Details of the Target

General Information of Target

Target ID LDTP04263
Target Name Cysteine--tRNA ligase, cytoplasmic (CARS1)
Gene Name CARS1
Gene ID 833
Synonyms
CARS; Cysteine--tRNA ligase, cytoplasmic; EC 6.1.1.16; Cysteinyl-tRNA synthetase; CysRS
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MADSSGQQGKGRRVQPQWSPPAGTQPCRLHLYNSLTRNKEVFIPQDGKKVTWYCCGPTVY
DASHMGHARSYISFDILRRVLKDYFKFDVFYCMNITDIDDKIIKRARQNHLFEQYREKRP
EAAQLLEDVQAALKPFSVKLNETTDPDKKQMLERIQHAVQLATEPLEKAVQSRLTGEEVN
SCVEVLLEEAKDLLSDWLDSTLGCDVTDNSIFSKLPKFWEGDFHRDMEALNVLPPDVLTR
VSEYVPEIVNFVQKIVDNGYGYVSNGSVYFDTAKFASSEKHSYGKLVPEAVGDQKALQEG
EGDLSISADRLSEKRSPNDFALWKASKPGEPSWPCPWGKGRPGWHIECSAMAGTLLGASM
DIHGGGFDLRFPHHDNELAQSEAYFENDCWVRYFLHTGHLTIAGCKMSKSLKNFITIKDA
LKKHSARQLRLAFLMHSWKDTLDYSSNTMESALQYEKFLNEFFLNVKDILRAPVDITGQF
EKWGEEEAELNKNFYDKKTAIHKALCDNVDTRTVMEEMRALVSQCNLYMAARKAVRKRPN
QALLENIALYLTHMLKIFGAVEEDSSLGFPVGGPGTSLSLEATVMPYLQVLSEFREGVRK
IAREQKVPEILQLSDALRDNILPELGVRFEDHEGLPTVVKLVDRNTLLKEREEKRRVEEE
KRKKKEEAARRKQEQEAAKLAKMKIPPSEMFLSETDKYSKFDENGLPTHDMEGKELSKGQ
AKKLKKLFEAQEKLYKEYLQMAQNGSFQ
Target Bioclass
Enzyme
Family
Class-I aminoacyl-tRNA synthetase family
Subcellular location
Cytoplasm
Function Catalyzes the ATP-dependent ligation of cysteine to tRNA(Cys).
Uniprot ID
P49589
Ensemble ID
ENST00000278224.13
HGNC ID
HGNC:1493
ChEMBL ID
CHEMBL4105937

