Serine/threonine protein kinase

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(Difference between revisions)

Revision as of 09:44, 10 December 2014

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

Drag the structure with the mouse to rotate

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.
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.
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).

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.

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. 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. For details on c-Raf see Molecular Playground/C-Raf.

For details on Snf1-related kinase see

Structure of Anticancer Ruthenium Half-Sandwich Complex Bound to Glycogen Synthase Kinase 3ß ^[1] 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 10-December-2014

References

↑ 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

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Joel L. Sussman, Alexander Berchansky

Retrieved from "http://52.214.119.220/wiki/index.php/Serine/threonine_protein_kinase"

Category: Topic Page

@@ Line 256: / Line 256: @@
 **[[2f57]] – hChk Pak-7<br />
-===''Mycobacterium tuberculosis'' Chk Pkn===
+*'''Mycobacterium tuberculosis Chk Pkn'''
-[[3ori]], [[3ork]], [[3orl]], [[3orm]], [[3oro]], [[3orp]], [[3ort]] - MtChk  PknB kinase domain (mutant) – ''Mycobacterium tuberculosis''<br />
+**[[3ori]], [[3ork]], [[3orl]], [[3orm]], [[3oro]], [[3orp]], [[3ort]] - MtChk  PknB kinase domain (mutant) – ''Mycobacterium tuberculosis''<br />
-[[3ouv]] - MtChk PknB extracellular domain<br />
+**[[3ouv]] - MtChk PknB extracellular domain<br />
-[[1o6y]] – MtChk PknB catalytic domain<br />
+**[[1o6y]] – MtChk PknB catalytic domain<br />
-[[2kud]], [[2kue]], [[2kuf]], [[2kui]] – MtChk PknB pasta domains - NMR<br />
+**[[2kud]], [[2kue]], [[2kuf]], [[2kui]] – MtChk PknB pasta domains - NMR<br />
-[[3f61]], [[3f69]] - MtChk  PknB kinase domain (mutant) + inhibitor<br />
+**[[3f61]], [[3f69]] - MtChk  PknB kinase domain (mutant) + inhibitor<br />
-[[1rwi]], [[1rwl]] - MtChk PknD extracellular domain<br />
+**[[1rwi]], [[1rwl]] - MtChk PknD extracellular domain<br />
-[[2h34]] – MtChk PknE catalytic domain<br />
+**[[2h34]] – MtChk PknE catalytic domain<br />
-[[4esq]] - MtChk PknH extracellular domain<br />
+**[[4esq]] - MtChk PknH extracellular domain<br />
-===hChk Nek===
+*'''hChk Nek'''
-[[4apc]] – hChk Nek1 kinase domain (mutant)<br />
+**[[4apc]] – hChk Nek1 kinase domain (mutant)<br />
-[[4b9d]] - hChk Nek1 kinase domain (mutant) + inhibitor<br />
+**[[4b9d]] - hChk Nek1 kinase domain (mutant) + inhibitor<br />
-[[2w5h]] – hChk Nek2 kinase domain<br />
+**[[2w5h]] – hChk Nek2 kinase domain<br />
-[[2jav]], [[2wqo]], [[2xk3]], [[2xk4]], [[2xk6]], [[2xk7]], [[2xk8]], [[2xkc]], [[2xkd]], [[2xke]], [[2xkf]], [[2xnm]], [[2xnn]], [[2xno]], [[2xnp]], [[4a4x]], [[4afe]] – hChk Nek2 + inhibitor<br />
+**[[2jav]], [[2wqo]], [[2xk3]], [[2xk4]], [[2xk6]], [[2xk7]], [[2xk8]], [[2xkc]], [[2xkd]], [[2xke]], [[2xkf]], [[2xnm]], [[2xnn]], [[2xno]], [[2xnp]], [[4a4x]], [[4afe]] – hChk Nek2 + inhibitor<br />
