GTPase KRas: Difference between revisions
Jump to navigation
Jump to search
No edit summary |
Michal Harel (talk | contribs) No edit summary |
||
| Line 20: | Line 20: | ||
*<scene name='78/781207/Cv/8'>Mg coordination site</scene>. | *<scene name='78/781207/Cv/8'>Mg coordination site</scene>. | ||
*<scene name='78/781207/Cv/10'>GDP/Mg binding cleft</scene>. | *<scene name='78/781207/Cv/10'>GDP/Mg binding cleft</scene>. | ||
== 3D Structures of GTPase KRas == | |||
[[GTPase KRas 3D structures]] | |||
</StructureSection> | </StructureSection> | ||
== 3D Structures of GTPase KRas == | == 3D Structures of GTPase KRas == | ||
| Line 30: | Line 34: | ||
**[[5uk9]] – hKRas + GCP + GDP – human <br /> | **[[5uk9]] – hKRas + GCP + GDP – human <br /> | ||
**[[5vq2]] – hKRas + GTP <br /> | **[[5vq2]] – hKRas + GTP <br /> | ||
**[[6god]] – hKRas + GPPNP <br /> | |||
**[[6goe]], [[6gof]], [[6gog]], [[6gom]] – hKRas (mutant) + GPPNP <br /> | |||
**[[5w22]], [[4obe]], [[4lpk]], [[5vq8]] – hKRas + GDP <br /> | **[[5w22]], [[4obe]], [[4lpk]], [[5vq8]] – hKRas + GDP <br /> | ||
**[[3gft]] – hKRas (mutant) + GTP analog <br /> | **[[3gft]] – hKRas (mutant) + GTP analog <br /> | ||
**[[4l8g]], [[4ldj]], [[4ql3]], [[4tq9]], [[4tqa]], [[6asa]], [[6ase]], [[5whd]], [[5uqw]], [[5us4]], [[5vp7]], [[5vq0]], [[5vq1]], [[4wa7]], [[4lrw]] – hKRas (mutant) + GDP <br /> | **[[4l8g]], [[4ldj]], [[4ql3]], [[4tq9]], [[4tqa]], [[6asa]], [[6ase]], [[5whd]], [[5uqw]], [[5us4]], [[5vp7]], [[5vq0]], [[5vq1]], [[4wa7]], [[4lrw]], [[6bof]] – hKRas (mutant) + GDP <br /> | ||
**[[5vpi]], [[5vpz]], [[5vq6]] – hKRas (mutant) + GTP <br /> | **[[5vpi]], [[5vpz]], [[5vq6]] – hKRas (mutant) + GTP <br /> | ||
**[[5usj]], [[5vpy]] – hKRas (mutant) + GNP <br /> | **[[5usj]], [[5vpy]] – hKRas (mutant) + GNP <br /> | ||
| Line 40: | Line 46: | ||
**[[5kyk]] – hKRas + inhibitor <br /> | **[[5kyk]] – hKRas + inhibitor <br /> | ||
**[[4nmm]] – hKRas (mutant) + inhibitor <br /> | **[[4nmm]] – hKRas (mutant) + inhibitor <br /> | ||
**[[5v9o]], [[5f2e]], [[5v9u]], [[4dsu]], [[4luc]], [[4lv6]], [[4lyf]], [[4lyh]], [[4lyj]], [[4m1o]], [[4m1s]], [[4m1t]], [[4m1w]], [[4m1y]], [[4m21]], [[4m22]], [[4epr]], [[4ept]], [[4epv]], [[4epw]], [[4epx]], [[4epy]], [[4q01]], [[4q02]], [[4q03]], [[5vbm]], [[5v6s]], [[5v6v]], [[6ark]], [[5xco]], [[6b0v]], [[6b0y]], [[5yxz]], [[5yy1]], [[4pzy]], [[4pzz]] – hKRas (mutant) + GDP + inhibitor <br /> | **[[5v9o]], [[5f2e]], [[5v9u]], [[4dsu]], [[4luc]], [[4lv6]], [[4lyf]], [[4lyh]], [[4lyj]], [[4m1o]], [[4m1s]], [[4m1t]], [[4m1w]], [[4m1y]], [[4m21]], [[4m22]], [[4epr]], [[4ept]], [[4epv]], [[4epw]], [[4epx]], [[4epy]], [[4q01]], [[4q02]], [[4q03]], [[5vbm]], [[5v6s]], [[5v6v]], [[6ark]], [[5xco]], [[6b0v]], [[6b0y]], [[5yxz]], [[5yy1]], [[4pzy]], [[4pzz]], [[6n2j]], [[6n2k]] – hKRas (mutant) + GDP + inhibitor <br /> | ||
**[[5vbz]] – hKRas (mutant) + GNP + inhibitor <br /> | **[[5vbz]], [[6gqy]], [[6gqw]], [[6gqx]], [[6gqt]] – hKRas (mutant) + GNP + inhibitor <br /> | ||
**[[6fa1]], [[6fa2]], [[6fa3]], [[6fa4]], [[5oct]], [[5oco]], [[5ocg]] – hKRas (mutant) + GNP + inhibitor<br /> | |||
**[[6f76]] – hKRas (mutant) + GPPNP + inhibitor<br /> | |||
**[[5v71]], [[5v9l]] – hKRas (mutant) + GDP + quinazoline inhibitor <br /> | **[[5v71]], [[5v9l]] – hKRas (mutant) + GDP + quinazoline inhibitor <br /> | ||
| Line 48: | Line 56: | ||
**[[5wha]], [[5whb]] – hKRas (mutant) + miniprotein + GDP <br /> | **[[5wha]], [[5whb]] – hKRas (mutant) + miniprotein + GDP <br /> | ||
**[[5wpl]], [[5whe]], [[5wpm]], [[5wlb]] – hKRas (mutant) + miniprotein + GNP <br /> | **[[5wpl]], [[5whe]], [[5wpm]], [[5wlb]] – hKRas (mutant) + miniprotein + GNP <br /> | ||
**[[6h46]] – hKRas + darpin K13 + GDP <br /> | |||
**[[6h47]] – hKRas + darpin K19 <br /> | |||
**[[5o2s]], [[5mlb]] – hKRas + darpin K27 + GDP <br /> | **[[5o2s]], [[5mlb]] – hKRas + darpin K27 + GDP <br /> | ||
**[[5tb5]], [[5tar]] – hKRas + GMP-PDE d + farnesyl + GDP <br /> | **[[5tb5]], [[5tar]] – hKRas + GMP-PDE d + farnesyl + GDP <br /> | ||
| Line 55: | Line 65: | ||
**[[2msc]], [[2msd]] – hKRas + apolipoprotein + GDP - NMR<br /> | **[[2msc]], [[2msd]] – hKRas + apolipoprotein + GDP - NMR<br /> | ||
**[[2mse]] – hKRas + apolipoprotein + A-Raf + GDP - NMR<br /> | **[[2mse]] – hKRas + apolipoprotein + A-Raf + GDP - NMR<br /> | ||
**[[6ccx]], [[6cch]], [[6cc9]] – hKRas (mutant) + apolipoprotein + inhibitor + GPPNP - NMR<br /> | |||
**[[6epl]] – hKRas (mutant) + son of sevenless homolog 1<br /> | |||
**[[6epm]], [[6epn]], [[6epo]], [[6epp]] – hKRas (mutant) + son of sevenless homolog 1 + inhibitor<br /> | |||
}} | }} | ||
Revision as of 10:30, 21 July 2019
FunctionGTPase KRas (KRas) plays a critical role in the control of cellular growth. Kras stands for Kirsten rat sarcoma virus gene. KRas is a small GTPase that functions as molecular switches by alternating between inactive GDP-bound state and active GTP-bound state[1]. DiseaseA single mutation of KRas G12C activates KRas and is implicated with various malignancies including lung adenocarcinoma, mutinous adenoma, ductal carcinoma of the pancreas and colorectal carcinoma[2]. KRas mutations are the most common genetic abnormalities in cancer. RelevanceKRas inhibition represents an attractive therapeutic strategy for many cancers. Structural highlightsThe GDP-bound KRas binds a following conformational change of the protein[3]. Water molecules are shown as red spheres.
3D Structures of GTPase KRas
|
| ||||||||||
3D Structures of GTPase KRas3D Structures of GTPase KRas
Updated on 21-July-2019
ReferencesReferences
- ↑ 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
- ↑ 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
- ↑ 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