Janus kinase
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
Jak2 containing <scene name='54/543313/Cv/5'>phosphotyrosine</scene> binds the <scene name='54/543313/Cv/6'>thienopyridine potent inhibitor</scene> in the ATP-binding pocket<ref>PMID:22087750</ref>. Water molecules shown as red spheres. | Jak2 containing <scene name='54/543313/Cv/5'>phosphotyrosine</scene> binds the <scene name='54/543313/Cv/6'>thienopyridine potent inhibitor</scene> in the ATP-binding pocket<ref>PMID:22087750</ref>. Water molecules shown as red spheres. | ||
| + | |||
| + | == 3D Structures of Janus kinase == | ||
| + | [[Janus kinase 3D structures]] | ||
| + | |||
</StructureSection> | </StructureSection> | ||
== 3D Structures of Janus kinase == | == 3D Structures of Janus kinase == | ||
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*JAK1 kinase or JH1 domain residues 869-1153 | *JAK1 kinase or JH1 domain residues 869-1153 | ||
| - | **[[4e4l]], [[4e4n]], [[4e5w]], [[4ehz]], [[4ei4]], [[4fk6]], [[4i5c]], [[4k6z]], [[3eyg]], [[3eyh]], [[5e1e]], [[5hx8]], [[5khx]] | + | **[[4e4l]], [[4e4n]], [[4e5w]], [[4ehz]], [[4ei4]], [[4fk6]], [[4i5c]], [[4k6z]], [[3eyg]], [[3eyh]], [[5e1e]], [[5hx8]], [[5khx]], [[6n77]], [[6n78]], [[6n79]], [[6n7a]], [[6n7b]], [[6n7c]], [[6n7d]], [[6elr]], [[6dbn]], [[4k77]], [[6bbu]], [[5wo4]] - 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 /> | **[[6c7y]]]] – hJAK1 kinase domain + PTyr + SOCY1 + ADP<br /> | ||
| - | **[[ | + | **[[6aah]] – hJAK1 kinase domain + PTyr + drug <br /> |
| - | *JAK1 pseudokinase domain | + | *JAK1 pseudokinase domain residues 561-860 |
**[[4l00]] – hJAK1 pseudokinase domain <br /> | **[[4l00]] – hJAK1 pseudokinase domain <br /> | ||
**[[4l01]] – hJAK1 pseudokinase domain (mutant)<br /> | **[[4l01]] – hJAK1 pseudokinase domain (mutant)<br /> | ||
| - | *JAK1 FERM-SH2 domain | + | *JAK1 FERM-SH2 domain residues 36-514 |
**[[5ixd]], [[5l04]] – hJAK1 + IFN l receptor <br /> | **[[5ixd]], [[5l04]] – hJAK1 + IFN l receptor <br /> | ||
**[[5ixi]] – hJAK1 + IFN l receptor/IL10 <br /> | **[[5ixi]] – hJAK1 + IFN l receptor/IL10 <br /> | ||
| + | **[[6e2p]] – hJAK1 + leptin receptor <br /> | ||
| + | **[[6e2q]] – hJAK1 + erythropoietin receptor <br /> | ||
*JAK2 kinase domain residues 536-812 | *JAK2 kinase domain residues 536-812 | ||
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**[[3ugc]], [[4bbe]], [[4bbf]], [[3zmm]], [[2xa4]], [[4c61]], [[4c62]], [[5l3a]], [[5tq3]], [[5tq4]], [[5tq5]], [[5tq6]], [[5tq7]], [[5tq8]] – hJAK2 kinase domain (mutant) + inhibitor <br /> | **[[3ugc]], [[4bbe]], [[4bbf]], [[3zmm]], [[2xa4]], [[4c61]], [[4c62]], [[5l3a]], [[5tq3]], [[5tq4]], [[5tq5]], [[5tq6]], [[5tq7]], [[5tq8]] – hJAK2 kinase domain (mutant) + inhibitor <br /> | ||
