Details of the Target

General Information of Target

Target ID LDTP02037
Target Name Tubulin beta-4A chain (TUBB4A)
Gene Name TUBB4A
Gene ID 10382
Synonyms
TUBB4; TUBB5; Tubulin beta-4A chain; Tubulin 5 beta; Tubulin beta-4 chain
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MREIVHLQAGQCGNQIGAKFWEVISDEHGIDPTGTYHGDSDLQLERINVYYNEATGGNYV
PRAVLVDLEPGTMDSVRSGPFGQIFRPDNFVFGQSGAGNNWAKGHYTEGAELVDAVLDVV
RKEAESCDCLQGFQLTHSLGGGTGSGMGTLLISKIREEFPDRIMNTFSVVPSPKVSDTVV
EPYNATLSVHQLVENTDETYCIDNEALYDICFRTLKLTTPTYGDLNHLVSATMSGVTTCL
RFPGQLNADLRKLAVNMVPFPRLHFFMPGFAPLTSRGSQQYRALTVPELTQQMFDAKNMM
AACDPRHGRYLTVAAVFRGRMSMKEVDEQMLSVQSKNSSYFVEWIPNNVKTAVCDIPPRG
LKMAATFIGNSTAIQELFKRISEQFTAMFRRKAFLHWYTGEGMDEMEFTEAESNMNDLVS
EYQQYQDATAEEGEFEEEAEEEVA
Target Bioclass
Other
Family
Tubulin family
Subcellular location
Cytoplasm, cytoskeleton
Function
Tubulin is the major constituent of microtubules, a cylinder consisting of laterally associated linear protofilaments composed of alpha- and beta-tubulin heterodimers. Microtubules grow by the addition of GTP-tubulin dimers to the microtubule end, where a stabilizing cap forms. Below the cap, tubulin dimers are in GDP-bound state, owing to GTPase activity of alpha-tubulin.
Uniprot ID
P04350
Ensemble ID
ENST00000264071.7
HGNC ID
HGNC:20774
ChEMBL ID
CHEMBL3838

