Details of the Target

General Information of Target

Target ID LDTP03064
Target Name Cytochrome c oxidase subunit 5A, mitochondrial (COX5A)
Gene Name COX5A
Gene ID 9377
Synonyms
Cytochrome c oxidase subunit 5A, mitochondrial; Cytochrome c oxidase polypeptide Va
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLGAALRRCAVAATTRADPRGLLHSARTPGPAVAIQSVRCYSHGSQETDEEFDARWVTYF
NKPDIDAWELRKGINTLVTYDMVPEPKIIDAALRACRRLNDFASTVRILEVVKDKAGPHK
EIYPYVIQELRPTLNELGISTPEELGLDKV
Target Bioclass
Transporter and channel
Family
Cytochrome c oxidase subunit 5A family
Subcellular location
Mitochondrion inner membrane
Function
Component of the cytochrome c oxidase, the last enzyme in the mitochondrial electron transport chain which drives oxidative phosphorylation. The respiratory chain contains 3 multisubunit complexes succinate dehydrogenase (complex II, CII), ubiquinol-cytochrome c oxidoreductase (cytochrome b-c1 complex, complex III, CIII) and cytochrome c oxidase (complex IV, CIV), that cooperate to transfer electrons derived from NADH and succinate to molecular oxygen, creating an electrochemical gradient over the inner membrane that drives transmembrane transport and the ATP synthase. Cytochrome c oxidase is the component of the respiratory chain that catalyzes the reduction of oxygen to water. Electrons originating from reduced cytochrome c in the intermembrane space (IMS) are transferred via the dinuclear copper A center (CU(A)) of subunit 2 and heme A of subunit 1 to the active site in subunit 1, a binuclear center (BNC) formed by heme A3 and copper B (CU(B)). The BNC reduces molecular oxygen to 2 water molecules using 4 electrons from cytochrome c in the IMS and 4 protons from the mitochondrial matrix.
Uniprot ID
P20674
Ensemble ID
ENST00000322347.11
HGNC ID
HGNC:2267

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
STPyne
 Probe Info  		K113(10.00); K72(1.46); K87(10.00)  LDD0277  [2]
ONAyne
 Probe Info  		K113(0.00); K72(0.00)  LDD0273  [2]
Jackson_14
 Probe Info  		2.78  LDD0123  [3]
HPAP
 Probe Info  		3.96  LDD0064  [4]
HHS-475
 Probe Info  		Y80(1.67)  LDD0264  [5]
5E-2FA
 Probe Info  		N.A.  LDD2235  [6]
m-APA
 Probe Info  		N.A.  LDD2231  [6]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
NHS
 Probe Info  		N.A.  LDD0010  [8]
SF
 Probe Info  		N.A.  LDD0028  [9]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [10]
1c-yne
 Probe Info  		N.A.  LDD0228  [11]
Acrolein
 Probe Info  		N.A.  LDD0217  [12]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [12]
Methacrolein
 Probe Info  		N.A.  LDD0218  [12]
HHS-465
 Probe Info  		Y80(0.00); K87(0.00)  LDD2240  [13]
PAL-AfBPP Probe
Click To Hide/Show 22 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C056
 Probe Info  		17.51  LDD1753  [14]
C107
 Probe Info  		5.62  LDD1794  [14]
C134
 Probe Info  		32.00  LDD1816  [14]
C187
 Probe Info  		26.91  LDD1865  [14]
C216
 Probe Info  		5.74  LDD1890  [14]
C232
 Probe Info  		43.41  LDD1905  [14]
C235
 Probe Info  		22.94  LDD1908  [14]
C278
 Probe Info  		99.73  LDD1948  [14]
C338
 Probe Info  		14.12  LDD2001  [14]
C355
 Probe Info  		24.59  LDD2016  [14]
C378
 Probe Info  		11.79  LDD2037  [14]
C388
 Probe Info  		93.05  LDD2047  [14]
C390
 Probe Info  		76.11  LDD2049  [14]
C403
 Probe Info  		14.72  LDD2061  [14]
C431
 Probe Info  		17.75  LDD2086  [14]
FFF probe11
 Probe Info  		17.82  LDD0471  [15]
FFF probe13
 Probe Info  		20.00  LDD0475  [15]
FFF probe14
 Probe Info  		14.64  LDD0477  [15]
FFF probe2
 Probe Info  		12.94  LDD0463  [15]
FFF probe3
 Probe Info  		19.95  LDD0464  [15]
STS-1
 Probe Info  		N.A.  LDD0137  [16]
LD-F
 Probe Info  		T79(0.00); Y80(0.00)  LDD0015  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [12]
 LDCM0116  HHS-0101 DM93 Y80(1.67)  LDD0264  [5]
 LDCM0117  HHS-0201 DM93 Y80(1.67)  LDD0265  [5]
 LDCM0118  HHS-0301 DM93 Y80(1.71)  LDD0266  [5]
 LDCM0107  IAA HeLa N.A.  LDD0221  [12]
 LDCM0109  NEM HeLa N.A.  LDD0223  [12]
 LDCM0014  Panhematin hPBMC 3.96  LDD0064  [4]
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 2.78  LDD0123  [3]

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
Exosome complex component RRP43 (EXOSC8) RNase PH family Q96B26
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
SAM pointed domain-containing Ets transcription factor (SPDEF) ETS family O95238
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cytoskeletal 40 (KRT40) Intermediate filament family Q6A162
LRP chaperone MESD (MESD) MESD family Q14696

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
Cholic Acid Small molecular drug DB02659
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
N-formylmethionine Small molecular drug DB04464

References

1 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.
2 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
3 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
4 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
5 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.
6 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
7 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
8 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
9 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
10 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
11 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.
12 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.
13 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
14 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
15 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.
16 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.
17 Evaluation of fully-functionalized diazirine tags for chemical proteomic applications. Chem Sci. 2021 May 7;12(22):7839-7847. doi: 10.1039/d1sc01360b.
Mass spectrometry data entry: PXD025652