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Paper · 24256730

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.

Ostrem JM and 4 others. Nature, 2013. Cited by 2,104 papers, by iCite.

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ConductScience Library. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Papers, record 24256730. Release papers-2026-11-12-0.1.0, 12 Nov 2026. https://conductscience.org/library/papers/24256730

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Paper

PubMed's record of the paper, with iCite's citation figures. No abstract is shown.

Title
K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions.
PubMed
Journal
Nature
PubMed
Year
2013
PubMed
Publication types
Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.
PubMed
Citations, by iCite
2,104
iCite
Relative citation ratio, by iCite
54.4
iCite
Revised in PubMed
2025-05-29
PubMed

Authors5

The authors in the order PubMed's record lists them, with the ORCID iDs it states.

OrderAuthorForenameKindORCID iD
1Ostrem JMJonathan M
2Peters UUlf
3Sos MLMartin L
4Wells JAJames A
5Shokat KMKevan M

Source PubMed

Topics18

NLM's MeSH indexing of the paper, its major topics first.

MeSH termMajor
Allosteric SiteMajor topic
Guanosine DiphosphateMajor topic
Guanosine TriphosphateMajor topic
Mutant ProteinsMajor topic
Oncogene Protein p21(ras)Major topic
Allosteric Regulation
Apoptosis
Cell Line, Tumor
Crystallography, X-Ray
Cysteine
Drug Discovery
Genes, ras
Humans
Lung Neoplasms
Models, Molecular
Static Electricity
Substrate Specificity
raf Kinases

Source PubMed

Grants2

Each grant PubMed's record writes, matched to the NIH project NIH's grant and paper links name for this paper, and each of those links the record does not write.

Grant, as the record writes itAgencyCountryNIH projectStated bySource
Howard Hughes Medical InstituteUnited StatesPubMedPubMed
T32 GM064337NIGMS NIH HHSUnited StatesT32GM064337PubMed and NIHNIH RePORTER

Trials0

The trials whose ClinicalTrials.gov record lists the paper, and the trial numbers the paper's PubMed record names.

None in this release.

Comments and corrections2

PubMed's comments and corrections, NLM's own indexing: retractions first, then expressions of concern, errata and updates, and comments last.

KindPMIDTitleIn PapersSource
Comment in24,256,732Drug discovery: Pocket of opportunity.https://conductscience.org/library/papers/24256732PubMed
Comment in24,304,874Oncogenes: direct hit on mutant RAS.https://conductscience.org/library/papers/24304874PubMed

References29

The papers the reference list in PubMed's record names, those in our copy of PubMed, in the list's order.

OrderPMIDTitleJournalYearIn PapersSource
13,145,408Inhibition of NIH 3T3 cell proliferation by a mutant ras protein with preferential affinity for GDP.Mol Cell Biol1988https://conductscience.org/library/papers/3145408PubMed
29,043,664Ras oncoprotein inhibitors: the discovery of potent, ras nucleotide exchange inhibitors and the structural determination of a drug-protein complex.Bioorg Med Chem1997https://conductscience.org/library/papers/9043664PubMed
36,148,751Intrinsic GTPase activity distinguishes normal and oncogenic ras p21 molecules.Proc Natl Acad Sci U S A1984https://conductscience.org/library/papers/6148751PubMed
42,406,906Molecular switch for signal transduction: structural differences between active and inactive forms of protooncogenic ras proteins.Science1990https://conductscience.org/library/papers/2406906PubMed
521,500,860Simple one-pot synthesis of disulfide fragments for use in disulfide-exchange screening.ACS Comb Sci2011https://conductscience.org/library/papers/21500860PubMed
62,199,829K-ras oncogene activation as a prognostic marker in adenocarcinoma of the lung.N Engl J Med1990https://conductscience.org/library/papers/2199829PubMed
72,200,519Kinetics of interaction of nucleotides with nucleotide-free H-ras p21.Biochemistry1990https://conductscience.org/library/papers/2200519PubMed
823,630,290In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction.Proc Natl Acad Sci U S A2013https://conductscience.org/library/papers/23630290PubMed
922,566,140Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.Angew Chem Int Ed Engl2012https://conductscience.org/library/papers/22566140PubMed
102,476,675Structure of the guanine-nucleotide-binding domain of the Ha-ras oncogene product p21 in the triphosphate conformation.Nature1989https://conductscience.org/library/papers/2476675PubMed

Cited by1,418

The papers in our copy of PubMed whose reference list names this one, newest first. iCite, which reads more sources, counts 2,104 citations.

