Serine/threonine protein kinase

From Proteopedia

Revision as of 09:55, 6 November 2017

spinqualitylabelsall models Crystal Structure of Glycogen Synthase Kinase 3ß bound to Anticancer Ruthenium Complex Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Function Serine/threonine protein kinase 1 (Chk1) phosphorylates cdc25A, cdc25B and cdc25C. Upon phosphorylation, cdc25 binds adaptor protein and the cell is prevented from entering mitosis[1]. Chk2 (Checkpoint kinase 2) phosphorylates cdc25C at Ser-216. Chk6 called also Aurora A is critical for the formation of mitotic spindles during cellular mitosis. Chk6 is phosphorylated at residues Thr287 and Thr288[2]. Chk13 (Polo-like kinase 1 or Plk1) functions during the M phase of the cell cycle including the regulation of centrosome maturation and spindle assembly. Chk13 binds and phosphorylates proteins which are already phosphorylated on a motif recognized by its POLO-box domain (Pbd) at the C terminal. Human Chk13 contains catalytic domain (residues 13-345) and POLO-box domain (residues 345-603)[3]. Chk11 see STK11. Chk Pak see Student Project 1 for UMass Chemistry 423 Spring 2015[4]. Glycogen synthase kinase 3 (GSK-3) is a serine/threonine protein kinase. GSK-3 is active in a number of intracellular signaling pathways. GSK-3 regulates glycogen synthase as well as other proteins. GSK-3 inhibition is studied as a therapeutic target in diseases like Alzheimer, diabetes, bipolar disorder and some cancers[5]. B-Raf is related to retroviral oncogenes and participates in cellular signal transduction. B-Raf domains include the kinase domain - residues 444-721 and Ras-binding domain - residues 153-237. Mutated B-Raf was found in some human cancers[6]. See more in B-RAF with PLX4032. c-Raf is part of the MAPK pathway. c-Raf domains include the kinase domain - residues 323-618, cysteine-rich domain – residues 136-187 and Ras-binding domain - residues 51-132. Mutations of c-Raf are possible causes of Noonan syndrome[7]. For details on c-Raf see Molecular Playground/C-Raf. mTOR (mammalian target of rapamycin) integrates the input from insulin, growth factors and amino acids. Rapamyacin inhibits mTOR by association with FKBP12[8]. Gcn2 (Generl Control Nonderepressible 2) senses amino acid deficiency by binding to uncharged tRNA[9]. PRK1 or serine/threonine protein kinase N1 belongs th protein kinase C family. PRK1 may mediate the Rho-independent signaling pathway. For more details see Student Project 1 for UMass Chemistry 423 Spring 2015. For details on Snf1-related kinase see ABA-regulated SNRK2 Protein Kinase ABA Signaling Pathway. Structure of Anticancer Ruthenium Half-Sandwich Complex Bound to Glycogen Synthase Kinase 3ß [10]         A crystal structure of an bound to the protein kinase glycogen synthase kinase 3ß (GSK-3ß) has been determined and reveals that the inhibitor binds to the via an induced fit mechanism utlizing several and . Importantly, the metal is not involved in any direct interaction with the protein kinase but fulfills a purely structural role. The unique, bulky molecular structure of the half-sandwich complex with the CO-ligand oriented perpendicular to the pyridocarbazole heterocycle allows the complex to stretch the whole distance and to interact tightly with . Although this complex is a conventional ATP-competitive binder, the unique shape of the complex allows novel interactions with the glycine-rich loop which are crucial for binding potency and selectivity. It can be hypothesized that coordination spheres which present other ligands towards the glycine-rich loop might display completely different protein kinase selectivities.

3D structures of serine/threonine protein kinase

Updated on 06-November-2017 {{#tree:id=OrganizedByTopic|openlevels=0|

• Chk1

• • 1ia8 – hChk1 – human
    
  • 1zlt – hChk1 + hymenaldisine
    
  • 1nvq, 1nvr – hChk1 kinase domain+ peptide + saurosporine

• • 1nvs, 1zys - hChk1 kinase domain + peptide + inhibitor

• • 2cgu, 2cgv, 2cgw, 2cgx, 2c3j, 2c3k, 2c3l, 2br1, 2brb, 2brg, 2brh, 2brm, 2brn, 2bro, 2ayp, 2gdo, 2ghg, 2hog, 2ywp, 2hxl, 2hxq, 2hy0, 2r0u, 2e9n, 2e9o, 2e9p, 2e9u, 2e9v, 2qhm, 2qhn, 3f9n, 2wmq, 2wmr, 2wms, 2wmt, 2wmu, 2wmv, 2wmx, 3jvr, 3jvs, 2xey, 2xf0, 2xez, 2x8d, 2x8e, 2x8i, 3ot3, 3ot8, 3pa3, 3pa4, 3pa5, 3nlb, 2wmw, 2ydi, 2ydj, 2ydk, 2yer, 2yex, 2ym3, 2ym4, 2ym5, 2ym6, 2ym7, 2ym8, 3tkh, 3tki, 3u9n, 4fsm, 4fsn, 4fsq, 4fsr, 4fst, 4fsu, 4fsw, 4fsy, 4fsz, 4ft0, 4ft3, 4ft5, 4ft7, 4ft9, 4fta, 4ftc, 4fti, 4ftj, 4ftk, 4ftl, 4ftm, 4ftn, 4fto, 4ftq, 4ftr, 4ftt, 4ftu, 4gh2, 4hyh, 4hyi, 4jik, 4rvm, 4rvl, 4rvk, 4qyh, 4qyg, 4qyf, 4qye, 5dls, 5f4n - hChk1 kinase domain + inhibitor
    
