Ribosomal protein S6 kinase
From Proteopedia
(Difference between revisions)
(2 intermediate revisions not shown.) | |||
Line 1: | Line 1: | ||
<StructureSection load='' size='350' side='right' caption='Human ribosomal protein S6 kinase α−1 complex with the inhibitor purvalanol (PDB entry [[2z7s]])' scene='43/434545/Cv/2'> | <StructureSection load='' size='350' side='right' caption='Human ribosomal protein S6 kinase α−1 complex with the inhibitor purvalanol (PDB entry [[2z7s]])' scene='43/434545/Cv/2'> | ||
+ | __TOC__ | ||
== Function == | == Function == | ||
[[Ribosomal protein S6 kinase]] (RPS6K) regulates RPS6<ref>PMID:22168436</ref>. RPS6K activity controls the ribosome biogenesis transcriptional program. | [[Ribosomal protein S6 kinase]] (RPS6K) regulates RPS6<ref>PMID:22168436</ref>. RPS6K activity controls the ribosome biogenesis transcriptional program. | ||
- | + | *'''Ribosomal protein S6 kinase alpha''' confers resistance towards therapy of acute myeloid leukaemia using venetoclax/azacitidine<ref>PMID:37414921</ref>. | |
== Relevance == | == Relevance == | ||
- | hRPS6K α is | + | hRPS6K α is overexpressed in breast cancer and is associated with poor prognosis<ref>PMID:19085255</ref>. Inhibitors of RPS6S are studied as potential therapeutic agents for treatment of variety of diseases including diabetes and cancer<ref>PMID:24072592</ref>. |
== Structural highlights == | == Structural highlights == | ||
The <scene name='43/434545/Cv/5'>inhibitor purvalanol binds hRPS6K in the ATP-binding pocket between the N- and C-terminal lobes</scene><ref>PMID:17965187</ref>. <scene name='43/434545/Cv/6'>Active site</scene>. Water molecule are shown as red sphere. | The <scene name='43/434545/Cv/5'>inhibitor purvalanol binds hRPS6K in the ATP-binding pocket between the N- and C-terminal lobes</scene><ref>PMID:17965187</ref>. <scene name='43/434545/Cv/6'>Active site</scene>. Water molecule are shown as red sphere. | ||
- | + | ||
== 3D Structures of Ribosomal protein S6 kinase == | == 3D Structures of Ribosomal protein S6 kinase == | ||
+ | [[Ribosomal protein S6 kinase 3D structures]] | ||
- | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | ||
- | {{#tree:id=OrganizedByTopic|openlevels=0| | ||
- | |||
- | *Ribosomal protein S6 kinase α | ||
- | |||
- | **[[3rny]], [[2wnt]] - hRPS6K α−1 C-terminal kinase domain - human<br /> | ||
- | **[[1vzo]] - hRPS6K α−5 N-terminal kinase domain (mutant) <br /> | ||
- | **[[3kn6]] - hRPS6K α−5 C-terminal kinase domain<br /> | ||
- | **[[2qr7]], [[2qr8]] - mRPS6K α−3 C-terminal kinase domain (mutant) - mouse<br /> | ||
- | **[[3g51]] - mRPS6K α−3 N-terminal kinase domain<br /> | ||
- | |||
- | *Ribosomal protein S6 kinase α complex | ||
- | |||
- | **[[2z7s]], [[2z7r]] - hRPS6K α−1 N-terminal kinase domain+inhibitor<br /> | ||
- | **[[4nif]] - hRPS6K α−1 C-terminal kinase domain + mitogen-activated protein kinase 1<br /> | ||
- | **[[5csf]], [[5csi]], [[5csj]], [[5csn]] - hRPS6K α−1 residues 683-735 + S100-B<br /> | ||
- | **[[3ubd]] - hRPS6K α−3 N-terminal kinase domain + flavonol glycoside<br /> | ||
- | **[[7opo]] - hRPS6K α−3 N-terminal kinase domain + ORF45<br /> | ||
- | **[[5d9k]], [[5d9l]] - hRPS6K α−3 N-terminal kinase domain + inhibitor<br /> | ||
- | **[[4nus]], [[4nw5]], [[4nw6]] - hRPS6K α−3 N-terminal kinase domain + inhibitor<br /> | ||
- | **[[4d9t]], [[4d9u]], [[4jg6]], [[4jg7]], [[4jg8]], [[5o1s]] - hRPS6K α−3 C-terminal kinase domain + inhibitor<br /> | ||
- | **[[3kn5]] - hRPS6K α−5 C-terminal kinase domain+AMPPNP<br /> | ||
- | **[[2z7q]] - hRPS6K α−1 N-terminal kinase domain + AMPPCP<br /> | ||
- | **[[6g76]], [[6g77]] - hRPS6K α-6 N-terminal kinase domain+AMPPNP<br /> | ||
- | **[[6g78]] - hRPS6K α-6 N-terminal kinase domain (mutant) +AMPPNP<br /> | ||
- | **[[4gue]] - mRPS6K α−3 N-terminal kinase domain + flavonol glycoside<br /> | ||
- | **[[4el9]] - mRPS6K α−3 N-terminal kinase domain + inhibitor<br /> | ||
- | **[[4m8t]], [[4mao]] - mRPS6K α−3 C-terminal kinase domain (mutant) + inhibitor<br /> | ||
- | |||
- | *Ribosomal protein S6 kinase β | ||
- | |||
- | **[[3a60]], [[3a61]], [[3a62]], [[4l3j]], [[4l3l]] - hRPS6K β−1 kinase domain<br /> | ||
- | **[[4l42]], [[4l43]], [[4l44]], [[4l45]], [[4l46]], [[3we4]], [[3wf5]], [[3wf6]], [[4rlo]], [[4rlp]] - hRPS6K β−1 kinase domain + pyrimidine derivative<br /> | ||
- | **[[3wf7]] - hRPS6K β−1 kinase domain + purine derivative<br /> | ||
- | **[[3wf8]], [[3wf9]] - hRPS6K β−1 kinase domain + quinoline derivative<br /> | ||
- | |||
- | }} | ||
== References == | == References == | ||
<references/> | <references/> | ||
+ | </StructureSection> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] |
Current revision
|