Janus kinase

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{{#tree:id=OrganizedByTopic|openlevels=0|
{{#tree:id=OrganizedByTopic|openlevels=0|
-
*JAK1 kinase domain
+
*JAK1 kinase or JH1 domain residues 869-1153
**[[4e4l]], [[4e4n]], [[4e5w]], [[4ehz]], [[4ei4]], [[4fk6]], [[4i5c]], [[4k6z]], [[3eyg]], [[3eyh]], [[5e1e]], [[5hx8]], [[5khx]] – hJAK1 kinase domain + PTyr + inhibitor - human<br />
**[[4e4l]], [[4e4n]], [[4e5w]], [[4ehz]], [[4ei4]], [[4fk6]], [[4i5c]], [[4k6z]], [[3eyg]], [[3eyh]], [[5e1e]], [[5hx8]], [[5khx]] – hJAK1 kinase domain + PTyr + inhibitor - human<br />
**[[5khw]] – hJAK1 kinase domain + PTyr + ADP<br />
**[[5khw]] – hJAK1 kinase domain + PTyr + ADP<br />
 +
**[[6c7y]]]] – hJAK1 kinase domain + PTyr + SOCY1 + ADP<br />
 +
**[[4k77]], [[6bbu]], [[5wo4]] – hJAK1 JH1 domain + PTyr + inhibitor <br />
-
*JAK1 JH1 domain
+
*JAK1 pseudokinase domain
-
**[[4k77]] – hJAK1 JH1 domain + PTyr + inhibitor <br />
 
- 
-
*JAK1 pseudokinase domain
 
**[[4l00]] – hJAK1 pseudokinase domain <br />
**[[4l00]] – hJAK1 pseudokinase domain <br />
**[[4l01]] – hJAK1 pseudokinase domain (mutant)<br />
**[[4l01]] – hJAK1 pseudokinase domain (mutant)<br />
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**[[5ixi]] – hJAK1 + IFN l receptor/IL10 <br />
**[[5ixi]] – hJAK1 + IFN l receptor/IL10 <br />
-
*JAK2 kinase domain
+
*JAK2 kinase domain residues 536-812
**[[4fvp]] - hJAK2 kinase domain <br />
**[[4fvp]] - hJAK2 kinase domain <br />
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**[[4gl9]] – mJAK2 kinase domain + PTyr + inhibitor + suppressor of cytokine signaling 3 + interleukin 6 receptor subunit β - mouse<br />
**[[4gl9]] – mJAK2 kinase domain + PTyr + inhibitor + suppressor of cytokine signaling 3 + interleukin 6 receptor subunit β - mouse<br />
-
*JAK2 JH1 domain
+
*JAK2 JH1 domain residues 833-1132
-
**[[4gfm]], [[4gmy]], [[4iva]], [[4ivb]], [[4ivc]], [[4ivd]], [[4ji9]], [[4jia]], [[5usy]], [[5usz]], [[5ut0]], [[5ut1]], [[5ut2]], [[5ut3]], [[5ut4]], [[5ut5]], [[5ut6]] - hJAK2 JH1 domain + PTyr + inhibitor <br />
+
**[[4gfm]], [[4gmy]], [[4iva]], [[4ivb]], [[4ivc]], [[4ivd]], [[4ji9]], [[4jia]], [[5usy]], [[5usz]], [[5ut0]], [[5ut1]], [[5ut2]], [[5ut3]], [[5ut4]], [[5ut5]], [[5ut6]], [[6drw]], [[5wev]] - hJAK2 JH1 domain + PTyr + inhibitor <br />
**[[5hez]] - hJAK2 JH1 domain (mutant) + PTyr + inhibitor <br />
**[[5hez]] - hJAK2 JH1 domain (mutant) + PTyr + inhibitor <br />
 +
**[[6bbv]] - hJAK2 JH1 domain + inhibitor <br />
*JAK2 pseudokinase domain
*JAK2 pseudokinase domain
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**[[4z32]] – hJAK2 <br />
**[[4z32]] – hJAK2 <br />
-
*JAK3 kinase domain
+
*JAK3 kinase domain residues 810-1100
**[[1yvj]] – hJAK3 kinase domain (mutant) + PTyr + staurosporine analog<br />
**[[1yvj]] – hJAK3 kinase domain (mutant) + PTyr + staurosporine analog<br />
-
**[[3lxk]], [[3lxl]] – hJAK3 kinase domain (mutant) + PTyr + inhibitor <br />
+
**[[3lxk]], [[3lxl]], [[5wfj]] – hJAK3 kinase domain (mutant) + PTyr + inhibitor <br />
-
**[[3pjc]], [[4v0g]], [[4z16]], [[5lwm]], [[5lwn]], [[5toz]] – hJAK3 kinase domain + inhibitor <br />
+
**[[3pjc]], [[4v0g]], [[4z16]], [[5lwm]], [[5lwn]], [[5toz]], [[6glb]], [[6gl9]], [[6gla]] – hJAK3 kinase domain + inhibitor <br />
 +
**[[5w86]] – hJAK3 kinase domain + PTyr + inhibitor <br />
**[[4hvd]], [[4hvg]], [[4hvh]], [[4hvi]], [[3zc6]], [[3zep]], [[4i6q]], [[4qps]], [[4rio]], [[4qt1]], [[5tts]], [[5ttu]], [[5ttv]], [[5vo6]] – hJAK3 kinase domain (mutant) + inhibitor <br />
**[[4hvd]], [[4hvg]], [[4hvh]], [[4hvi]], [[3zc6]], [[3zep]], [[4i6q]], [[4qps]], [[4rio]], [[4qt1]], [[5tts]], [[5ttu]], [[5ttv]], [[5vo6]] – hJAK3 kinase domain (mutant) + inhibitor <br />

Revision as of 07:32, 24 July 2018

JAK2 kinase domain complex with inhibitor thienopyridine 3tjc

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3D Structures of Janus kinase

Updated on 24-July-2018

References

  1. Liu KD, Gaffen SL, Goldsmith MA, Greene WC. Janus kinases in interleukin-2-mediated signaling: JAK1 and JAK3 are differentially regulated by tyrosine phosphorylation. Curr Biol. 1997 Nov 1;7(11):817-26. PMID:9382798
  2. O'Shea JJ, Kontzias A, Yamaoka K, Tanaka Y, Laurence A. Janus kinase inhibitors in autoimmune diseases. Ann Rheum Dis. 2013 Apr;72 Suppl 2:ii111-5. doi: 10.1136/annrheumdis-2012-202576. PMID:23532440 doi:http://dx.doi.org/10.1136/annrheumdis-2012-202576
  3. Levine RL. Janus kinase mutations. Semin Oncol. 2009 Apr;36(2 Suppl 1):S6-11. doi: 10.1053/j.seminoncol.2009.02.005. PMID:19393837 doi:http://dx.doi.org/10.1053/j.seminoncol.2009.02.005
  4. Schenkel LB, Huang X, Cheng A, Deak HL, Doherty E, Emkey R, Gu Y, Gunaydin H, Kim JL, Lee J, Loberg R, Olivieri P, Pistillo J, Tang J, Wan Q, Wang HL, Wang SW, Wells MC, Wu B, Yu V, Liu L, Geuns-Meyer S. Discovery of Potent and Highly Selective Thienopyridine Janus Kinase 2 Inhibitors. J Med Chem. 2011 Nov 16. PMID:22087750 doi:10.1021/jm200911r

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Michal Harel, Alexander Berchansky, Joel L. Sussman, Jaime Prilusky

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