Reference Detail

Ref Type Journal Article
PMID (22819198)
Authors Kontzias A, Kotlyar A, Laurence A, Changelian P, O'Shea JJ
Title Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease.
Journal Current opinion in pharmacology
Vol 12
Issue 4
Date 2012 Aug
URL
Abstract Text Cytokines are critical for normal cell growth and immunoregulation but also contribute to growth of malignant cells and drive immune-mediated disease. A large subset of immunoregulatory cytokines uses the type I and type II cytokine receptors and pharmacological targeting of these cytokines/cytokines receptors has proven to be efficacious in treating immune and inflammatory diseases. These receptors rely on Janus family of kinases (Jaks) for signal transduction. Recently the first Jak inhibitor (jakinib) has been approved by the FDA and a second has been recommended for approval. Many other Jakinibs are likely to follow and in this brief review, we will discuss the state-of-the art of this new class of pharmacological agents.

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

Sorting

  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

Molecular Profile Treatment Approach
JAK3 P132A JAK3 Inhibitor - ATP competitive
JAK3 I87T JAK3 Inhibitor
JAK3 M576L JAK3 Inhibitor
JAK3 P132T JAK Inhibitor (Pan)
JAK3 A572T JAK Inhibitor (Pan) - ATP competitive
JAK3 V678M JAK Inhibitor (Pan) - ATP competitive
JAK3 A572T JAK3 Inhibitor - ATP competitive
JAK3 F666L JAK Inhibitor (Pan)
JAK3 E183G JAK3 Inhibitor
JAK3 act mut JAK3 Inhibitor - ATP competitive
JAK3 A572V JAK Inhibitor (Pan)
JAK3 V674A JAK3 Inhibitor - ATP competitive
JAK3 A572T JAK Inhibitor (Pan)
JAK3 M576L JAK Inhibitor (Pan) - ATP competitive
JAK3 P132A JAK3 Inhibitor
JAK3 P132T JAK3 Inhibitor - ATP competitive
JAK3 A572V JAK3 Inhibitor - ATP competitive
JAK3 I87T JAK Inhibitor (Pan) - ATP competitive
JAK3 act mut JAK Inhibitor (Pan)
JAK3 L156P JAK Inhibitor (Pan)
JAK3 F666L JAK3 Inhibitor
JAK3 L156P JAK3 Inhibitor - ATP competitive
JAK3 act mut JAK3 Inhibitor
JAK3 T848A JAK Inhibitor (Pan) - ATP competitive
JAK3 P132T JAK Inhibitor (Pan) - ATP competitive
JAK3 P132A JAK Inhibitor (Pan)
JAK3 M511I JAK3 Inhibitor - ATP competitive
JAK3 A573V JAK3 Inhibitor - ATP competitive
JAK3 P906S JAK3 Inhibitor - ATP competitive
JAK3 M511I JAK Inhibitor (Pan)
JAK3 E958K JAK3 Inhibitor - ATP competitive
JAK3 A573V JAK Inhibitor (Pan) - ATP competitive
JAK3 V678M JAK Inhibitor (Pan)
JAK3 I87T JAK3 Inhibitor - ATP competitive
JAK3 L857P JAK Inhibitor (Pan)
JAK3 R657W JAK3 Inhibitor - ATP competitive
JAK3 R172Q JAK Inhibitor (Pan) - ATP competitive
JAK3 L857Q JAK Inhibitor (Pan)
JAK3 T848A JAK Inhibitor (Pan)
JAK3 V674A JAK Inhibitor (Pan)
JAK3 R172Q JAK3 Inhibitor - ATP competitive
JAK3 P906S JAK Inhibitor (Pan)
JAK3 T848A JAK3 Inhibitor - ATP competitive
JAK3 V674A JAK Inhibitor (Pan) - ATP competitive
JAK3 L156P JAK3 Inhibitor
JAK3 P132A JAK Inhibitor (Pan) - ATP competitive
JAK3 V678M JAK3 Inhibitor
JAK3 R172Q JAK3 Inhibitor
JAK3 F666L JAK Inhibitor (Pan) - ATP competitive
JAK3 P906S JAK3 Inhibitor
JAK3 A572V JAK Inhibitor (Pan) - ATP competitive
JAK3 M511I JAK3 Inhibitor
JAK3 R657Q JAK3 Inhibitor - ATP competitive
JAK3 E183G JAK3 Inhibitor - ATP competitive
JAK3 Q501H JAK3 Inhibitor
JAK3 A572T JAK3 Inhibitor
JAK3 F666L JAK3 Inhibitor - ATP competitive
JAK3 L857H JAK Inhibitor (Pan) - ATP competitive
JAK3 L857H JAK Inhibitor (Pan)
JAK3 V722I JAK3 Inhibitor - ATP competitive
JAK3 V722I JAK Inhibitor (Pan)
JAK3 L857P JAK Inhibitor (Pan) - ATP competitive
JAK3 L156P JAK Inhibitor (Pan) - ATP competitive
JAK3 V722I JAK3 Inhibitor
JAK3 L857H JAK3 Inhibitor
JAK3 R657Q JAK Inhibitor (Pan)
JAK3 E183G JAK Inhibitor (Pan) - ATP competitive
JAK3 R657W JAK Inhibitor (Pan)
JAK3 L857H JAK3 Inhibitor - ATP competitive
JAK3 R657W JAK Inhibitor (Pan) - ATP competitive
JAK3 L857P JAK3 Inhibitor
JAK3 act mut JAK Inhibitor (Pan) - ATP competitive
JAK3 M511I JAK Inhibitor (Pan) - ATP competitive
JAK3 V722I JAK Inhibitor (Pan) - ATP competitive
JAK3 V674A JAK3 Inhibitor
JAK3 Q501H JAK3 Inhibitor - ATP competitive
JAK3 R172Q JAK Inhibitor (Pan)
JAK3 L857Q JAK3 Inhibitor - ATP competitive
JAK3 E958K JAK Inhibitor (Pan) - ATP competitive
JAK3 A573V JAK Inhibitor (Pan)
JAK3 L857P JAK3 Inhibitor - ATP competitive
JAK3 T848A JAK3 Inhibitor
JAK3 I87T JAK Inhibitor (Pan)
JAK3 A573V JAK3 Inhibitor
JAK3 A572V JAK3 Inhibitor
JAK3 R657Q JAK Inhibitor (Pan) - ATP competitive
JAK3 P906S JAK Inhibitor (Pan) - ATP competitive
JAK3 P132T JAK3 Inhibitor
JAK3 E183G JAK Inhibitor (Pan)
JAK3 R657W JAK3 Inhibitor
JAK3 V678M JAK3 Inhibitor - ATP competitive
JAK3 R657Q JAK3 Inhibitor
JAK3 Q501H JAK Inhibitor (Pan)
JAK3 M576L JAK Inhibitor (Pan)
JAK3 M576L JAK3 Inhibitor - ATP competitive
JAK3 E958K JAK Inhibitor (Pan)
JAK3 L857Q JAK3 Inhibitor
JAK3 Q501H JAK Inhibitor (Pan) - ATP competitive
JAK3 E958K JAK3 Inhibitor
JAK3 L857Q JAK Inhibitor (Pan) - ATP competitive
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References