  • 5oot, 5op2, 5op4, 5op5, 5op7, 5opb, 5opr, 5ops, 5opu, 5opv, 5oq5, 5oq6, 5oq7, 5oq8 - hChk1 kinase domain (mutant) + inhibitor
    
  • 5oop - hChk1 kinase domain (mutant) + AMPPNP
    
  • 5oor - hChk1 kinase domain (mutant) + staurosporine
    
  • 2jqi – yChk1 – yeast
    

• Chk2 (Checkpoint kinase)

• • 1gxc – hChk2 phosphothreonine-binding domain + phosphopeptide

• • 2cn5 – hChk2 kinase domain + ADP

• • 2cn8 – hChk2 kinase domain + inhibitor

• • 2w0j, 2w7x, 2wtc, 2wtd, 2xbj, 2xm8, 2xm9, 2yiq, 2yir, 2yit, 2cn8, 2ycf, 2ycq, 2ycr, 2ycs, 2wti, 2wtj, 2xk9, 4a9r, 4a9s, 4a9t, 4bda, 4bdb, 4bdc, 4bdd, 4bde, 4bdf, 4bdg, 4bdh, 4bdi, 4bdj, 4bdk, 2uv2 - hChk2 kinase domain + inhibitor

• • 3i6u, 3i6w – hChk2 residues 84-502 (mutant)

• Chk3 (Mst2)

• • 4hkd, 4l0n, 4oh9 – hChk3 SARAH domain
    
  • 4lg4 – hChk3 kinase domain
    
  • 4lgd – hChk3 kinase domain + RASSF5 SARAH domain
    
  • 5dh3 – hChk3 kinase domain + inhibitor
    

• Chk4 (Mst1)

• • 2jo8 – hChk4 C terminal domain - NMR
    
  • 3com – hChk4 kinase domain
    
  • 4nr2 – hChk4 SARAH domain
    
  • 4oh8 – hChk4 SARAH domain + Ras association domain-containing protein
    

• Chk5 (Aurora kinase b)

• • 4af3 – hChk5 + inhibitor
    

• Chk6 (Aurora A)

• • 1muo, 1mq4 – hChk6 kinase domain
    
  • 1ol6 – hChk6 kinase domain (mutant) + ATP
    
  • 2wqe – hChk6 kinase domain (mutant) + ADP
    
  • 2c6d – hChk6 kinase domain (mutant) + ADPNP
    
  • 2dwb – hChk6 kinase domain + AMPPNP
    
  • 3daj, 3d14, 3dj5, 3dj6, 3dj7, 3d15, 3d2i, 3d2k – Chk6 kinase domain (mutant) + inhibitor - mouse
    
  • 2j4z, 2j50, 2np8, 3efw, 2x81, 2x6d, 2x6e, 3myg, 3vap, 4b0g – hChk6 kinase domain + inhibitor
    
  • 2bmc, 2c6e, 3coh, 3h0y, 3h0z, 3h10, 3fdn, 2wtw, 3lau, 3nrm, 2xne, 2xng, 2xru, 3k5u, 3m11, 3p9j, 3r21, 3r22, 3qbn, 3unz, 3uo4, 3uo5, 3uo6, 3uod, 3uoh, 3uoj, 3uok, 3uol, 3up2, 3up7, 4dhf, 4dea, 4deb, 4ded, 4dee – hChk6 kinase domain (mutant) + inhibitor
    

• Chk6 with phosphorylated Thr 287, Thr288

• • 1ol5, 1ol7 – hChk6 kinase domain + PThr + ADP
    
  • 2w1c, 2w1d, 2w1e, 2w1f, 2w1g – hChk6 kinase domain + PThr + inhibitor
    
  • 2wtv – hChk6 kinase domain (mutant) + PThr + inhibitor
    
  • 3e5a, 3ha6 – hChk6 kinase domain + PThr + inhibitor + targeting protein for XKLP2
    

• Chk10 (lymphocyte-oriented kinase)

• • 2j7t, 4aot, 4equ, 5ajq, 5owq, 5owr – hChk10 kinase domain + inhibitor
    

• Chk11

• • 2wtk – hChk11 (mutant) + calcium-binding protein
    

• Chk12-A (Aurora kinase b-a or Aurora B kinase)