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 32 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		14.66  LDD0402  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
N1
 Probe Info  		100.00  LDD0242  [2]
TH211
 Probe Info  		Y60(20.00)  LDD0257  [3]
YN-1
 Probe Info  		100.00  LDD0444  [4]
STPyne
 Probe Info  		K280(10.00); K39(6.20); K412(7.34); K48(5.56)  LDD0277  [5]
DBIA
 Probe Info  		C589(1.99); C608(2.64); C27(1.89)  LDD3311  [6]
BTD
 Probe Info  		C506(0.83); C525(0.68)  LDD2089  [7]
Sulforaphane-probe2
 Probe Info  		1.72  LDD0160  [8]
AHL-Pu-1
 Probe Info  		C335(2.41)  LDD0170  [9]
HHS-482
 Probe Info  		Y53(1.20)  LDD0285  [10]
HHS-465
 Probe Info  		Y60(10.00)  LDD2237  [11]
ATP probe
 Probe Info  		K148(0.00); K149(0.00); K503(0.00)  LDD0199  [12]
4-Iodoacetamidophenylacetylene
 Probe Info  		C506(0.00); C525(0.00); C335(0.00); C204(0.00)  LDD0038  [13]
IA-alkyne
 Probe Info  		C506(0.00); C525(0.00); C335(0.00); C204(0.00)  LDD0036  [13]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [14]
Lodoacetamide azide
 Probe Info  		C506(0.00); C525(0.00); C335(0.00); C204(0.00)  LDD0037  [13]
WYneN
 Probe Info  		N.A.  LDD0021  [15]
WYneO
 Probe Info  		N.A.  LDD0022  [15]
Compound 10
 Probe Info  		C27(0.00); C335(0.00)  LDD2216  [16]
Compound 11
 Probe Info  		N.A.  LDD2213  [16]
ENE
 Probe Info  		N.A.  LDD0006  [15]
IPM
 Probe Info  		N.A.  LDD0005  [15]
NHS
 Probe Info  		N.A.  LDD0010  [15]
VSF
 Probe Info  		N.A.  LDD0007  [15]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [17]
Ox-W18
 Probe Info  		N.A.  LDD2175  [18]
Acrolein
 Probe Info  		C182(0.00); C405(0.00); C506(0.00); H157(0.00)  LDD0217  [19]
Methacrolein
 Probe Info  		C506(0.00); C27(0.00)  LDD0218  [19]
W1
 Probe Info  		N.A.  LDD0236  [20]
AOyne
 Probe Info  		10.90  LDD0443  [21]
NAIA_5
 Probe Info  		C525(0.00); C335(0.00); C92(0.00); C506(0.00)  LDD2223  [22]
PAL-AfBPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C056
 Probe Info  		16.11  LDD1753  [23]
C072
 Probe Info  		22.01  LDD1768  [23]
C112
 Probe Info  		18.25  LDD1799  [23]
C161
 Probe Info  		10.13  LDD1841  [23]
C210
 Probe Info  		51.98  LDD1884  [23]
FFF probe3
 Probe Info  		6.79  LDD0465  [24]
FFF probe4
 Probe Info  		18.26  LDD0466  [24]
JN0003
 Probe Info  		12.02  LDD0469  [24]
STS-2
 Probe Info  		N.A.  LDD0139  [25]
DA-2
 Probe Info  		N.A.  LDD0070  [26]
STS-1
 Probe Info  		N.A.  LDD0068  [27]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C525(0.75)  LDD2130  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C525(0.91)  LDD2117  [7]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C506(2.24); C525(0.96)  LDD2152  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C335(0.73)  LDD2132  [7]
 LDCM0025  4SU-RNA DM93 C335(2.41)  LDD0170  [9]
 LDCM0545  Acetamide MDA-MB-231 C525(0.70)  LDD2138  [7]
 LDCM0156  Aniline NCI-H1299 C27(0.00); C204(0.00)  LDD0404  [1]
 LDCM0108  Chloroacetamide HeLa H157(0.00); C506(0.00); C405(0.00)  LDD0222  [19]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C27(2.28); C182(1.28)  LDD1702  [7]
 LDCM0625  F8 Ramos C27(1.53)  LDD2187  [28]
 LDCM0572  Fragment10 Ramos C27(0.89)  LDD2189  [28]
 LDCM0573  Fragment11 Ramos C27(0.09)  LDD2190  [28]
 LDCM0574  Fragment12 Ramos C27(0.22)  LDD2191  [28]
 LDCM0575  Fragment13 Ramos C27(0.52)  LDD2192  [28]
 LDCM0576  Fragment14 Ramos C27(0.73)  LDD2193  [28]
 LDCM0579  Fragment20 Ramos C27(0.33)  LDD2194  [28]
 LDCM0580  Fragment21 Ramos C27(0.77)  LDD2195  [28]
 LDCM0582  Fragment23 Ramos C27(0.24)  LDD2196  [28]
 LDCM0578  Fragment27 Ramos C27(0.57)  LDD2197  [28]
 LDCM0586  Fragment28 Ramos C27(0.30)  LDD2198  [28]
 LDCM0588  Fragment30 Ramos C27(0.67)  LDD2199  [28]
 LDCM0589  Fragment31 Ramos C27(0.43)  LDD2200  [28]
 LDCM0590  Fragment32 Ramos C27(0.29)  LDD2201  [28]
 LDCM0468  Fragment33 Ramos C27(1.17)  LDD2202  [28]
 LDCM0596  Fragment38 Ramos C27(0.46)  LDD2203  [28]
 LDCM0566  Fragment4 Ramos C27(0.74)  LDD2184  [28]
 LDCM0610  Fragment52 Ramos C27(0.52)  LDD2204  [28]
 LDCM0614  Fragment56 Ramos C27(0.79)  LDD2205  [28]
 LDCM0569  Fragment7 Ramos C27(0.85)  LDD2186  [28]
 LDCM0571  Fragment9 Ramos C27(0.34)  LDD2188  [28]
 LDCM0107  IAA HeLa H157(0.00); C506(0.00)  LDD0221  [19]
 LDCM0123  JWB131 DM93 Y53(1.20)  LDD0285  [10]
 LDCM0124  JWB142 DM93 Y53(0.50)  LDD0286  [10]
 LDCM0125  JWB146 DM93 Y53(2.12)  LDD0287  [10]
