Serine/threonine protein kinase

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**[[6cj5]], [[6cje]], [[6cjh]], [[6cjw]], [[6cjy]], [[6ck3]], [[6ck6]], [[6cki]] – hChk 2 catalytic domain (mutant) + inhibitor<br />
**[[6cj5]], [[6cje]], [[6cjh]], [[6cjw]], [[6cjy]], [[6ck3]], [[6ck6]], [[6cki]] – hChk 2 catalytic domain (mutant) + inhibitor<br />
-
*'''hChk Pak'''
+
*'''hChk Pak''' or '''Chk N''' or '''PRK1''';Domains - CRIB 74-109;
 +
**[[1urf]] – hChk Pak-1 Hr1b domain - NMR<br />
 +
**[[4nkg]] – hChk Pak-1 Hr1b domain + SSPH1 LRR domain<br />
 +
**[[2rmk]] – hChk Pak-1 Hr1bb domain + Rac1 - NMR<br />
**[[1f3m]] – hChk Pak-1 autoregulatory+kinase domains<br />
**[[1f3m]] – hChk Pak-1 autoregulatory+kinase domains<br />
**[[4otd]] - hChk Pak-1 kinase domain<br />
**[[4otd]] - hChk Pak-1 kinase domain<br />
**[[1yhv]], [[1yhw]], [[3q4z]], [[3q52]], [[3q53]] – hChk Pak-1 kinase domain (mutant)<br />
**[[1yhv]], [[1yhw]], [[3q4z]], [[3q52]], [[3q53]] – hChk Pak-1 kinase domain (mutant)<br />
**[[4o0r]], [[4o0t]], [[4zji]], [[4zjj]], [[4zlo]], [[4zy4]], [[4zy5]], [[4zy7]], [[5ime]], [[5kbq]], [[5kbr]], [[6b16]] – hChk Pak-1 kinase domain + inhibitor<br />
**[[4o0r]], [[4o0t]], [[4zji]], [[4zjj]], [[4zlo]], [[4zy4]], [[4zy5]], [[4zy7]], [[5ime]], [[5kbq]], [[5kbr]], [[6b16]] – hChk Pak-1 kinase domain + inhibitor<br />
-
**[[4oti]], [[4oth]], [[4otg]] – hChk Pak-1 catalytic domain + inhibitor<br />
+
**[[4oti]], [[4oth]], [[4otg]] – hChk Pak-1 kinase domain + inhibitor<br />
**[[4eqc]], [[4p90]], [[5dew]], [[5dey]], [[5dfp]] – hChk Pak-1 kinase domain (mutant) + inhibitor<br />
**[[4eqc]], [[4p90]], [[5dew]], [[5dey]], [[5dfp]] – hChk Pak-1 kinase domain (mutant) + inhibitor<br />
**[[2hy8]] – hChk Pak-1 kinase domain + staurosporin<br />
**[[2hy8]] – hChk Pak-1 kinase domain + staurosporin<br />
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**[[5eoa]], [[5eof]] – hChk Tbk1 residues 677-729 + optineurin <br />
**[[5eoa]], [[5eof]] – hChk Tbk1 residues 677-729 + optineurin <br />
**[[4jl9]], [[4jlc]] – mChk Tbk1 + inhibitor <br />
**[[4jl9]], [[4jlc]] – mChk Tbk1 + inhibitor <br />
- 
-
*'''Mechanistic target of rapamycin'''
 
- 
-
**[[2rse]] – hChk Mtor + FKBP1A - NMR <br />
 
-
**[[4drh]], [[4dri]], [[4drj]], [[5gpg]] – hChk Mtor FRB domain + FKBP + rapamycin <br />
 
-
**[[5wbh]] – hChk Mtor FRB domain + S6K1 peptide <br />
 
-
**[[4jsn]], [[4jsp]], [[4jsv]], [[4jsx]], [[4jt5]], [[4jt6]] – hChk Mtor residues 1376-2549 + target of rapamycin complex<br />
 