-[[2w5a]], [[2w5b]] – hChk Nek2 + nucleotide<br />
+**[[2w5a]], [[2w5b]] – hChk Nek2 + nucleotide<br />
-[[2wqm]] – hChk Nek7<br />
+**[[2wqm]] – hChk Nek7<br />
-[[2wqn]] – hChk Nek7 + ADP<br />
+**[[2wqn]] – hChk Nek7 + ADP<br />
-===TANK-binding kinase===
+*'''TANK-binding kinase'''
-[[4efo]] – hChk Tbk1 ubiquitin-like domain  <br />
+**[[4efo]] – hChk Tbk1 ubiquitin-like domain  <br />
-[[4im0]], [[4im2]], [[4im3]], [[4iw0]], [[4iwo]], [[4iwp]], [[4ipq]] – hChk Tbk1 (mutant) + inhibitor  <br />
+**[[4im0]], [[4im2]], [[4im3]], [[4iw0]], [[4iwo]], [[4iwp]], [[4ipq]] – hChk Tbk1 (mutant) + inhibitor  <br />
-[[4eut]], [[4euu]] – hChk Tbk1 kinase+ubiquitin-like domains (mutant) + inhibitor  <br />
+**[[4eut]], [[4euu]] – hChk Tbk1 kinase+ubiquitin-like domains (mutant) + inhibitor  <br />
-[[4jl9]], [[4jlc]] – mChk Tbk1 + inhibitor  <br />
+**[[4jl9]], [[4jlc]] – mChk Tbk1 + inhibitor  <br />
-===Mechanistic target of rapamycin===
+*'''Mechanistic target of rapamycin'''
-[[2rse]] – hChk Mtor + FKBP1A - NMR <br />
+**[[2rse]] – hChk Mtor + FKBP1A - NMR <br />
-[[4drh]], [[4dri]], [[4drj]] – hChk Mtor + FKBP + rapamycin <br />
+**[[4drh]], [[4dri]], [[4drj]] – hChk Mtor + FKBP + rapamycin <br />
-[[4jsn]], [[4jsp]], [[4jsv]], [[4jsx]], [[4jt5]], [[4jt6]] – hChk Mtor + target of rapamycin complex<br />
+**[[4jsn]], [[4jsp]], [[4jsv]], [[4jsx]], [[4jt5]], [[4jt6]] – hChk Mtor + target of rapamycin complex<br />
-===Haspin===
+*'''Haspin'''
-[[2vuw]], [[2wb8]] – hChk Haspin kinase domain <br />
+**[[2vuw]], [[2wb8]] – hChk Haspin kinase domain <br />
-[[3dle]] – hChk Haspin kinase domain + AMP<br />
+**[[3dle]] – hChk Haspin kinase domain + AMP<br />
-[[3e7v]], [[3f2n]], [[3fmd]], [[3iq7]] – hChk Haspin kinase domain + inhibitor<br />
+**[[3e7v]], [[3f2n]], [[3fmd]], [[3iq7]] – hChk Haspin kinase domain + inhibitor<br />
-[[4ouc]] – hChk Haspin kinase domain + histone H3 peptide<br />
+**[[4ouc]] – hChk Haspin kinase domain + histone H3 peptide<br />
-===MAP/microtubule affinity-regulating kinase (Mark)===
+*'''MAP/microtubule affinity-regulating kinase (Mark)'''
-[[2r0i]] – rChk Mark1 catalytic+UBA domains (mutant)<br />
+**[[2r0i]] – rChk Mark1 catalytic+UBA domains (mutant)<br />
-[[2wzj]] – rChk Mark2 catalytic+UBA domains (mutant)<br />
+**[[2wzj]] – rChk Mark2 catalytic+UBA domains (mutant)<br />
-[[2hak]] – hChk Mark1 catalytic+UBA domains <br />
+**[[2hak]] – hChk Mark1 catalytic+UBA domains <br />
-[[3ose]] - hChk Mark1 kinase domain <br />
+**[[3ose]] - hChk Mark1 kinase domain <br />
-[[3iec]] – hChk Mark1 catalytic+UBA domains + cytotoxicity-associated immunodominant antigen<br />
+**[[3iec]] – hChk Mark1 catalytic+UBA domains + cytotoxicity-associated immunodominant antigen<br />
-===Mitotic checkpoint Chk Bub===
+*'''Mitotic checkpoint Chk (Bub)'''
-[[2lah]] – hChk Bub1 N terminal – NMR<br />
+**[[2lah]] – hChk Bub1 N terminal – NMR<br />
-[[2wvi]] – hChk Bub1β N terminal <br />
+**[[2wvi]] – hChk Bub1β N terminal <br />