• • 2vgo, 2vgp, 2vrx, 3ztx, 4c2v, 5eyk – fChk12-A + inner centromere protein A peptide + inhibitor - frog
    
  • 4c2w – fChk12-A + inner centromere protein A peptide + AMPPNP
    
  • 4b8l, 4b8m, 5k3y – fChk12-A (mutant) + inner centromere protein A peptide + inhibitor
    

• Chk13 (Polo-like kinase Plk)

• Plk1 Polo-box domain (Pbd)

• • 1q4o, 2ogq, 3hih, 3p2w, 4h5x – Plk1 Pbd
    

• Plk1 Pbd complex with polypeptide

• • 1umw, 2ojx, 3bzi, 3c5l, 3rq7, 4dfw, 4whl, 4whk, 4whh, 4rcp, 4o6w, 4o56, 5dms, 5dmv, 5dnj – Plk1 Pbd + peptide
    
  • 3hik, 3fvh, 3p2z, 3p34, 3p35, 3p36, 3p37, 3q1i, 4e67, 4e9c, 4e9d, 4hab, 4hy2, 4o9w, 4x9r, 4x9v, 4x9w, 5j19 – Plk1 Pbd + phosphopeptide
    
  • 1q4k – Plk1 Pbd (mutant) + phosphopeptide
    
  • 2v5q – Plk1 Pbd + design ankyrin repeat protein
    
  • 4lkl – hChk Plk1 + PL-55
    
  • 4lkm – hChk Plk1 + PL-74
    

• Plk1 Pbd complex with small molecule inhibitor

• • 4h71, 4hco, 5ta6, 5ta8 – Plk1 Pbd + inhibitor
    
  • 2rku – Plk1 Pbd (mutant) + inhibitor
    
  • 3db6, 3db8, 3dbc, 3dbd, 3dbe, 3dbf – zfPlk1 Pbd (mutant) + inhibitor – zebra fish
    

• Plk1 catalytic domain

• • 2owb – Plk1 catalytic domain
    
  • 2ou7 – Plk1 catalytic domain + AMPPNP
    
  • 3d5w – zfPlk1 catalytic domain + ADP
    
  • 3kb7, 2yac, 3thb, 4a4l, 4a4o – Plk1 catalytic domain + inhibitor
    
  • 3fc2 – Plk1catalytic domain (mutant) + inhibitor
    
  • 4j52, 4j53 – hChk Plk1 (mutant) + inhibitor
    
  • 3d5x – zfPlk1 catalytic domain (mutant) + wortmannin
    

• Plk2

• • 4i5m, 4i5p, 4i6f, 4i6h – hChk Plk2 kinase domain (mutant) + inhibitor
    
  • 4xb0, 4rs6 – hChk Plk2 Pbd
    

• Plk3

• • 4b6l, 4i6b – hChk Plk3 kinase domain + inhibitor
    

• Plk4

• • 3cok – hChk Plk4 kinase domain
    
  • 4n9j – hChk Plk4 Pbd domain
    
  • 4n7z, 4n7v – hChk Plk4 Pbd domain + centrosomal protein
    
  • 4jxf, 4yur – hChk Plk4 kinase domain + inhibitor
    
  • 5lhy – hChk Plk4 Pb3 domain
    
  • 4yyp, 5lhz – hChk Plk4 Pb3 domain + Scl-interrupting locus protein
    
  • 4nk7, 4g7n, 5lhx – Chk Plk4 Pbd domain – Drosophila melanogaster
    

• Chk15 (Aurora kinase a)

• • 4o0s – hChk15 kinase domain
    
  • 4bn1, 4o0w, 4o0u – hChk15 kinase domain (mutant)
    
  • 4byi, 4byj, 4jai, 4jaj, 3w10, 3w16, 3w18, 3w2c, 4uzh, 4uzd, 4uyn, 4zs0, 4ztq, 4ztr, 4zts, 5aad, 5aae, 5aag, 5dr6, 5dr9, 5dt0, 5ew9, 5obr, 5one – hChk15 kinase domain + inhibitor
    
  • 4jbo, 4jbp, 4jbq, 4prj, 5dpv – hChk15 kinase domain (mutant) + inhibitor
    
  • 5dn3, 5dos, 5dt4, 5obj – hChk15 kinase domain + ATP + inhibitor
    
  • 5dr2 – hChk15 kinase domain (mutant) + ATP + inhibitor
    
  • 5dnr, 5drd, 5dt3 – hChk15 kinase domain + ATP
    
  • 5g1x – hChk15 kinase domain (mutant) + N-Myc
    
  • 5l8j, 5l8k, 5l8l – hChk15 kinase domain (mutant) + new antigen receptor variable domain
    
  • 5lxm – hChk15 kinase domain (mutant) + Targeting protein for XKLP2
    

• Chk16

• • 2buj – hChk13 (mutant) + staurosporin
    

• Chk17

• • 3lm0 – hChk17B
    
  • 3lm5 – hChk17B + quercetin
    

• Chk24 (Mst3)