-
**[[5wby]], [[5wbu]] – hChk Mtor residues 1376-2549 + target of rapamycin complex + proline-rich Akt1 substrate<br />
 
-
**[[5flc]] – hChk Mtor complex 1 – Cryo EM <br />
 
-
**[[5h64]] – hChk Mtor complex 1 + LST8 – Cryo EM <br />
 
-
**[[5zcs]] – hChk Mtor complex 2 – Cryo EM <br />
 
*'''Haspin'''
*'''Haspin'''
Line 405: Line 397:
**[[3dle]] – hChk Haspin kinase domain + AMP<br />
**[[3dle]] – hChk Haspin kinase domain + AMP<br />
**[[3e7v]], [[3f2n]], [[3fmd]], [[3iq7]], [[4qtc]], [[5htb]], [[5htc]] – hChk Haspin kinase domain + inhibitor<br />
**[[3e7v]], [[3f2n]], [[3fmd]], [[3iq7]], [[4qtc]], [[5htb]], [[5htc]] – hChk Haspin kinase domain + inhibitor<br />
 +
**[[6g38]], [[6g34]], [[6g35]], [[6g36]], [[6g37]] – hChk Haspin kinase domain + tubercidin derivative<br />
 +
**[[6g39]], [[6g3a]] – hChk Haspin kinase domain (mutant) + tubercidin derivative<br />
**[[4ouc]] – hChk Haspin kinase domain + histone H3 peptide<br />
**[[4ouc]] – hChk Haspin kinase domain + histone H3 peptide<br />
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**[[2hak]] – hChk MARK1 catalytic+UBA domains <br />
**[[2hak]] – hChk MARK1 catalytic+UBA domains <br />
-
**[[3ose]] - hChk MARK1 kinase domain <br />
+
**[[3ose]] - hChk MARK1 KA1 domain <br />
-
**[[5eak]], [[5kz7]], [[5kz8]] – hChk Mark2 catalytic domain + inhibitor <br />
+
**[[6c9d]] – hChk MARK1 catalytic+UBA+KA1 domains (mutant)<br />
 +
**[[5eak]], [[5kz7]], [[5kz8]] – hChk MARK2 catalytic+UBA domains + inhibitor <br />
**[[1zmu]] – rChk MARK2 catalytic+UBA domains <br />
**[[1zmu]] – rChk MARK2 catalytic+UBA domains <br />
**[[2wzj]], [[2r0i]], [[1zmv]], [[1y8g]], [[1zmw]] – rChk MARK2 catalytic+UBA domains (mutant)<br />
**[[2wzj]], [[2r0i]], [[1zmv]], [[1y8g]], [[1zmw]] – rChk MARK2 catalytic+UBA domains (mutant)<br />
**[[3iec]] – hChk MARK2 catalytic+UBA domains + cytotoxicity-associated immunodominant antigen peptide<br />
**[[3iec]] – hChk MARK2 catalytic+UBA domains + cytotoxicity-associated immunodominant antigen peptide<br />
**[[2qnj]] – hChk MARK3 catalytic+UBA domains <br />
**[[2qnj]] – hChk MARK3 catalytic+UBA domains <br />
-
**[[1ul7]], [[1v5s]] - mChk MARK3 kinase domain – mouse - NMR<br />
+
**[[1ul7]], [[1v5s]] - mChk MARK3 catalytic domain – mouse - NMR<br />
**[[3fe3]] – hChk MARK3 catalytic+UBA domains (mutant)<br />
**[[3fe3]] – hChk MARK3 catalytic+UBA domains (mutant)<br />
**[[5es1]] – hChk MARK4 catalytic+UBA domains + inhibitor<br />
**[[5es1]] – hChk MARK4 catalytic+UBA domains + inhibitor<br />
-
*'''Mitotic checkpoint Chk (Bub)'''
+
*'''Mitotic checkpoint Chk (Bub)'''; Domains: TPR 1-220; kinase 726-1085
-
**[[2lah]] – hChk Bub1 N terminal – NMR<br />
+
**[[2lah]] – hChk Bub1 TPR domain – NMR<br />
-
**[[2wvi]] – hChk Bub1β N terminal <br />
+
**[[2wvi]] – hChk Bub1β TPR domain <br />
-
