Details of the Target

General Information of Target

Target ID LDTP02125
Target Name Keratin, type II cytoskeletal 8 (KRT8)
Gene Name KRT8
Gene ID 3856
Synonyms
CYK8; Keratin, type II cytoskeletal 8; Cytokeratin-8; CK-8; Keratin-8; K8; Type-II keratin Kb8
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSIRVTQKSYKVSTSGPRAFSSRSYTSGPGSRISSSSFSRVGSSNFRGGLGGGYGGASGM
GGITAVTVNQSLLSPLVLEVDPNIQAVRTQEKEQIKTLNNKFASFIDKVRFLEQQNKMLE
TKWSLLQQQKTARSNMDNMFESYINNLRRQLETLGQEKLKLEAELGNMQGLVEDFKNKYE
DEINKRTEMENEFVLIKKDVDEAYMNKVELESRLEGLTDEINFLRQLYEEEIRELQSQIS
DTSVVLSMDNSRSLDMDSIIAEVKAQYEDIANRSRAEAESMYQIKYEELQSLAGKHGDDL
RRTKTEISEMNRNISRLQAEIEGLKGQRASLEAAIADAEQRGELAIKDANAKLSELEAAL
QRAKQDMARQLREYQELMNVKLALDIEIATYRKLLEGEESRLESGMQNMSIHTKTTSGYA
GGLSSAYGGLTSPGLSYSLGSSFGSGAGSSSFSRTSSSRAVVVKKIETRDGKLVSESSDV
LPK
Target Bioclass
Other
Family
Intermediate filament family
Subcellular location
Cytoplasm
Function Together with KRT19, helps to link the contractile apparatus to dystrophin at the costameres of striated muscle.
Uniprot ID
P05787
Ensemble ID
ENST00000293308.11
HGNC ID
HGNC:6446

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 Deletion: p.N146del .
HUCCT1 Deletion: p.N100del .
LS180 SNV: p.R252H .
MFE319 SNV: p.Y204C; p.D479N .
MKN45 Deletion: p.F443_S450del .
SNU1 SNV: p.I106T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 22 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
P1
 Probe Info  		10.00  LDD0452  [1]
P2
 Probe Info  		7.33  LDD0449  [1]
P3
 Probe Info  		10.00  LDD0454  [1]
P8
 Probe Info  		10.00  LDD0451  [1]
A-EBA
 Probe Info  		3.74  LDD0215  [2]
AZ-9
 Probe Info  		4.64  LDD0393  [3]
YN-1
 Probe Info  		10.77  LDD0444  [4]
YN-4
 Probe Info  		100.00  LDD0445  [4]
ONAyne
 Probe Info  		K11(0.70); K117(0.79); K122(0.89); K130(0.57)  LDD0274  [5]
STPyne
 Probe Info  		K11(8.38); K117(8.22); K122(6.69); K130(6.87)  LDD0277  [5]
OPA-S-S-alkyne
 Probe Info  		K483(2.46); K472(2.67); K207(3.47); K8(5.03)  LDD3494  [6]
5E-2FA
 Probe Info  		H412(0.00); H296(0.00)  LDD2235  [7]
m-APA
 Probe Info  		H412(0.00); H296(0.00)  LDD2231  [7]
CY-1
 Probe Info  		D107(0.00); E120(0.00); M118(0.00); S124(0.00)  LDD0246  [8]
ATP probe
 Probe Info  		K122(0.00); K92(0.00); K325(0.00); K8(0.00)  LDD0035  [9]
Acrolein
 Probe Info  		H412(0.00); H296(0.00)  LDD0217  [10]
Crotonaldehyde
 Probe Info  		H412(0.00); H296(0.00)  LDD0219  [10]
Methacrolein
 Probe Info  		H412(0.00); H296(0.00)  LDD0218  [10]
W1
 Probe Info  		K122(0.00); E120(0.00); N100(0.00); Q90(0.00)  LDD0236  [11]
HHS-465
 Probe Info  		Y427(0.00); Y54(0.00); Y25(0.00); Y286(0.00)  LDD2240  [12]
HHS-475
 Probe Info  		Y10(1.21); Y204(1.56); Y25(0.86); Y267(0.57)  LDD2238  [13]
HHS-482
 Probe Info  		Y10(0.68); Y143(0.62); Y204(0.67); Y25(0.49)  LDD2239  [13]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DR-1
 Probe Info  		3.25  LDD0398  [14]
STS-2
 Probe Info  		N.A.  LDD0139  [15]
Kambe_22
 Probe Info  		2.25  LDD0132  [16]
Photocelecoxib
 Probe Info  		L217(0.00); N222(0.00)  LDD0153  [17]
Photonaproxen
 Probe Info  		L214(0.00); E220(0.00); L356(0.00)  LDD0156  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0151  AZ-11 HeLa 10.00  LDD2154  [3]
 LDCM0108  Chloroacetamide HeLa H412(0.00); H296(0.00)  LDD0222  [10]
 LDCM0107  IAA HeLa H412(0.00); H296(0.00)  LDD0221  [10]
 LDCM0076  kambe_cp71 PC-3 2.25  LDD0132  [16]
 LDCM0109  NEM HeLa H412(0.00); H296(0.00)  LDD0223  [10]
 LDCM0112  W16 Hep-G2 Q365(0.53)  LDD0239  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cystic fibrosis transmembrane conductance regulator (CFTR) ABCC family P13569
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leukocyte immunoglobulin-like receptor subfamily B member 3 (LILRB3) . O75022
Other
Click To Hide/Show 18 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cuticular Ha3-II (KRT33B) Intermediate filament family Q14525
Keratin, type I cuticular Ha4 (KRT34) Intermediate filament family O76011
Keratin, type I cuticular Ha5 (KRT35) Intermediate filament family Q92764
Keratin, type I cuticular Ha8 (KRT38) Intermediate filament family O76015
Keratin, type I cytoskeletal 15 (KRT15) Intermediate filament family P19012
Keratin, type I cytoskeletal 16 (KRT16) Intermediate filament family P08779
Keratin, type I cytoskeletal 18 (KRT18) Intermediate filament family P05783
Keratin, type I cytoskeletal 19 (KRT19) Intermediate filament family P08727
Keratin, type I cytoskeletal 24 (KRT24) Intermediate filament family Q2M2I5
Keratin, type I cytoskeletal 25 (KRT25) Intermediate filament family Q7Z3Z0
Keratin, type I cytoskeletal 27 (KRT27) Intermediate filament family Q7Z3Y8
Keratin, type I cytoskeletal 28 (KRT28) Intermediate filament family Q7Z3Y7
Keratin, type I cytoskeletal 40 (KRT40) Intermediate filament family Q6A162
Vimentin (VIM) Intermediate filament family P08670
Tuftelin-interacting protein 11 (TFIP11) TFP11/STIP family Q9UBB9
NF-kappa-B essential modulator (IKBKG) . Q9Y6K9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tenecteplase BiotechDrug DB00031
Copper . DB09130
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lanoteplase . DB06245

References

1 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
2 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
3 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
4 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.
5 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
6 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
7 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
8 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
9 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
10 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.
11 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
12 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
13 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
14 Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor. ACS Med Chem Lett. 2020 Feb 5;11(4):535-540. doi: 10.1021/acsmedchemlett.9b00658. eCollection 2020 Apr 9.
15 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
16 Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells. J Am Chem Soc. 2014 Jul 30;136(30):10777-82. doi: 10.1021/ja505517t. Epub 2014 Jul 21.
17 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094