• • 3a7f, 3a7g, 3a7h, 3a7i, 3a7j, 3ckw – hChk24 kinase domain
    
  • 4w8e, 4w8d, 4u8z, 4qmm, 4qmn, 4qmo, 4qmp, 4qmq, 4qms, 4qmt, 4qmu, 4qmv, 4qmw, 4qmx, 4qmy, 4qmz, 4qna, 4qo9 – hChk Mst3 + inhibitor
    
  • 3ckx – hChk24 kinase domain + staurosporin
    
  • 3zhp – hChk24 kinase domain + calcium-binding protein
    
  • 4o27 – hChk24 kinase domain (mutant) + calcium-binding protein
    
  • 4qml – hChk Mst3 kinase domain + AMPPNP
    

• Chk26 (Mst4)

• • 3ggf – hChk Mst4 + inhibitor
    
  • 4geh, 3w8i - hChk Mst4 dimerization domain + programmed cell death protein 10
    
  • 4fza, 4fzd, 4fzf – hChk Mst4 (mutant) + calcium-binding protein
    

• Chk25

• • 2xik – hChk25 kinase domain
    
  • 3w8h – hChk25 regulatory domain + programmed cell death protein 10
    
  • 4nzw – hChk25 kinase domain (mutant) + calcium-binding protein
    

• Chk32

• • 4fr4 – hChk32A
    

• Chk40

• • 5l2q – hChk40 kinase homology domain
    

• Rac-α hChk

• • 1h10, 1unq, 2uvm – hRac-α hChk pleckstrin homology domain + inositol tetrakisphosphate
    
  • 1unp, 1unr – hRac-α hChk pleckstrin homology domain
    
  • 2uzr, 2uzs – hRac-α hChk pleckstrin homology domain (mutant)
    
  • 3o96, 4ejn - hRac-α hChk + inhibitor
    
  • 4gv1 - hRac-α hChk kinase domain + inhibitor
    
  • 4ekl, 5kcv - hRac-α hChk (mutant) + inhibitor
    
  • 4ekk - hRac-α hChk (mutant) + glycogen synthase kinase-3 peptide + AMPPNP
    
  • 3ow4, 3qkk, 3qkl - hRac-α hChk kinase domain (mutant) + GSK3 peptide + inhibitor
    
  • 3qkm - hRac-α hChk kinase domain (mutant) + inhibitor
    

• Rac-β hChk

• • 1gzk, 1gzn, 1gzo, 1mrv, 1mry – Rac-β hChk kinase domain
    
  • 1p6s - Rac-β hChk pleckstrin homology domain - NMR
    
  • 1o6k - Rac-β hChk kinase domain + GSK3 peptide + AMPPNP
    
  • 2jdo, 2jdr, 2uw9, 2x39, 3cqu, 3cqw - Rac-β hChk kinase domain + GSK3 peptide + inhibitor
    
  • 3e87, 3e88, 3e8d - Rac-β hChk kinase domain (mutant) + GSK3 peptide + inhibitor<br /
  • 1o6l - Rac-β hChk kinase domain (mutant) + GSK3 peptide + AMPPNP
    
  • 3d0e - Rac-β hChk kinase domain (mutant) + inhibitor
    

• Rac-γ hChk

• • 2x18 – Rac-γ hChk PH domain
    

• A-Raf

• • 1wxm – hA-Raf RAS-binding domain - NMR
    

• B-Raf

• • 1uwh, 3c4c – hB-Raf kinase domain + anticancer drug
    
  • 1uwj – hB-Raf kinase domain (mutant) + anticancer drug
    
  • 2fb8, 3d4q, 3ii5, 3psd, 3skc, 3tv6, 4g9c, 4ksp, 4ksq, 3psb, 3ppj, 3ppk, 3prf, 3pri, 3tv4, 4dbn, 4e4x, 4mbj, 4ehe, 3q4c, 3q96, 3e26, 4h58, 4e26, 4fc0, 4pp7 – hB-Raf kinase domain + pyrazole inhibitor
    
  • 5csw, 5csx, 5ct7, 5fd2, 5hid, 5hie, 5val, 5vam - hB-Raf kinase domain + inhibitor
    
  • 4jvg, 4ehg, 4fk3, 3idp, 4g9r, 4wo5, 4mnf, 4r5y, 4rzv, 4rzw, 4xv1, 4xv2, 4xv3, 4xv9, 4yht, 5c9c, 5hi2, 5ita, 5jrq, 5jsm, 5jt2 – hB-Raf kinase domain (mutant) + pyrazole inhibitor
    
