Details of the Target

General Information of Target

Target ID LDTP01827
Target Name GTPase KRas (KRAS)
Gene Name KRAS
Gene ID 3845
Synonyms
KRAS2; RASK2; GTPase KRas; EC 3.6.5.2; K-Ras 2; Ki-Ras; c-K-ras; c-Ki-ras) [Cleaved into: GTPase KRas, N-terminally processed]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAG
QEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDL
PSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGC
VKIKKCIIM
Target Type
Successful
Target Bioclass
Enzyme
Family
Small GTPase superfamily, Ras family
Subcellular location
Cell membrane
Function
Ras proteins bind GDP/GTP and possess intrinsic GTPase activity. Plays an important role in the regulation of cell proliferation. Plays a role in promoting oncogenic events by inducing transcriptional silencing of tumor suppressor genes (TSGs) in colorectal cancer (CRC) cells in a ZNF304-dependent manner.
TTD ID
T59480
Uniprot ID
P01116
DrugMap ID
TTLJX8E
Ensemble ID
ENST00000256078.10
HGNC ID
HGNC:6407
ChEMBL ID
CHEMBL2189121

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
OPA-S-S-alkyne
 Probe Info  		K128(1.02)  LDD3494  [2]
Acrolein
 Probe Info  		H94(0.00); H95(0.00)  LDD0227  [3]
DBIA
 Probe Info  		C12(6.66)  LDD0078  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [5]
IPM
 Probe Info  		N.A.  LDD0025  [6]
JW-RF-010
 Probe Info  		C80(0.00); C118(0.00)  LDD0026  [6]
TFBX
 Probe Info  		C118(0.00); C80(0.00)  LDD0027  [6]
WYneN
 Probe Info  		N.A.  LDD0021  [7]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [8]
AOyne
 Probe Info  		15.00  LDD0443  [9]
NAIA_5
 Probe Info  		N.A.  LDD2223  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0020  ARS-1620 HCC44 C12(6.66)  LDD0078  [4]
 LDCM0022  KB02 22RV1 C80(1.21)  LDD2243  [11]
 LDCM0023  KB03 22RV1 C80(1.34)  LDD2660  [11]
 LDCM0024  KB05 HMCB C51(1.75); C80(1.36)  LDD3312  [11]
 LDCM0109  NEM HeLa H94(0.00); H95(0.00)  LDD0227  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
RAF proto-oncogene serine/threonine-protein kinase (RAF1) TKL Ser/Thr protein kinase family P04049
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha (PIP5K1A) . Q99755
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ras association domain-containing protein 2 (RASSF2) . P50749

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adagrasib . DB15568
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mrtx849 Small molecular drug DUQV41
Sotorasib Small molecular drug D0R7LD
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly3499446 Small molecular drug DEXM29
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jnj-74699157 . DZY4R2
Rg6330 . DDZ6B0
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Farnesyl Diphosphate Small molecular drug DB07780
[(3711-trimethyl-dodeca-2610-trienyloxycarbamoyl)-methyl]-phosphonic Acid . DB07771

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
4 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
5 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
6 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
8 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
9 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
10 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
11 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840