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Record W3023317226 · doi:10.1158/1557-3125.ras18-ia09

Abstract IA09: Targeting K-RAS4B on biologic membranes

2020· article· en· W3023317226 on OpenAlexaff
Mitsuhiko Ikura

Bibliographic record

VenueMolecular Cancer Research · 2020
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicCancer Research and Treatments
Canadian institutionsPrincess Margaret Cancer Centre
Fundersnot available
KeywordsPrenylationSignal transductionCell biologyCancerMembraneKinaseMutantChemistryBiologyCancer researchBiochemistryGeneGeneticsEnzyme

Abstract

fetched live from OpenAlex

Abstract RAS proteins are frequently mutated in cancer (~30% of all human tumors) and an estimated worldwide death toll of RAS-associated cancers exceeds 2 million/yr. Despite enormous efforts in RAS research over three decades, there is no clinically approved RAS inhibitor and the RAS protein remains a challenging target for cancer therapy development. In order to overcome this challenge, we sought to better understand how RAS functions under physiologic conditions and alters related signaling pathways in the mutant RAS-driven tumors. Fully matured protein K-RAS4B, the major target for cancer therapeutics, is prenylated and methylated at the carboxy-terminus, which enables K-RAS4B to anchor to the plasma membrane where it receives an upstream signal and transmits the signal to a number of downsteam pathways. There is, however, a large gap in our understanding of how the matured K-RAS4B protein functions at the surface of the plasma membrane. As a first step, we sought to develop new conformational and functional assays for the RAS protein on lipid bilayers (i.e., nanodiscs) using various biochemical and biophysical techniques. We elucidated how the membrane environment dictates the conformation of K-RAS4B and how oncogenic mutations influence the membrane-dependent conformational states of the protein (Mazhab-Jafari et al., PNAS 2015). More recently, we have been investigating multiple aspects of K-RAS4B functions and I will discuss (i) how the biologic membrane influences K-RAS4B interaction with a binding domain of RAF kinases and (ii) how we could inhibit K-RAS4B at the membrane surface by small molecules (Fang et al., Cell Chem Biol 2018) and an engineered protein. Supported by CCS, CIHR, CFI and PMCF. Citation Format: Mitsu Ikura. Targeting K-RAS4B on biologic membranes [abstract]. In: Proceedings of the AACR Special Conference on Targeting RAS-Driven Cancers; 2018 Dec 9-12; San Diego, CA. Philadelphia (PA): AACR; Mol Cancer Res 2020;18(5_Suppl):Abstract nr IA09.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.092
Threshold uncertainty score0.752

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.079
GPT teacher head0.401
Teacher spread0.323 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations0
Published2020
Admission routes1
Has abstractyes

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