-[[3e7e]] – hChk Bub1 residues 724-1025<br />
+**[[3e7e]] – hChk Bub1 residues 724-1025<br />
-[[3si5]] – hChk Bub1 residues 67-220 + CASC5 peptide<br />
+**[[3si5]] – hChk Bub1 residues 67-220 + CASC5 peptide<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 />
+**[[4ggd]] - hChk Bub1 + cell division cycle protein<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 />
-===Microtubule-associated Chk===
+*'''Microtubule-associated Chk'''
-[[2m9x]] – hChk 1 residues 187-287 – NMR<br />
+**[[2m9x]] – hChk 1 residues 187-287 – NMR<br />
-[[3ps4]] - hChk 1 residues 965-1057<br />
+**[[3ps4]] - hChk 1 residues 965-1057<br />
-[[2kqf]], [[2kyl]] – hChk 2 PDZ domain + glycoprotein C terminal – NMR<br />
+**[[2kqf]], [[2kyl]] – hChk 2 PDZ domain + glycoprotein C terminal – NMR<br />
-[[3khf]] - hChk 3 PDZ domain <br />
+**[[3khf]] - hChk 3 PDZ domain <br />
-[[2w7r]] – hChk 4 PDZ domain <br />
+**[[2w7r]] – hChk 4 PDZ domain <br />
-===Various Chk===
+*'''Other Chk'''
-[[1u5q]], [[1u5r]] – rChk Tao2 kinase domain <br />
+**[[1u5q]], [[1u5r]] – rChk Tao2 kinase domain <br />
-[[2lru]] – rChk Wnk1 autoinhibitory domain - NMR<br />
+**[[2lru]] – rChk Wnk1 autoinhibitory domain - NMR<br />
-[[2cos]] – Chk Lats2 – mouse – NMR<br />
+**[[2cos]] – Chk Lats2 – mouse – NMR<br />
-[[1wak]] – hChk Sprk1 <br />
+**[[1wak]] – hChk Sprk1 <br />
-[[2kty]], [[2kul]], [[2lav]], [[2rsv]] – hChk Vrk1 - NMR <br />
+**[[2kty]], [[2kul]], [[2lav]], [[2rsv]] – hChk Vrk1 - NMR <br />
-[[3op5]] – hChk Vrk1 kinase domain (mutant)<br />
+**[[3op5]] – hChk Vrk1 kinase domain (mutant)<br />
-[[2v62]] – hChk Vrk2 kinase domain <br />
+**[[2v62]] – hChk Vrk2 kinase domain <br />
-[[3dak]] – hChk Osr1 kinase domain  <br />
+**[[3dak]] – hChk Osr1 kinase domain  <br />
-[[3fpq]] - hChk Wnk1 kinase domain  (mutant)<br />
+**[[3fpq]] - hChk Wnk1 kinase domain  (mutant)<br />
-[[4aw2]] – hChk Mrckα kinase domain<br />
+**[[4aw2]] – hChk Mrckα kinase domain<br />
-[[1how]], [[1zxe]], [[1zy4]] – yChk  (mutant)<br />
+**[[1how]], [[1zxe]], [[1zy4]] – yChk  (mutant)<br />
-[[1q8z]], [[1zyc]] – yChk <br />
+**[[1q8z]], [[1zyc]] – yChk <br />
-[[1ow5]], [[1x9x]] – yChk Ste11 SAM domain – NMR<br />
+**[[1ow5]], [[1x9x]] – yChk Ste11 SAM domain – NMR<br />
-[[2kio]], [[2kit]] – yChk Tor1 FATC domain – NMR<br />
+**[[2kio]], [[2kit]] – yChk Tor1 FATC domain – NMR<br />
-[[2yz0]] – yChk Gcn2 RWD/GI domain – NMR<br />
+**[[2yz0]] – yChk Gcn2 RWD/GI domain – NMR<br />
-[[4otm]] – yChk Gcn2 C terminal domain <br />
+**[[4otm]] – yChk Gcn2 C terminal domain <br />
-[[3gre]] – yChk Vps15 WD repeat domain<br />
+**[[3gre]] – yChk Vps15 WD repeat domain<br />
-[[3osm]], [[3ost]] - yChk Kcc4 kinase domain <br />
+**[[3osm]], [[3ost]] - yChk Kcc4 kinase domain <br />
-[[1uf0]] – hChk Dcamkl1 DCX domain – NMR<br />
+**[[1uf0]] – hChk Dcamkl1 DCX domain – NMR<br />
-[[1xte]], [[1xtn]] – mChk Sgk3 PX domain <br />
+**[[1xte]], [[1xtn]] – mChk Sgk3 PX domain <br />
-[[3tpd]], [[3tpe]] – EcChk Hipa – ''Escherichia coli''<br />