  • 4mne – hB-Raf kinase domain + MAPKK1
    
  • 2l05, 5j17, 5j2r – hB-Raf RAS-binding domain - NMR
    
  • 3ny5 – hB-Raf RAS-binding domain
    
  • 5j18 – hB-Raf RAS-binding domain + inhibitor - NMR
    

• c-Raf

• • 1rfa – hc-Raf RAS-binding domain - NMR
    
  • 1rrb – c-Raf RAS-binding domain – NMR - rat
    
  • 1faq, 1far – hc-Raf cysteine-rich domain - NMR
    
  • 3omv – hc-Raf kinase domain
    

• c-Raf complex with protein

• • 1c1y – hc-Raf RAS-binding domain + RAP1A
    
  • 3kuc – hc-Raf RAS-binding domain (mutant) + RAP1A
    
  • 1gua – hc-Raf RAS-binding domain + RAP1A + GPPNHP
    
  • 4g0n, 4g3x – hc-Raf RAS-binding domain + GTPase Hras
    
  • 3kud – hc-Raf RAS-binding domain (mutant) + GTPase Hras
    

• Snf1-related Chk

• • 3uc4, 3uc3, 3udb, 3zut, 3zuu – AtChk Srk2E kinase domain (mutant) – Arabidopsis thaliana
    
  • 3ujg – AtChk Srk2E kinase domain (mutant) + protein phosphatase 2C
    

• MAPK-interacting Chk

• • 2hw6 – hChk 1 catalytic domain
    
  • 2hw7 – hChk 1 catalytic domain + staurosporin
    
  • 2ac3 – hChk 2
    
  • 2ac5 – hChk 2 (mutant)
    

• hChk Pak

• • 1f3m – hChk Pak-1 autoregulatory+kinase domains
    
  • 4otd - hChk Pak-1 catalytic domain
    
  • 1yhv, 1yhw, 3q4z, 3q52, 3q53 – hChk Pak-1 kinase domain (mutant)
    
  • 4o0r, 4o0t, 4zji, 4zjj, 4zlo, 4zy4, 4zy5, 4zy7, 5ime, 5kbq, 5kbr, 6b16 – hChk Pak-1 kinase domain + inhibitor
    
  • 4oti, 4oth, 4otg – hChk Pak-1 catalytic domain + inhibitor
    
  • 4eqc, 4p90, 5dew, 5dey, 5dfp – hChk Pak-1 kinase domain (mutant) + inhibitor
    
  • 2hy8 – hChk Pak-1 kinase domain + staurosporin
    
  • 2qme – hChk Pak-1 CRIB domain + RAC3
    
  • 3fxz, 3fy0, 4daw – hChk Pak-1 kinase domain (mutant) + Ru complex
    
  • 2j0i, 4fie – hChk Pak-4
    
  • 4fig, 4fij, 4l67 – hChk Pak-4 kinase domain
    
  • 2cdz – hChk Pak-4 + purine derivative
    
  • 2ov2 – hChk Pak-4 CRIB domain + RAC3
    
  • 2qon, 4fif, 4fih, 4fii, 4jdh, 4jdi, 4jdj, 4jdk – hChk Pak-4 kinase domain + peptide
    
  • 4app, 4o0v, 4o0x, 4o0y, 4njd, 4xbu, 5bms, 5i0b, 5vee, 5vef – hChk Pak-4 kinase domain + inhibitor
    
  • 2x4z, 2xh5 – hChk Pak-4 kinase domain (mutant) + inhibitor
    
  • 5ved – hChk Pak-4 kinase domain + staurosporine
    
  • 2c30 – hChk Pak-6
    
  • 2odb – hChk Pak-6 CRIB domain + CDC42
    
  • 4ks8 – hChk Pak-6 kinase domain + sunitinib
    
  • 4ks7 – hChk Pak-6 kinase domain (mutant) + inhibitor
    
  • 2f57 – hChk Pak-7
    

• Mycobacterium tuberculosis Chk Pkn

• • 4x3f - MtChk PknA – Mycobacterium tuberculosis
    
  • 4ow8 - MtChk PknA kinase domain
    
  • 3ori, 3ork, 3orl, 3orm, 3oro, 3orp, 3ort - MtChk PknB kinase domain (mutant)
    
  • 3ouv - MtChk PknB extracellular domain
    
  • 1o6y – MtChk PknB catalytic domain
    
  • 2kud, 2kue, 2kuf, 2kui – MtChk PknB pasta domains - NMR
    
  • 5e0y – MtChk PknB pasta domain 4
    
  • 5e10 – MtChk PknB pasta domains 1-2
    
  • 5e0z – MtChk PknB pasta domains 3-4
    
  • 5e12 – MtChk PknB pasta domains 2-4
    
  • 3f61, 3f69 - MtChk PknB kinase domain (mutant) + inhibitor
    
  • 1rwi, 1rwl - MtChk PknD extracellular domain
    
  • 2h34 – MtChk PknE catalytic domain
    
  • 4y12 - MtChk PknG + ATP-gS
    
  • 4y0x - MtChk PknG + ADP
    
  • 4esq - MtChk PknH extracellular domain
    
  • 5m06 - MtChk PknI kinase domain
    
  • 5m07, 5m08, 5m09 - MtChk PknI kinase domain (mutant)
    

