases that are structurally distinguished from RIBOSOMAL PROTEIN S6 KINASES, 70-KDA by their apparent molecular size and the fact they contain two functional kinase domains. Although considered RIBOSOMAL PROTEIN S6 KINASES, members of this family are activated via the MAP KINASE SIGNALING SYSTEM and have been shown to act on a diverse array of substrates that are involved in cellular regulation such as RIBOSOMAL PROTEIN S6 and CAMP RESPONSE ELEMENT-BINDING PROTEIN.

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