PMIDTitleJournalYearIn PapersSource
42,972,081A selective TNKS2 inhibitor for tumor-restricted WNT suppression.Nat Chem Biol2026https://conductscience.org/library/papers/42972081PubMed
42,963,543KRAS in pancreatic cancer: from molecular biology to transformative therapeutics.J Hematol Oncol2026https://conductscience.org/library/papers/42963543PubMed
42,958,559Targeted protein degradation in cancer: strategies for undruggable targets and progress towards clinical translation.Biomark Res2026https://conductscience.org/library/papers/42958559PubMed
42,957,732Structural mechanisms underlying resistance to Switch-II pocket inhibitors in KRAS.Nat Commun2026https://conductscience.org/library/papers/42957732PubMed
42,943,275Drugging the Undruggable in Oncology: Structural Computation, Machine Learning, and Generative AI for Historically Intractable Targets.Pharmaceuticals (Basel)2026https://conductscience.org/library/papers/42943275PubMed
42,936,912Uncovering KRAS-mutant allele-specific biology and vulnerabilities in non-small cell lung cancer.Biochem J2026https://conductscience.org/library/papers/42936912PubMed
42,924,280Drugging the "undruggable" p53: a structure-guided strategy against the Y220C mutation.Med Rev (2021)2026https://conductscience.org/library/papers/42924280PubMed
42,922,582Engineered caspases directly rewire mutant Ras to cell death.bioRxiv2026https://conductscience.org/library/papers/42922582PubMed
42,899,594In Pursuit of Enduring Inactivation: A Perspective on the Development and Study of Irreversible-Covalent Inhibitors.Biochemistry2026https://conductscience.org/library/papers/42899594PubMed
42,892,656Difluoromethylornithine modulates mutant K-RAS signaling pathways in pancreatic cancer cells.Amino Acids2026https://conductscience.org/library/papers/42892656PubMed

1 to 10 of 1,418

See all 1,418 cited by

Genes8

The genes the Gene search release ties to the paper: Swiss-Prot's references first, then PubTator's text mining.

GeneNCBI Gene IDLinked byIn GenesSource
BRAF673PubTator's text mininghttps://conductscience.org/library/genes/673NCBI Gene
GSTK1373,156PubTator's text mininghttps://conductscience.org/library/genes/373156NCBI Gene
HRAS3,265PubTator's text mininghttps://conductscience.org/library/genes/3265NCBI Gene
KRAS3,845PubTator's text mininghttps://conductscience.org/library/genes/3845NCBI Gene
NCKAP5344,148PubTator's text mininghttps://conductscience.org/library/genes/344148NCBI Gene
RAF15,894PubTator's text mininghttps://conductscience.org/library/genes/5894NCBI Gene
XYLT264,132PubTator's text mininghttps://conductscience.org/library/genes/64132NCBI Gene
ZHX222,882PubTator's text mininghttps://conductscience.org/library/genes/22882NCBI Gene

Drugs0

The drugs whose trials, in the Pipelines release, list the paper.

None in this release.

Data0

The data bank entries PubMed's record names. Trial numbers are under Trials.

None in this release.

Data dates

The date of each source this release read.

PubMed
2026-11-06
PubMed
iCite
2026-11-05
iCite
PMC's ID file
2026-11-05
PMC's ID file
NIH RePORTER's grant and paper links
2026-11-01
NIH RePORTER's grant and paper links
Trials
2026-11-12
Gene search
2026-11-11
Pipelines
2026-09-18

Sources 11

  • ChEMBL, through Open TargetsCC BY-SA 3.0
  • ClinicalTrials.govNo license stated
  • HGNCCC0
  • iCiteCC BY 4.0
  • NCBI GenePublic domain (US government)
  • NIH RePORTER's grant and paper linksPublic domain
  • Open TargetsCC0 1.0
  • PMC's ID filePublic domain (US government)
  • PubMedNLM's terms
  • PubTator 3Public domain
  • UniProtCC BY 4.0
Each source's terms
  • ChEMBL, through Open TargetsCC BY-SA 3.0, for the parts from ChEMBL. Read on 8 Nov 2026 at https://platform-docs.opentargets.org/licence
  • ClinicalTrials.govnone stated
  • HGNCCC0: https://www.genenames.org/about/license/
  • iCiteCC BY 4.0
  • NCBI GeneNone named for the file. NCBI says information created by or for the US government on its site is in the public domain, and asks that NLM be acknowledged: https://www.ncbi.nlm.nih.gov/home/about/policies/
  • NIH RePORTER's grant and paper linksPublic domain (NIH RePORTER)
  • Open TargetsCC0 1.0. Open Targets asks that users cite its latest paper: Buniello et al. 2025, Open Targets Platform: facilitating therapeutic hypotheses building in drug discovery, Nucleic Acids Research 53(D1):D1467, PMID 39657122. Read on 8 Nov 2026 at https://platform-docs.opentargets.org/licence
  • PMC's ID fileNone named for the file. NCBI says information created by or for the US government on its site is in the public domain, and asks that NLM be acknowledged: https://www.ncbi.nlm.nih.gov/home/about/policies/
  • PubMedNLM's terms
  • PubTator 3Public domain
  • UniProtCC BY 4.0. UniProt's licence file: "All databases and documents in the UniProt FTP directory may be copied and redistributed freely, without advance permission, provided that this copyright statement is reproduced with each copy." UniProt asks that users cite its latest paper: The UniProt Consortium, UniProt: the Universal Protein Knowledgebase in 2025, Nucleic Acids Research 53:D609-D617, https://doi.org/10.1093/nar/gkae1010. Read on 9 Nov 2026 at https://www.uniprot.org/help/license

ClinicalTrials.gov's data carry an international copyright outside the United States: https://clinicaltrials.gov/about-site/terms-conditions.

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