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 23 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y106(20.00); Y50(20.00); Y59(20.00); Y51(11.40)  LDD0257  [1]
TH214
 Probe Info  		Y59(20.00); Y106(16.94)  LDD0258  [1]
TH216
 Probe Info  		Y106(20.00); Y50(20.00); Y59(20.00); Y51(7.25)  LDD0259  [1]
AZ-9
 Probe Info  		E383(0.90)  LDD2208  [2]
Probe 1
 Probe Info  		Y36(10.21)  LDD3495  [3]
THZ1-DTB
 Probe Info  		C239(1.11); C211(1.04); C239(0.99); C201(1.03)  LDD0460  [4]
AHL-Pu-1
 Probe Info  		C129(2.47); C303(2.15)  LDD0168  [5]
HPAP
 Probe Info  		5.81  LDD0062  [6]
HHS-482
 Probe Info  		Y106(0.89); Y50(0.86); Y51(0.87); Y59(0.79)  LDD0285  [7]
HHS-475
 Probe Info  		Y222(0.69); Y310(0.76); Y281(0.79); Y36(0.83)  LDD0264  [8]
HHS-465
 Probe Info  		Y106(9.01); Y183(10.00); Y200(3.29); Y208(10.00)  LDD2237  [9]
5E-2FA
 Probe Info  		H6(0.00); H227(0.00)  LDD2235  [10]
m-APA
 Probe Info  		H6(0.00); H28(0.00); H227(0.00)  LDD2231  [10]
N1
 Probe Info  		C239(0.00); C303(0.00); C354(0.00); D224(0.00)  LDD0245  [11]
IA-alkyne
 Probe Info  		C127(0.00); C239(0.00); C201(0.00); C354(0.00)  LDD0032  [12]
IPIAA_H
 Probe Info  		C239(0.00); C127(0.00); C303(0.00)  LDD0030  [13]
IPIAA_L
 Probe Info  		C127(0.00); C354(0.00); C239(0.00); C303(0.00)  LDD0031  [13]
JW-RF-010
 Probe Info  		C129(0.00); C127(0.00); C354(0.00); C201(0.00)  LDD0026  [14]
SF
 Probe Info  		Y310(0.00); Y340(0.00); K252(0.00); Y222(0.00)  LDD0028  [15]
VSF
 Probe Info  		C239(0.00); C127(0.00); C129(0.00)  LDD0007  [16]
Ox-W18
 Probe Info  		N.A.  LDD2175  [17]
Acrolein
 Probe Info  		H28(0.00); H37(0.00)  LDD0217  [18]
NAIA_5
 Probe Info  		C303(0.00); C12(0.00); C239(0.00)  LDD2223  [19]
PAL-AfBPP Probe
Click To Hide/Show 23 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C049
 Probe Info  		8.06  LDD1747  [20]
C153
 Probe Info  		15.24  LDD1834  [20]
C159
 Probe Info  		23.75  LDD1839  [20]
C160
 Probe Info  		7.52  LDD1840  [20]
C198
 Probe Info  		41.64  LDD1874  [20]
C213
 Probe Info  		19.56  LDD1887  [20]
C255
 Probe Info  		5.24  LDD1928  [20]
C264
 Probe Info  		53.82  LDD1935  [20]
C270
 Probe Info  		6.96  LDD1940  [20]
C287
 Probe Info  		17.51  LDD1957  [20]
C349
 Probe Info  		9.71  LDD2010  [20]
C363
 Probe Info  		17.15  LDD2024  [20]
C382
 Probe Info  		21.86  LDD2041  [20]
C413
 Probe Info  		11.71  LDD2069  [20]
FFF probe11
 Probe Info  		17.78  LDD0472  [21]
FFF probe13
 Probe Info  		16.59  LDD0476  [21]
FFF probe3
 Probe Info  		20.00  LDD0465  [21]
FFF probe6
 Probe Info  		8.45  LDD0468  [21]
Alk-rapa
 Probe Info  		3.07  LDD0213  [22]
Photocelecoxib
 Probe Info  		E123(0.00); S138(0.00)  LDD0019  [23]
Photonaproxen
 Probe Info  		T218(0.00); S230(0.00); T219(0.00)  LDD0157  [23]
DA-2
 Probe Info  		N.A.  LDD0070  [24]
STS-1
 Probe Info  		N.A.  LDD0068  [25]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C129(2.47); C303(2.15)  LDD0168  [5]
 LDCM0108  Chloroacetamide HeLa H28(0.00); H37(0.00)  LDD0222  [18]
 LDCM0116  HHS-0101 DM93 Y222(0.69); Y310(0.76); Y281(0.79); Y36(0.83)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y222(0.59); Y310(0.74); Y281(0.80); Y340(0.92)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y222(0.62); Y310(0.75); Y281(0.85); Y340(0.89)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y222(0.63); Y310(0.74); Y281(0.91); Y36(1.03)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y222(0.63); Y36(0.74); Y281(0.76); Y310(0.78)  LDD0268  [8]
 LDCM0107  IAA HeLa H28(0.00); H37(0.00)  LDD0221  [18]
 LDCM0123  JWB131 DM93 Y106(0.89); Y50(0.86); Y51(0.87); Y59(0.79)  LDD0285  [7]
 LDCM0124  JWB142 DM93 Y106(0.57); Y50(0.61); Y51(1.32); Y59(0.53)  LDD0286  [7]
 LDCM0125  JWB146 DM93 Y106(1.05); Y50(1.07); Y51(1.87); Y59(1.25)  LDD0287  [7]
 LDCM0126  JWB150 DM93 Y106(2.48); Y50(3.41); Y51(2.57); Y59(2.36)  LDD0288  [7]
 LDCM0127  JWB152 DM93 Y106(1.69); Y50(2.02); Y51(1.80); Y59(1.63)  LDD0289  [7]
 LDCM0128  JWB198 DM93 Y106(0.93); Y50(0.95); Y51(1.01); Y59(1.15)  LDD0290  [7]
 LDCM0129  JWB202 DM93 Y106(0.34); Y50(0.36); Y51(0.46); Y59(0.44)  LDD0291  [7]
 LDCM0130  JWB211 DM93 Y106(0.87); Y50(1.07); Y51(0.92); Y59(0.92)  LDD0292  [7]
 LDCM0109  NEM HeLa H37(0.00); H28(0.00)  LDD0223  [18]
 LDCM0014  Panhematin HEK-293T 5.81  LDD0062  [6]
 LDCM0090  Rapamycin JHH-7 3.07  LDD0213  [22]
 LDCM0021  THZ1 HeLa S3 C239(1.11); C211(1.04); C239(0.99); C201(1.03)  LDD0460  [4]

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
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear receptor subfamily 4immunitygroup A member 1 (NR4A1) Nuclear hormone receptor family P22736

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
Artenimol . DB11638
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Epothilone D Small molecular drug DB01873
Patupilone Small molecular drug DB03010
Cyt997 . DB05147
Zen-012 . DB06042

References

1 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.
2 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.
3 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.
4 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.
5 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
6 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
7 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.
8 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.
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 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.
12 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
13 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
14 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
15 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
16 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
17 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
18 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.
19 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
20 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
21 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.
22 Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth. Cell Chem Biol. 2022 Mar 17;29(3):373-385.e6. doi: 10.1016/j.chembiol.2021.10.006. Epub 2021 Oct 26.
23 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
24 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.
25 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.