• hChk Nek

• • 4apc – hChk Nek1 kinase domain (mutant)
    
  • 4b9d - hChk Nek1 kinase domain (mutant) + inhibitor
    
  • 2w5h – hChk Nek2 kinase domain
    
  • 2jav, 2wqo, 2xk3, 2xk4, 2xk6, 2xk7, 2xk8, 2xkc, 2xkd, 2xke, 2xkf, 2xnm, 2xnn, 2xno, 2xnp, 4a4x, 4afe, 5m51, 5m53, 5m55, 5m57 – hChk Nek2 + inhibitor
    
  • 2w5a, 2w5b – hChk Nek2 + nucleotide
    
  • 2wqm – hChk Nek7
    
  • 2wqn – hChk Nek7 + ADP
    
  • 5de2 – hChk Nek7 + hChk Nek9
    

• hChk Vrk (vaccinia-related kinase)

• • 2kty, 2kul, 2lav, 2rsv – hChk Vrk1 - NMR
    
  • 3op5 – hChk Vrk1 kinase domain (mutant)
    
  • 5ukf – hChk Vrk1 kinase domain + inhibitor
    
  • 5uvf – hChk Vrk1 kinase domain (mutant) + inhibitor
    
  • 2v62 – hChk Vrk2 kinase domain
    
  • 5uu1 – hChk Vrk2 kinase domain + inhibitor
    

• Chk Wnk (protein kinase lysine-deficient)

• • 2lru – rChk Wnk1 autoinhibitory domain - NMR
    
  • 3fpq, 4q2a, 4pwn - hChk Wnk1 kinase domain (mutant)
    
  • 5wdy, 5we8 - hChk Wnk1 kinase domain + inhibitor
    
  • 5drb - rChk Wnk1 kinase domain (mutant) + inhibitor
    
  • 5o1v, 5o21, 5o23 - hChk Wnk3 kinase domain
    
  • 5o2c - hChk Wnk3 kinase + CCT1 domains
    
  • 5o26, 5tf9 - hChk Wnk3 kinase domain + AMPPNP
    
  • 5o2b - hChk Wnk3 kinase domain + inhibitor
    

• TANK-binding kinase

• • 4efo – hChk Tbk1 ubiquitin-like domain
    
  • 4im0, 4im2, 4im3, 4iw0, 4iwo, 4iwp, 4ipq – hChk Tbk1 (mutant) + inhibitor
    
  • 4eut, 4euu – hChk Tbk1 kinase+ubiquitin-like domains (mutant) + inhibitor
    
  • 4jl9, 4jlc – mChk Tbk1 + inhibitor
    

• Mechanistic target of rapamycin

• • 2rse – hChk Mtor + FKBP1A - NMR
    
  • 4drh, 4dri, 4drj, 5gpg – hChk Mtor FRB domain + FKBP + rapamycin
    
  • 4jsn, 4jsp, 4jsv, 4jsx, 4jt5, 4jt6 – hChk Mtor + target of rapamycin complex
    
  • 5flc – hChk Mtor complex 1 – Cryo EM
    
  • 5h64 – hChk Mtor complex 1 + LST8 – Cryo EM
    

• Haspin

• • 2vuw, 2wb8 – hChk Haspin kinase domain
    
  • 3dle – hChk Haspin kinase domain + AMP
    
  • 3e7v, 3f2n, 3fmd, 3iq7, 4qtc, 5htb, 5htc – hChk Haspin kinase domain + inhibitor
    
  • 4ouc – hChk Haspin kinase domain + histone H3 peptide
    

• MAP/microtubule affinity-regulating kinase (Mark)

• • 2r0i – rChk Mark1 catalytic+UBA domains (mutant)
    
  • 2wzj – rChk Mark2 catalytic+UBA domains (mutant)
    
  • 2hak – hChk Mark1 catalytic+UBA domains
    
  • 3ose - hChk Mark1 kinase domain
    
  • 3iec – hChk Mark1 catalytic+UBA domains + cytotoxicity-associated immunodominant antigen
    
  • 5eak, 5kz7, 5kz8 – hChk Mark2 catalytic domain + inhibitor
    

• Mitotic checkpoint Chk (Bub)

