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GTPase KRas

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<StructureSection load='4ept' size='400' side='right' caption='Structure of human GDP-bound GTPase KRas G12 mutant complex with inhibitor and GDP (PDB entry [[4ept]])' scene='78/781207/Cv/1'>
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<StructureSection load='' size='400' side='right' caption='Structure of human GDP-bound GTPase KRas G12 mutant complex with inhibitor and GDP (PDB entry [[4ept]])' scene='78/781207/Cv/1'>
== Function ==
== Function ==
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== Structural highlights ==
== Structural highlights ==
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The GDP-bound KRas binds a <scene name='78/781207/Cv/2'>small molecule inhibitor in its binding cleft</scene> following conformational change of the protein<ref>PMID:22566140</ref>. <scene name='78/781207/Cv/6'>GDP binding site</scene>.
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The GDP-bound KRas binds a <scene name='78/781207/Cv/2'>small molecule inhibitor in its binding cleft</scene> following conformational change of the protein<ref>PMID:22566140</ref>. Water molecules are shown as red spheres.
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</StructureSection>
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*<scene name='78/781207/Cv/9'>Inhibitor binding cleft</scene>.
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*<scene name='78/781207/Cv/7'>GDP binding site</scene>.
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*<scene name='78/781207/Cv/8'>Mg coordination site</scene>.
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*<scene name='78/781207/Cv/10'>GDP/Mg binding cleft</scene>.
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== 3D Structures of GTPase KRas ==
== 3D Structures of GTPase KRas ==
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[[GTPase KRas 3D structures]]
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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</StructureSection>
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{{#tree:id=OrganizedByTopic|openlevels=0|
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*GTPase KRas
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**[[5uk9]] – hKRas + GCP + GDP – human <br />
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**[[5vq2]] – hKRas + GTP <br />
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**[[5w22]], [[4obe]], [[4lpk]], [[5vq8]] – hKRas + GDP <br />
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**[[3gft]] – hKRas (mutant) + GTP analog <br />
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**[[4l8g]], [[4ldj]], [[4ql3]], [[4tq9]], [[4tqa]], [[6asa]], [[6ase]], [[5whd]], [[5uqw]], [[5us4]], [[5vp7]], [[5vq0]], [[5vq1]], [[4wa7]], [[4lrw]] – hKRas (mutant) + GDP <br />
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**[[5vpi]], [[5vpz]], [[5vq6]] – hKRas (mutant) + GTP <br />
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**[[5usj]], [[5vpy]] – hKRas (mutant) + GNP <br />
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**[[6bp1]], [[4dsn]] – hKRas (mutant) + GCP <br />
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**[[4dso]] – hKRas (mutant) + inhibitor + GSP <br />
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**[[4dst]] – hKRas (mutant) + inhibitor + GCP <br />
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**[[5kyk]] – hKRas + inhibitor <br />
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**[[4nmm]] – hKRas (mutant) + inhibitor <br />
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**[[5v9o]], [[5f2e]], [[5v9u]], [[4dsu]], [[4luc]], [[4lv6]], [[4lyf]], [[4lyh]], [[4lyj]], [[4m1o]], [[4m1s]], [[4m1t]], [[4m1w]], [[4m1y]], [[4m21]], [[4m22]], [[4epr]], [[4ept]], [[4epv]], [[4epw]], [[4epx]], [[4epy]], [[4q02]], [[4q03]], [[5vbm]], [[5v6s]], [[5v6v]], [[6ark]], [[5xco]] – hKRas (mutant) + GDP + inhibitor <br />
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**[[5vbz]] – hKRas (mutant) + GNP + inhibitor <br />
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**[[5v71]], [[5v9l]] – hKRas (mutant) + GDP + quinazoline inhibitor <br />
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*GTPase KRas complex with protein
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**[[5wha]], [[5whb]] – hKRas (mutant) + miniprotein + GDP <br />
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**[[5wpl]], [[5whe]], [[5wpm]], [[5wlb]] – hKRas (mutant) + miniprotein + GNP <br />
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**[[5o2s]], [[5mlb]] – hKRas + darpin K27 + GDP <br />
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**[[5o2s]], [[5tb5]] – hKRas + GMP-PDE d + farnesyl + GDP <br />
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**[[5o2t]], [[5mla]] – hKRas + darpin 55 + GSP <br />
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**[[5o2s]] – hKRas + R11.1.6 + GNP <br />
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**[[5ufq]] – hKRas (mutant) + R11.1.6 + GNP <br />
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**[[2msc]], [[2msd]] – hKRas + apolipoprotein + GDP - NMR<br />
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**[[2mse]] – hKRas + apolipoprotein + A-Raf + GDP - NMR<br />
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}}
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== References ==
== References ==
<references/>
<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]

Current revision

Structure of human GDP-bound GTPase KRas G12 mutant complex with inhibitor and GDP (PDB entry 4ept)

Drag the structure with the mouse to rotate

References

  1. ↑ Milburn MV, Tong L, deVos AM, Brunger A, Yamaizumi Z, Nishimura S, Kim SH. Molecular switch for signal transduction: structural differences between active and inactive forms of protooncogenic ras proteins. Science. 1990 Feb 23;247(4945):939-45. PMID:2406906
  2. ↑ Shibata H, Ohike N, Norose T, Isobe T, Suzuki R, Imai H, Shiokawa A, Aoki T, Murakami M, Mizukami H, Tanaka JI, Takimoto M. Mucinous Cystic Neoplasms Lined by Abundant Mucinous Epithelium Frequently Involve KRAS Mutations and Malignant Progression. Anticancer Res. 2017 Dec;37(12):7063-7068. doi: 10.21873/anticanres.12178. PMID:29187496 doi:http://dx.doi.org/10.21873/anticanres.12178
  3. ↑ Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW. Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation. Angew Chem Int Ed Engl. 2012 May 8. doi: 10.1002/anie.201201358. PMID:22566140 doi:10.1002/anie.201201358

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman

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