+**[[3tpd]], [[3tpe]] – EcChk Hipa – ''Escherichia coli''<br />
-[[3tpb]] – EcChk Hipa (mutant) <br />
+**[[3tpb]] – EcChk Hipa (mutant) <br />
-[[4f0g]] – smChk Roco4 kinase domain – slime mold<br />
+**[[4f0g]] – smChk Roco4 kinase domain – slime mold<br />
-===Various Chk complexes===
+*Other Chk complexes
-[[2gcd]] – rChk Tao2 kinase domain + staurosporin<br />
+**[[2gcd]] – rChk Tao2 kinase domain + staurosporin<br />
-[[3hgk ]]– Chk Pto + effector protein AVRPTOB – Currant tomato<br />
+**[[3hgk]] – Chk Pto + effector protein AVRPTOB – Currant tomato<br />
-[[1wbp]] – hChk Sprk1 + peptide<br />
+**[[1wbp]] – hChk Sprk1 + peptide<br />
-[[3beg]] – hChk Srpk1 + splicing factor SF2<br />
+**[[3beg]] – hChk Srpk1 + splicing factor SF2<br />
-[[3hdm]], [[3hdn]] – hChk Sgk1 (mutant) + inhibitor <br />
+**[[3hdm]], [[3hdn]] – hChk Sgk1 (mutant) + inhibitor <br />
-[[2r5t]] – hChk Sgk3 + AMPPNP <br />
+**[[2r5t]] – hChk Sgk3 + AMPPNP <br />
-[[2uv2]] – hChk Ste20 + inhibitor <br />
+**[[2uv2]] – hChk Ste20 + inhibitor <br />
-[[2v3s]] – hChk Osr1 + hChk Wnk4 peptide <br />
+**[[2v3s]] – hChk Osr1 + hChk Wnk4 peptide <br />
-[[2vwi]] – hChk Osr1 kinase domain + ANP <br />
+**[[2vwi]] – hChk Osr1 kinase domain + ANP <br />
-[[3ggf]] – hChk Mst4 + inhibitor <br />
+**[[3ggf]] – hChk Mst4 + inhibitor <br />
-[[4geh]], [[3w8i]] - hChk Mst4 dimerization domain + programmed cell death protein 10<br />
+**[[4geh]], [[3w8i]] - hChk Mst4 dimerization domain + programmed cell death protein 10<br />
-[[4fza]], [[4fzd]], [[4fzf]] – hChk Mst4 (mutant) + calcium-binding protein <br />
+**[[4fza]], [[4fzd]], [[4fzf]] – hChk Mst4 (mutant) + calcium-binding protein <br />
-[[4crs]] – hChk N2 kinase domain + ATPγS<br />
+**[[4crs]] – hChk N2 kinase domain + ATPγS<br />
-[[3tku]] – hChk Mrckβ + fasudil<br />
+**[[3tku]] – hChk Mrckβ + fasudil<br />
-[[1q8y]], [[1q97]], [[1q99]], [[1zyd]] – yChk + nucleotide<br />
+**[[1q8y]], [[1q97]], [[1q99]], [[1zyd]] – yChk + nucleotide<br />
-[[1zy5]] – yChk (mutant) + nucleotide<br />
+**[[1zy5]] – yChk (mutant) + nucleotide<br />
-[[2jd5]] – yChk + NPL-3P<br />
+**[[2jd5]] – yChk + NPL-3P<br />
-[[3p86]], [[3ppz]] - AtChk Ctr1 + staurosporin<br />
+**[[3p86]], [[3ppz]] - AtChk Ctr1 + staurosporin<br />
-[[3tpt]] – EcChk Hipa (mutant) + ADP<br />
+**[[3tpt]] – EcChk Hipa (mutant) + ADP<br />
-[[3tpv]] – EcChk Hipa + ADP<br />
+**[[3tpv]] – EcChk Hipa + ADP<br />
-[[4f0f]] – smChk Roco4 kinase domain + APPCP <br />
+**[[4f0f]] – smChk Roco4 kinase domain + APPCP <br />
-[[4f1m]], [[4f1o]] – smChk Roco4 kinase domain (mutant) + APPCP <br />
+**[[4f1m]], [[4f1o]] – smChk Roco4 kinase domain (mutant) + APPCP <br />
-[[4f1t]] – smChk Roco4 kinase domain + inhibitor <br />
+**[[4f1t]] – smChk Roco4 kinase domain + inhibitor <br />
+}}
+===References===
-'''References'''
 <references/>
 [[Category:Topic Page]]

Serine/threonine protein kinase

From Proteopedia

Revision as of 09:44, 10 December 2014

3D structures of serine/threonine protein kinase

References

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