• • 2lah – hChk Bub1 N terminal – NMR
    
  • 2wvi – hChk Bub1β N terminal
    
  • 3si5 – hChk Bub1 residues 67-220 + CASC5 peptide
    
  • 4r8q, 4qpm, 5dmz – hChk Bub1 kinase domain + ADP
    
  • 4a1g – hChk Bub1 TPR domain + CASC5 KI motif
    
  • 4ggd - hChk Bub1 + cell division cycle protein
    
  • 3esl – yChk Bub1 N terminal
    
  • 4bl0 - yChk Bub1 + cell cycle arrest protein Bub3
    

• Microtubule-associated Chk

• • 2m9x – hChk 1 residues 187-287 – NMR
    
  • 3ps4 - hChk 1 residues 965-1057
    
  • 2kqf, 2kyl – hChk 2 PDZ domain + glycoprotein C terminal – NMR
    
  • 3khf - hChk 3 PDZ domain
    
  • 2w7r – hChk 4 PDZ domain
    

• mTOR

• mTOR FRB domain residues 2015-2114

• • 1nsg, 1fap – hFRAP FRB domain + FKBP
    
  • 2rse – hFRAP FRB domain + FKBP – NMR
    
  • 1aue – hFRAP FRB domain
    
  • 2gaq, 2npu – hFRAP FRB domain - NMR
    
  • 3fap, 2fap, 4fap – hFRAP FRB domain + FKBP + rapamycin analog
    
  • 4drh, 4dri, 4drj – hFRAP FRB domain + FKBP + rapamycin
    

• mTOR domain residues 1376-2549

• • 4jsn – hFRAP + TORC subunit LST8
    
  • 4jsp – hFRAP + TORC subunit LST8 + ATP
    
  • 4jsv – hFRAP + TORC subunit LST8 + ADP
    
  • 4jsx – hFRAP + TORC subunit LST8 + torin2
    
  • 4jt5 – hFRAP + TORC subunit LST8 + pp242
    
  • 4jt6 – hFRAP + TORC subunit LST8 + PI-103
    

• Gcn2

• • 1zyc – yChk Gcn2
    
  • 1zxe, 1zy4, 1zy5 – yChk Gcn2 (mutant)
    
  • 2yz0 – yChk Gcn2 RWD/GI domain – NMR
    
  • 4otm – yChk Gcn2 C terminal domain
    
  • 1zyd – yChk Gcn2 + ATP
    

• PRK1

• • 4otd – hPRK1 catalytic domain
    
  • 1urf – hPRK1 Hrb1 domain - NMR
    
  • 4otg, 4oth, 4oti – hPRK1 catalytic domain + clinical inhibitor
    
  • 4nkg – hPRK1 Hrb1 domain + SSPH1 LRR domain
    
  • 2rmk – hPRK1 Hrb1 domain + Rac1 - NMR
    
  • 1cxz – hPRK1 effector domain + RhoA
    

• Pim-2

• • 4x7q – hPim2 + inhibitor
    

• Other Chk

• • 1u5q, 1u5r – rChk Tao2 kinase domain
    
  • 2cos – Chk Lats2 – mouse – NMR
    
  • 1wak – hChk Sprk1
    
  • 3dak – hChk Osr1 kinase domain
    
  • 3fpq, 4q2a, 4pwn - hChk Wnk1 kinase domain (mutant)
    
  • 4aw2 – hChk Mrckα kinase domain
    
  • 4pxw – hChk Vprbp WD repeat domain (mutant)
    
  • 1how, 1zxe, 1zy4 – yChk (mutant)
    
  • 1q8z, 1zyc – yChk
    
  • 1ow5, 1x9x – yChk Ste11 SAM domain – NMR
    
  • 2kio, 2kit – yChk Tor1 FATC domain – NMR
    
  • 3gre – yChk Vps15 WD repeat domain
    
  • 3osm, 3ost - yChk Kcc4 kinase domain
    
  • 1uf0 – hChk Dcamkl1 DCX domain – NMR
    
  • 1xte, 1xtn – mChk Sgk3 PX domain
    
  • 3tpd, 3tpe – EcChk Hipa – Escherichia coli
    
  • 3tpb – EcChk Hipa (mutant)
    
