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Transmembrane Domain Oligomerization Propensity determined by ToxR Assay
Published on: May 26, 2011
Capturing RAS oligomerization on a membrane
Sangho D Yun1, Elena Scott1, Jing-Yuan Chang1
1Department of Chemistry, Texas A&M University, College Station, TX 77843.
Abstract:
RAS GTPases associate with the biological membrane where they function as molecular switches to regulate cell growth. Recent studies indicate that RAS proteins oligomerize on membranes, and disrupting these assemblies represents an alternative therapeutic strategy. However, conflicting reports on RAS assemblies, ranging in size from dimers to nanoclusters, have brought to the fore key questions regarding the stoichiometry and parameters that influence oligomerization. Here, we probe three isoforms of RAS [Kirsten Rat Sarcoma viral oncogene (KRAS), Harvey Rat Sarcoma viral oncogene (HRAS), and Neuroblastoma oncogene (NRAS)] directly from membranes using mass spectrometry. We show that KRAS on membranes in the inactive state (GDP-bound) is monomeric but forms dimers in the active state (GTP-bound). We demonstrate that the small molecule BI2852 can induce dimerization of KRAS, whereas the binding of effector proteins disrupts dimerization. We also show that RAS dimerization is dependent on lipid composition and reveal that oligomerization of NRAS is regulated by palmitoylation. By monitoring the intrinsic GTPase activity of RAS, we capture the emergence of a dimer containing either mixed nucleotides or GDP on membranes. We find that the interaction of RAS with the catalytic domain of Son of Sevenless (SOScat) is influenced by membrane composition. We also capture the activation and monomer to dimer conversion of KRAS by SOScat. These results not only reveal the stoichiometry of RAS assemblies on membranes but also uncover the impact of critical factors on oligomerization, encompassing regulation by nucleotides, lipids, and palmitoylation.
Insights
RAS GTPases form dimers on cell membranes when active, a process influenced by lipids and palmitoylation. This dimerization is key to regulating cell growth and offers a potential therapeutic target.
Area of Science:
- Molecular Biology
- Cellular Signaling
- Biochemistry
Background:
- RAS GTPases are crucial molecular switches regulating cell growth by associating with cell membranes.
- RAS protein oligomerization on membranes is a recent finding, suggesting it as a therapeutic target.
- Conflicting reports on RAS assembly size necessitate clarification of stoichiometry and regulatory factors.
Purpose of the Study:
- To investigate the stoichiometry and influencing parameters of RAS protein oligomerization on membranes.
- To analyze three RAS isoforms (KRAS, HRAS, NRAS) directly from membranes.
- To understand how nucleotides, lipids, and palmitoylation affect RAS assembly and activity.
Main Methods:
- Mass spectrometry was used to analyze RAS isoforms (KRAS, HRAS, NRAS) directly from cell membranes.
- Intrinsic GTPase activity was monitored to observe RAS dimerization dynamics.
- The effect of small molecule BI2852 and effector protein Son of Sevenless (SOScat) on RAS was assessed.
Main Results:
- Inactive (GDP-bound) KRAS is monomeric on membranes, while active (GTP-bound) KRAS forms dimers.
- The small molecule BI2852 induces KRAS dimerization; effector protein binding disrupts it.
- RAS dimerization depends on lipid composition, and NRAS oligomerization is regulated by palmitoylation.
Conclusions:
- RAS assembly stoichiometry on membranes is revealed, with dimers forming upon activation.
- Nucleotide-bound state, lipid composition, and palmitoylation critically regulate RAS oligomerization.
- Understanding these factors provides insights into RAS signaling and potential therapeutic strategies.
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