Details of the Target

General Information of Target

Target ID LDTP04931
Target Name 10 kDa heat shock protein, mitochondrial (HSPE1)
Gene Name HSPE1
Gene ID 3336
Synonyms
10 kDa heat shock protein, mitochondrial; Hsp10; 10 kDa chaperonin; Chaperonin 10; CPN10; Early-pregnancy factor; EPF
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGQAFRKFLPLFDRVLVERSAAETVTKGGIMLPEKSQGKVLQATVVAVGSGSKGKGGEI
QPVSVKVGDKVLLPEYGGTKVVLDDKDYFLFRDGDILGKYVD
Target Type
Clinical trial
Target Bioclass
Other
Family
GroES chaperonin family
Subcellular location
Mitochondrion matrix
Function
Co-chaperonin implicated in mitochondrial protein import and macromolecular assembly. Together with Hsp60, facilitates the correct folding of imported proteins. May also prevent misfolding and promote the refolding and proper assembly of unfolded polypeptides generated under stress conditions in the mitochondrial matrix. The functional units of these chaperonins consist of heptameric rings of the large subunit Hsp60, which function as a back-to-back double ring. In a cyclic reaction, Hsp60 ring complexes bind one unfolded substrate protein per ring, followed by the binding of ATP and association with 2 heptameric rings of the co-chaperonin Hsp10. This leads to sequestration of the substrate protein in the inner cavity of Hsp60 where, for a certain period of time, it can fold undisturbed by other cell components. Synchronous hydrolysis of ATP in all Hsp60 subunits results in the dissociation of the chaperonin rings and the release of ADP and the folded substrate protein (Probable).
TTD ID
T30940
Uniprot ID
P61604
DrugMap ID
TTWYMFE
Ensemble ID
ENST00000233893.10
HGNC ID
HGNC:5269
ChEMBL ID
CHEMBL4106131

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 27 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
P2
 Probe Info  		10.00  LDD0449  [1]
P8
 Probe Info  		10.00  LDD0451  [1]
FBPP2
 Probe Info  		5.87  LDD0318  [2]
C-Sul
 Probe Info  		11.23  LDD0066  [3]
TH211
 Probe Info  		Y76(13.51)  LDD0257  [4]
TH216
 Probe Info  		Y88(10.49)  LDD0259  [4]
YN-1
 Probe Info  		100.00  LDD0444  [5]
AZ-9
 Probe Info  		E75(0.99)  LDD2208  [6]
ONAyne
 Probe Info  		K36(0.00); K28(0.00); K56(0.00); K70(0.00)  LDD0273  [7]
OPA-S-S-alkyne
 Probe Info  		K86(1.85); K8(4.22); K99(4.89)  LDD3494  [8]
Probe 1
 Probe Info  		Y76(8.69); Y88(85.18)  LDD3495  [9]
m-APA
 Probe Info  		6.16  LDD0403  [10]
HHS-482
 Probe Info  		Y76(2.92)  LDD0285  [11]
HHS-475
 Probe Info  		Y76(1.28)  LDD0264  [12]
W1
 Probe Info  		K8(1.78)  LDD0237  [13]
AMP probe
 Probe Info  		K56(0.00); K40(0.00); K86(0.00)  LDD0200  [14]
ATP probe
 Probe Info  		K56(0.00); K40(0.00); K86(0.00); K28(0.00)  LDD0199  [14]
Alkyne tyramide
 Probe Info  		Y76(0.00); Y88(0.00)  LDD0003  [15]
2PCA
 Probe Info  		N.A.  LDD0034  [16]
ATP probe
 Probe Info  		K36(0.00); K8(0.00); K70(0.00); K66(0.00)  LDD0035  [17]
1d-yne
 Probe Info  		N.A.  LDD0356  [18]
NHS
 Probe Info  		K36(0.00); K56(0.00); K70(0.00); K80(0.00)  LDD0010  [15]
OSF
 Probe Info  		N.A.  LDD0029  [19]
SF
 Probe Info  		K56(0.00); K36(0.00); K40(0.00); Y76(0.00)  LDD0028  [19]
STPyne
 Probe Info  		K70(0.00); K54(0.00); K28(0.00); K56(0.00)  LDD0009  [15]
1c-yne
 Probe Info  		K40(0.00); K70(0.00); K66(0.00); K80(0.00)  LDD0228  [18]
HHS-465
 Probe Info  		K36(0.00); K40(0.00); K54(0.00); K56(0.00)  LDD2240  [20]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		9.94  LDD0475  [21]
FFF probe2
 Probe Info  		7.28  LDD0463  [21]
CR-1
 Probe Info  		2.88  LDD0430  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 6.16  LDD0403  [10]
 LDCM0168  Crenolanib MV4-11 2.88  LDD0430  [22]
 LDCM0116  HHS-0101 DM93 Y76(1.28)  LDD0264  [12]
 LDCM0117  HHS-0201 DM93 Y76(0.92)  LDD0265  [12]
 LDCM0118  HHS-0301 DM93 Y76(1.13)  LDD0266  [12]
 LDCM0119  HHS-0401 DM93 Y76(0.82)  LDD0267  [12]
 LDCM0120  HHS-0701 DM93 Y76(1.23)  LDD0268  [12]
 LDCM0123  JWB131 DM93 Y76(2.92)  LDD0285  [11]
 LDCM0124  JWB142 DM93 Y76(3.27)  LDD0286  [11]
 LDCM0125  JWB146 DM93 Y76(2.34)  LDD0287  [11]
 LDCM0126  JWB150 DM93 Y76(8.33)  LDD0288  [11]
 LDCM0127  JWB152 DM93 Y76(7.13)  LDD0289  [11]
 LDCM0128  JWB198 DM93 Y76(2.42)  LDD0290  [11]
 LDCM0129  JWB202 DM93 Y76(3.32)  LDD0291  [11]
 LDCM0130  JWB211 DM93 Y76(2.52)  LDD0292  [11]
 LDCM0110  W12 Hep-G2 K8(1.78)  LDD0237  [13]

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
Protein N-terminal glutamine amidohydrolase (NTAQ1) NTAQ1 family Q96HA8
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Selenoprotein M (SELENOM) Selenoprotein M/F family Q8WWX9

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Xtoll . D0FN4K
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 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 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
3 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
4 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.
5 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.
6 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.
7 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
8 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
9 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.
10 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.
11 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.
12 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.
13 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.
14 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.
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 Unveiling the Multifaceted Capabilities of Endophytic Aspergillus flavus Isolated from Annona squamosa Fruit Peels against Staphylococcus Isolates and HCoV 229E-In Vitro and In Silico Investigations. Pharmaceuticals (Basel). 2024 May 19;17(5):656. doi: 10.3390/ph17050656.
Mass spectrometry data entry: PXD013019
17 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
18 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.
19 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
20 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
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 Crenolanib-Derived Probes Suitable for Cell- and Tissue-Based Protein Profiling and Single-Cell Imaging. Chembiochem. 2019 Jul 15;20(14):1783-1788. doi: 10.1002/cbic.201900067. Epub 2019 Jul 3.