  • 4f0g – smChk Roco4 kinase domain – slime mold
    
  • 4yom – mChk Sad
    
  • 4ynz – mChk Sad N terminal domain
    
  • 5iri – mChk Sad residues 592-719
    
  • 5fvm – Chk Tor2 + LST8 – Kluyveromyces maximanus
    
  • 5oat – Chk – red flour beetle
    

• Other Chk complexes

• • 2gcd – rChk Tao2 kinase domain + staurosporine
    
  • 3hgk – Chk Pto + effector protein AVRPTOB – Currant tomato
    
  • 1wbp – hChk Sprk1 + peptide
    
  • 3beg – hChk Srpk1 + splicing factor SF2
    
  • 3hdm, 3hdn – hChk Sgk1 (mutant) + inhibitor
    
  • 2r5t – hChk Sgk3 + AMPPNP
    
  • 4yff, 4yfi – hChk Tnni3k + inhibitor
    
  • 4otp – hChk Rio1 Rio domain + ADP
    
  • 2v3s – hChk Osr1 + hChk Wnk4 peptide
    
  • 2vwi – hChk Osr1 kinase domain + ANP
    
  • 5jzj – hChk Dclk1 kinase domain + AMPPN
    
  • 5jzn – hChk Dclk1 kinase domain + inhibitor
    
  • 4crs – hChk N2 kinase domain + ATPγS
    
  • 3tku, 4ual – hChk Mrckβ + inhibitor
    
  • 4uak – hChk Mrckβ + ADP
    
  • 5aja – hChk Vprbp WD repeat domain + VPX + SAMHD1
    
  • 4wzx – hChk Ulk3 MIT 2 domain + inhibitor
    
  • 5ci7 – hChk Ulk1 (mutant) + inhibitor
    
  • 4wnp, 4wno – hChk Ulk1 + IST1 homolog
    
  • [[5b5w, 5b6b, 5brk – hChk Lats1 residues 622-704 + MOB1
    
  • 1q8y, 1q97, 1q99, 1zyd – yChk + nucleotide
    
  • 1zy5 – yChk (mutant) + nucleotide
    
  • 2jd5 – yChk + NPL-3P
    
  • 4lqs, 4lqq, 4lqp – yChk Cbk1 residues 251-756 + Cbk1 activator Mob2
    
  • 6kc2 – yChk Vps15 + Vps34
    
  • 3p86, 3ppz - AtChk Ctr1 + staurosporine
    
  • 3tpt – EcChk Hipa (mutant) + ADP
    
  • 3tpv – EcChk Hipa + ADP
    
  • 4yg7, 5k98 – EcChk Hipa + antitoxin Hipb + DNA
    
  • 4f0f – smChk Roco4 kinase domain + APPCP
    
  • 4f1m, 4f1o – smChk Roco4 kinase domain (mutant) + APPCP
    
  • 4f1t – smChk Roco4 kinase domain + inhibitor
    

• Serine/threonine protein kinase Rad53 see Rad53

}}

References

1. ↑ Bartek J, Lukas J. Chk1 and Chk2 kinases in checkpoint control and cancer. Cancer Cell. 2003 May;3(5):421-9. PMID:12781359
2. ↑ Ducat D, Zheng Y. Aurora kinases in spindle assembly and chromosome segregation. Exp Cell Res. 2004 Nov 15;301(1):60-7. PMID:15501446 doi:http://dx.doi.org/10.1016/j.yexcr.2004.08.016
3. ↑ Takai N, Hamanaka R, Yoshimatsu J, Miyakawa I. Polo-like kinases (Plks) and cancer. Oncogene. 2005 Jan 10;24(2):287-91. PMID:15640844 doi:http://dx.doi.org/10.1038/sj.onc.1208272
4. ↑ Dummler B, Ohshiro K, Kumar R, Field J. Pak protein kinases and their role in cancer. Cancer Metastasis Rev. 2009 Jun;28(1-2):51-63. doi: 10.1007/s10555-008-9168-1. PMID:19165420 doi:http://dx.doi.org/10.1007/s10555-008-9168-1
5. ↑ Forde JE, Dale TC. Glycogen synthase kinase 3: a key regulator of cellular fate. Cell Mol Life Sci. 2007 Aug;64(15):1930-44. PMID:17530463 doi:http://dx.doi.org/10.1007/s00018-007-7045-7
6. ↑ Brose MS, Volpe P, Feldman M, Kumar M, Rishi I, Gerrero R, Einhorn E, Herlyn M, Minna J, Nicholson A, Roth JA, Albelda SM, Davies H, Cox C, Brignell G, Stephens P, Futreal PA, Wooster R, Stratton MR, Weber BL. BRAF and RAS mutations in human lung cancer and melanoma. Cancer Res. 2002 Dec 1;62(23):6997-7000. PMID:12460918
7. ↑ Antony R, Emery CM, Sawyer AM, Garraway LA. C-RAF mutations confer resistance to RAF inhibitors. Cancer Res. 2013 Aug 1;73(15):4840-51. doi: 10.1158/0008-5472.CAN-12-4089. Epub, 2013 Jun 4. PMID:23737487 doi:http://dx.doi.org/10.1158/0008-5472.CAN-12-4089
8. ↑ Laplante M, Sabatini DM. mTOR signaling in growth control and disease. Cell. 2012 Apr 13;149(2):274-93. doi: 10.1016/j.cell.2012.03.017. PMID:22500797 doi:http://dx.doi.org/10.1016/j.cell.2012.03.017
9. ↑ Ravindran R, Loebbermann J, Nakaya HI, Khan N, Ma H, Gama L, Machiah DK, Lawson B, Hakimpour P, Wang YC, Li S, Sharma P, Kaufman RJ, Martinez J, Pulendran B. The amino acid sensor GCN2 controls gut inflammation by inhibiting inflammasome activation. Nature. 2016 Mar 24;531(7595):523-7. doi: 10.1038/nature17186. Epub 2016 Mar 16. PMID:26982722 doi:http://dx.doi.org/10.1038/nature17186
10. ↑ Atilla-Gokcumen GE, Di Costanzo L, Meggers E. Structure of anticancer ruthenium half-sandwich complex bound to glycogen synthase kinase 3beta. J Biol Inorg Chem. 2010 Sep 7. PMID:20821241 doi:10.1007/s00775-010-0699-x