 LDCM0126  JWB150 DM93 Y53(1.59)  LDD0288  [10]
 LDCM0127  JWB152 DM93 Y53(1.16)  LDD0289  [10]
 LDCM0128  JWB198 DM93 Y53(0.74)  LDD0290  [10]
 LDCM0130  JWB211 DM93 Y53(0.77)  LDD0292  [10]
 LDCM0022  KB02 HEK-293T C27(1.05); C405(0.97); C389(1.10); C335(0.87)  LDD1492  [29]
 LDCM0023  KB03 Jurkat C525(4.13)  LDD0315  [30]
 LDCM0024  KB05 G361 C589(1.99); C608(2.64); C27(1.89)  LDD3311  [6]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C525(0.57)  LDD2121  [7]
 LDCM0109  NEM HeLa H157(0.00); H224(0.00)  LDD0223  [19]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C506(0.83); C525(0.68)  LDD2089  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C506(5.44)  LDD2093  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C525(0.88)  LDD2099  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C525(0.91)  LDD2107  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C27(0.70); C525(0.73)  LDD2109  [7]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C525(1.04)  LDD2111  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C525(1.67)  LDD2119  [7]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C525(1.02)  LDD2122  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C525(0.92)  LDD2123  [7]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C525(1.29)  LDD2124  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C525(0.96)  LDD2125  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C525(1.01)  LDD2127  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C506(6.03); C27(0.97); C525(0.95)  LDD2129  [7]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C525(0.96)  LDD2134  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C27(1.07)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C525(1.10)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C27(0.99); C525(0.95)  LDD2137  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C525(0.83)  LDD2140  [7]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C525(1.67)  LDD2144  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C525(0.94)  LDD2146  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C506(0.44); C525(0.56); C335(0.46)  LDD2150  [7]
 LDCM0627  NUDT7-COV-1 HEK-293T C27(0.86); C27(0.85)  LDD2206  [31]
 LDCM0628  OTUB2-COV-1 HEK-293T C27(0.56); C27(0.35)  LDD2207  [31]
 LDCM0131  RA190 MM1.R C27(1.15)  LDD0304  [32]
 LDCM0003  Sulforaphane MDA-MB-231 1.72  LDD0160  [8]
 LDCM0112  W16 Hep-G2 C27(0.74)  LDD0239  [20]

The Interaction Atlas With This Target

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
Cysteine Small molecular drug DB00151

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 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.
3 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
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 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
7 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
8 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
9 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
10 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
11 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.
12 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
13 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
14 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
15 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
16 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
17 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
18 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
19 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.
20 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.
21 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.
22 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
23 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
24 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
25 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.
26 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
27 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
28 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
29 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
30 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
31 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
32 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.