**[[3e62]], [[3e63]], [[3e64]], [[2w1i]], [[4ytc]], [[4ytf]], [[4yth]], [[4yti]], [[4zim]], [[5aep]], [[5cf4]], [[5cf5]], [[5cf6]], [[3io7]], [[3iok]], [[3kck]], [[3jy9]], [[3lpb]], [[3krr]], [[3q32]], [[3tjc]], [[3tjd]], [[3rvg]], [[4aqc]], [[4e4m]], [[4f09]], [[4hge]], [[4d0w]], [[4d0x]], [[4d1s]], [[4p7e]], [[4aep]], [[5cf8]] – hJAK2 kinase domain + PTyr + inhibitor <br /> | **[[3e62]], [[3e63]], [[3e64]], [[2w1i]], [[4ytc]], [[4ytf]], [[4yth]], [[4yti]], [[4zim]], [[5aep]], [[5cf4]], [[5cf5]], [[5cf6]], [[3io7]], [[3iok]], [[3kck]], [[3jy9]], [[3lpb]], [[3krr]], [[3q32]], [[3tjc]], [[3tjd]], [[3rvg]], [[4aqc]], [[4e4m]], [[4f09]], [[4hge]], [[4d0w]], [[4d0x]], [[4d1s]], [[4p7e]], [[4aep]], [[5cf8]] – hJAK2 kinase domain + PTyr + inhibitor <br /> | ||
| + | **[[6aaj]] – hJAK2 kinase domain (mutant) + PTyr + drug <br /> | ||
**[[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 /> | ||
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**[[6bbv]] - hJAK2 JH1 domain + inhibitor <br /> | **[[6bbv]] - hJAK2 JH1 domain + inhibitor <br /> | ||
| - | *JAK2 pseudokinase domain | + | *JAK2 JH2 or pseudokinase domain residues 536-812 |
| - | **[[3ugc]] – hJAK2 | + | **[[6brw]], [[6d2i]], [[6bs0]], [[6bss]], [[5wij]], [[5wik]], [[5wil]], [[5wim]] - hJAK2 JH2 domain (mutant) + inhibitor <br /> |
| - | **[[4fvq]], [[4fvr]], [[5i4n]] – hJAK2 | + | **[[3ugc]] – hJAK2 JH2 domain (mutant) <br /> |
| + | **[[4fvq]], [[4fvr]], [[5i4n]] – hJAK2 JH2 domain (mutant) + ATP<br /> | ||
| - | *JAK2 FERM-SH2 domain | + | *JAK2 FERM-SH2 domain residues 31-516 |
**[[4z32]] – hJAK2 <br /> | **[[4z32]] – hJAK2 <br /> | ||
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**[[1yvj]] – hJAK3 kinase domain (mutant) + PTyr + staurosporine analog<br /> | **[[1yvj]] – hJAK3 kinase domain (mutant) + PTyr + staurosporine analog<br /> | ||
**[[3lxk]], [[3lxl]], [[5wfj]] – hJAK3 kinase domain (mutant) + PTyr + inhibitor <br /> | **[[3lxk]], [[3lxl]], [[5wfj]] – hJAK3 kinase domain (mutant) + PTyr + inhibitor <br /> | ||
| - | **[[3pjc]], [[4v0g]], [[4z16]], [[5lwm]], [[5lwn]], [[5toz]], [[6glb]], [[6gl9]], [[6gla]] | + | **[[3pjc]], [[4v0g]], [[4z16]], [[5lwm]], [[5lwn]], [[5toz]], [[6glb]], [[6gl9]], [[6gla]], [[6ny4]], [[6dud]], [[6da4]] – hJAK3 kinase domain + 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 /> | ||
| + | **[[5w86]] – hJAK3 kinase domain + PTyr + inhibitor <br /> | ||
| + | **[[6aak]] – hJAK3 kinase domain (mutant) + PTyr + drug <br /> | ||
*TYK2 see [[Tyrosine kinase]] | *TYK2 see [[Tyrosine kinase]] | ||
Revision as of 07:36, 8 September 2019
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3D Structures of Janus kinase
Updated on 08-September-2019
References
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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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