GTPase KRas: Difference between revisions
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<StructureSection load='4ept' size='350' side='right' caption='Structure of yeast cytosine deaminase complex with pyrimidine-based inhibitor, acetate, Ca+2 (green) and Zn+2 (grey) ions (PDB entry [[4ept]])' scene=''> | |||
== Function == | == Function == | ||
'''GTPase 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<ref>PMID:2406906</ref>. | |||
== Disease == | == Disease == | ||
A 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<ref>PMID:29187496</ref>. KRas mutations are the most common genetic abnormalities in cancer. | |||
== Relevance == | == Relevance == | ||
KRas inhibition represents an attractive therapeutic strategy for many cancers. | |||
== Structural highlights == | == Structural highlights == | ||
The GDP-bound KRas binds a small molecule inhibitor in its binding cleft following conformational change of the protein<ref>PMID:22566140</ref>. | |||
</StructureSection> | </StructureSection> | ||
== 3D Structures of GTPase KRas == | == 3D Structures of GTPase KRas == | ||
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**[[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]], | **[[4l8g]], [[4ldj]], [[4ql3]], [[4tq9]], [[4tqa]], [[6asa]], [[6ase]], [[5whd]], [[5uqw]], [[5us4]], [[5vp7]], [[5vq0]], [[5vq1]], [[4wa7]], [[4lrw]] – 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 /> | ||
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== References == | == References == | ||
<references/> | <references/> | ||
[[Category:Topic Page]] | |||