Details of the Target

General Information of Target

Target ID LDTP04999
Target Name Actin, aortic smooth muscle (ACTA2)
Gene Name ACTA2
Gene ID 59
Synonyms
ACTSA; ACTVS; Actin, aortic smooth muscle; EC 3.6.4.-; Alpha-actin-2; Cell growth-inhibiting gene 46 protein) [Cleaved into: Actin, aortic smooth muscle, intermediate form]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MCEEEDSTALVCDNGSGLCKAGFAGDDAPRAVFPSIVGRPRHQGVMVGMGQKDSYVGDEA
QSKRGILTLKYPIEHGIITNWDDMEKIWHHSFYNELRVAPEEHPTLLTEAPLNPKANREK
MTQIMFETFNVPAMYVAIQAVLSLYASGRTTGIVLDSGDGVTHNVPIYEGYALPHAIMRL
DLAGRDLTDYLMKILTERGYSFVTTAEREIVRDIKEKLCYVALDFENEMATAASSSSLEK
SYELPDGQVITIGNERFRCPETLFQPSFIGMESAGIHETTYNSIMKCDIDIRKDLYANNV
LSGGTTMYPGIADRMQKEITALAPSTMKIKIIAPPERKYSVWIGGSILASLSTFQQMWIS
KQEYDEAGPSIVHRKCF
Target Bioclass
Enzyme
Family
Actin family
Subcellular location
Cytoplasm, cytoskeleton
Function Actins are highly conserved proteins that are involved in various types of cell motility and are ubiquitously expressed in all eukaryotic cells.
Uniprot ID
P62736
Ensemble ID
ENST00000224784.10
HGNC ID
HGNC:130

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 18 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		6.40  LDD0402  [1]
Nap-2
 Probe Info  		N.A.  LDD0435  [2]
STPyne
 Probe Info  		K70(9.96)  LDD2217  [3]
Probe 1
 Probe Info  		Y71(27.63)  LDD3495  [4]
DBIA
 Probe Info  		C219(2.42)  LDD3314  [5]
THZ1-DTB
 Probe Info  		C219(1.08)  LDD0460  [6]
HHS-475
 Probe Info  		Y242(0.75); Y55(0.77); Y71(0.92); Y339(1.09)  LDD0264  [7]
IA-alkyne
 Probe Info  		C287(0.37)  LDD2182  [8]
HHS-465
 Probe Info  		Y190(10.00); Y242(10.00); Y55(10.00); Y71(9.20)  LDD2237  [9]
5E-2FA
 Probe Info  		H89(0.00); H90(0.00); H373(0.00); H103(0.00)  LDD2235  [10]
ATP probe
 Probe Info  		K52(0.00); K63(0.00); K330(0.00)  LDD0035  [11]
AZ-9
 Probe Info  		D27(0.00); E243(0.00)  LDD0395  [12]
NAIA_4
 Probe Info  		C219(0.00); C259(0.00)  LDD2226  [13]
1c-yne
 Probe Info  		K293(0.00); K70(0.00); C219(0.00)  LDD0228  [14]
Acrolein
 Probe Info  		C12(0.00); C19(0.00); K20(0.00)  LDD0217  [15]
Methacrolein
 Probe Info  		C19(0.00); K20(0.00)  LDD0218  [15]
AOyne
 Probe Info  		8.30  LDD0443  [16]
NAIA_5
 Probe Info  		C287(0.00); C259(0.00); C219(0.00)  LDD2223  [13]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		5.06  LDD0472  [17]
FFF probe13
 Probe Info  		5.85  LDD0475  [17]
FFF probe14
 Probe Info  		7.95  LDD0477  [17]
JN0003
 Probe Info  		7.95  LDD0469  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 8.42  LDD0403  [1]
 LDCM0625  F8 Ramos C287(0.44)  LDD2187  [8]
 LDCM0572  Fragment10 Ramos C287(0.49)  LDD2189  [8]
 LDCM0573  Fragment11 Ramos C287(0.01)  LDD2190  [8]
 LDCM0574  Fragment12 Ramos C287(0.43)  LDD2191  [8]
 LDCM0575  Fragment13 Ramos C287(0.12)  LDD2192  [8]
 LDCM0576  Fragment14 Ramos C287(0.74)  LDD2193  [8]
 LDCM0579  Fragment20 Ramos C287(0.89)  LDD2194  [8]
 LDCM0580  Fragment21 Ramos C287(0.51)  LDD2195  [8]
 LDCM0582  Fragment23 Ramos C287(0.50)  LDD2196  [8]
 LDCM0578  Fragment27 Ramos C287(0.54)  LDD2197  [8]
 LDCM0586  Fragment28 Ramos C287(0.14)  LDD2198  [8]
 LDCM0588  Fragment30 Ramos C287(0.17)  LDD2199  [8]
 LDCM0589  Fragment31 Ramos C287(0.68)  LDD2200  [8]
 LDCM0590  Fragment32 Ramos C287(0.75)  LDD2201  [8]
 LDCM0468  Fragment33 Ramos C287(0.23)  LDD2202  [8]
 LDCM0596  Fragment38 Ramos C287(0.18)  LDD2203  [8]
 LDCM0566  Fragment4 Ramos C287(0.64)  LDD2184  [8]
 LDCM0610  Fragment52 Ramos C287(0.09)  LDD2204  [8]
 LDCM0614  Fragment56 Ramos C287(0.35)  LDD2205  [8]
 LDCM0569  Fragment7 Ramos C287(0.61)  LDD2186  [8]
 LDCM0571  Fragment9 Ramos C287(0.50)  LDD2188  [8]
 LDCM0116  HHS-0101 DM93 Y242(0.75); Y55(0.77); Y71(0.92); Y339(1.09)  LDD0264  [7]
 LDCM0117  HHS-0201 DM93 Y339(0.60); Y242(0.62); Y55(0.67); Y71(0.87)  LDD0265  [7]
 LDCM0118  HHS-0301 DM93 Y55(0.71); Y71(0.85); Y190(1.11); Y242(1.16)  LDD0266  [7]
 LDCM0119  HHS-0401 DM93 Y339(0.63); Y242(0.73); Y55(0.75); Y71(0.97)  LDD0267  [7]
 LDCM0120  HHS-0701 DM93 Y242(0.52); Y55(0.71); Y71(0.72); Y190(1.00)  LDD0268  [7]
 LDCM0022  KB02 Ramos C287(0.37)  LDD2182  [8]
 LDCM0023  KB03 Ramos C287(0.35)  LDD2183  [8]
 LDCM0024  KB05 IGR37 C219(2.42)  LDD3314  [5]
 LDCM0109  NEM HeLa N.A.  LDD0223  [15]
 LDCM0021  THZ1 HeLa S3 C219(1.08)  LDD0460  [6]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Phenethyl Isothiocyanate Small molecular drug DB12695

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 Proteome-Wide Identification of On- and Off-Targets of Bcl-2 Inhibitors in Native Biological Systems by Using Affinity-Based Probes (AfBPs). Chembiochem. 2018 Nov 2;19(21):2312-2320. doi: 10.1002/cbic.201800380. Epub 2018 Oct 18.
3 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
4 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
5 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
6 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
7 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
8 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
9 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.
10 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
11 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
12 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.
13 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
14 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
15 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.
16 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.
17 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.