GTPase KRas

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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>.
+
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.
*<scene name='78/781207/Cv/9'>Inhibitor binding cleft</scene>.
*<scene name='78/781207/Cv/9'>Inhibitor binding cleft</scene>.
*<scene name='78/781207/Cv/7'>GDP binding site</scene>.
*<scene name='78/781207/Cv/7'>GDP binding site</scene>.

Revision as of 11:35, 4 April 2019

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

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3D Structures of GTPase KRas

Updated on 04-April-2019

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

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