**[[3si5]] – hChk Bub1 residues 67-220 + CASC5 peptide<br />
+
**[[3si5]] – hChk Bub1 TPR domain + CASC5 peptide<br />
**[[4r8q]], [[4qpm]], [[5dmz]] – hChk Bub1 kinase domain + ADP<br />
**[[4r8q]], [[4qpm]], [[5dmz]] – hChk Bub1 kinase domain + ADP<br />
**[[4a1g]] – hChk Bub1 TPR domain + CASC5 KI motif<br />
**[[4a1g]] – hChk Bub1 TPR domain + CASC5 KI motif<br />
-
**[[4ggd]] - hChk Bub1 + cell division cycle protein<br />
+
**[[5jja]] hChk Bub1 residues 661-734 + PP2A<br />
**[[3esl]] – yChk Bub1 N terminal <br />
**[[3esl]] – yChk Bub1 N terminal <br />
**[[4bl0]] - yChk Bub1 + cell cycle arrest protein Bub3 <br />
**[[4bl0]] - yChk Bub1 + cell cycle arrest protein Bub3 <br />
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**[[2w7r]] – hChk 4 PDZ domain <br />
**[[2w7r]] – hChk 4 PDZ domain <br />
-
*'''mTOR'''
+
*'''mTOR''' or '''Mechanistic target of rapamycin'''
*''mTOR FRB domain residues 2015-2114''
*''mTOR FRB domain residues 2015-2114''
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**[[2gaq]], [[2npu]] – hFRAP FRB domain - NMR<BR />
**[[2gaq]], [[2npu]] – hFRAP FRB domain - NMR<BR />
**[[3fap]], [[2fap]], [[4fap]] – hFRAP FRB domain + FKBP + rapamycin analog<BR />
**[[3fap]], [[2fap]], [[4fap]] – hFRAP FRB domain + FKBP + rapamycin analog<BR />
-
**[[4drh]], [[4dri]], [[4drj]] – hFRAP FRB domain + FKBP + rapamycin<BR />
+
**[[4drh]], [[4dri]], [[4drj]], [[5gpg]] – hFRAP FRB domain + FKBP + rapamycin<BR />
 +
**[[5wbh]] – hFRAP FRB domain + S6K1 peptide <br />
*''mTOR domain residues 1376-2549''
*''mTOR domain residues 1376-2549''
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**[[4jt5]] – hFRAP + TORC subunit LST8 + pp242<BR />
**[[4jt5]] – hFRAP + TORC subunit LST8 + pp242<BR />
**[[4jt6]] – hFRAP + TORC subunit LST8 + PI-103<BR />
**[[4jt6]] – hFRAP + TORC subunit LST8 + PI-103<BR />
 +
**[[5wby]], [[5wbu]] – hFRAP + TORC subunit LST8 + proline-rich Akt1 substrate<br />
 +
 +
*''mTOR complex''
 +
 +
**[[5flc]] – hmTOR complex 1 – Cryo EM <br />
 +
**[[5h64]] – hmTOR complex 1 + LST8 – Cryo EM <br />
 +
**[[5zcs]] – hmTOR complex 2 – Cryo EM <br />
*'''Gcn2'''
*'''Gcn2'''
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**[[4otm]] – yChk Gcn2 C terminal domain <br />
**[[4otm]] – yChk Gcn2 C terminal domain <br />
**[[1zyd]] – yChk Gcn2 + ATP<br />
**[[1zyd]] – yChk Gcn2 + ATP<br />
 +
**[[4otn]] – mChk Gcn2 C terminal domain <br />
*'''PRK1'''
*'''PRK1'''

Revision as of 19:31, 18 September 2018

Crystal Structure of Glycogen Synthase Kinase 3ß bound to Anticancer Ruthenium Complex

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3D structures of serine/threonine protein kinase

Updated on 18-September-2018

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

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