Details of the Target

General Information of Target

Target ID LDTP11869
Target Name Growth hormone-inducible transmembrane protein (GHITM)
Gene Name GHITM
Gene ID 27069
Synonyms
DERP2; MICS1; TMBIM5; Growth hormone-inducible transmembrane protein; Dermal papilla-derived protein 2; Mitochondrial morphology and cristae structure 1; MICS1; Transmembrane BAX inhibitor motif-containing protein 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTVGLFHFPTPLTRICPAPWGLRLWEKLTLLSPGIAVTPVQMAGKKDYPALLSLDENEL
EEQFVKGHGPGGQATNKTSNCVVLKHIPSGIVVKCHQTRSVDQNRKLARKILQEKVDVFY
NGENSPVHKEKREAAKKKQERKKRAKETLEKKKLLKELWESSKKVH
Target Bioclass
Transporter and channel
Family
BI1 family
Subcellular location
Mitochondrion inner membrane
Function
Plays an important role in maintenance of mitochondrial morphology and in mediating either calcium or potassium/proton antiport. Mediates proton-dependent calcium efflux from mitochondrion. Functions also as an electroneutral mitochondrial proton/potassium exchanger. Required for the mitochondrial tubular network and cristae organization. Involved in apoptotic release of cytochrome c. Inhibits the proteolytic activity of AFG3L2, stimulating respiration and stabilizing respiratory enzymes in actively respiring mitochondria. However, when mitochondria become hyperpolarized, GHITM loses its inhibitory activity toward AFG3L2 and the now the active AFG3L2 turns first on GHITM and, if hyperpolarization persists, on other proteins of the mitochondria, leading to a broad remodeling of the mitochondrial proteome.
Uniprot ID
Q9H3K2
Ensemble ID
ENST00000372134.6
HGNC ID
HGNC:17281

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
IA-alkyne
 Probe Info  		C235(2.51)  LDD2157  [2]
OPA-S-S-alkyne
 Probe Info  		K76(4.44)  LDD3494  [3]
DBIA
 Probe Info  		C235(2.69)  LDD3338  [4]
Jackson_14
 Probe Info  		2.22  LDD0123  [5]
HPAP
 Probe Info  		3.32  LDD0062  [6]
NHS
 Probe Info  		N.A.  LDD0010  [7]
SF
 Probe Info  		N.A.  LDD0028  [8]
STPyne
 Probe Info  		N.A.  LDD0009  [7]
1c-yne
 Probe Info  		N.A.  LDD0228  [9]
AOyne
 Probe Info  		15.00  LDD0443  [10]
PAL-AfBPP Probe
Click To Hide/Show 71 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C022
 Probe Info  		8.88  LDD1728  [11]
C040
 Probe Info  		11.47  LDD1740  [11]
C055
 Probe Info  		17.75  LDD1752  [11]
C056
 Probe Info  		32.22  LDD1753  [11]
C063
 Probe Info  		12.04  LDD1760  [11]
C091
 Probe Info  		13.83  LDD1782  [11]
C092
 Probe Info  		27.28  LDD1783  [11]
C094
 Probe Info  		46.21  LDD1785  [11]
C106
 Probe Info  		19.70  LDD1793  [11]
C112
 Probe Info  		22.78  LDD1799  [11]
C134
 Probe Info  		22.16  LDD1816  [11]
C143
 Probe Info  		14.32  LDD1825  [11]
C153
 Probe Info  		18.64  LDD1834  [11]
C161
 Probe Info  		11.71  LDD1841  [11]
C163
 Probe Info  		5.98  LDD1843  [11]
C169
 Probe Info  		22.63  LDD1849  [11]
C186
 Probe Info  		9.25  LDD1864  [11]
C194
 Probe Info  		10.63  LDD1870  [11]
C196
 Probe Info  		11.08  LDD1872  [11]
C198
 Probe Info  		10.20  LDD1874  [11]
C201
 Probe Info  		35.26  LDD1877  [11]
C210
 Probe Info  		42.81  LDD1884  [11]
C218
 Probe Info  		17.88  LDD1892  [11]
C219
 Probe Info  		6.06  LDD1893  [11]
C220
 Probe Info  		25.28  LDD1894  [11]
C228
 Probe Info  		18.51  LDD1901  [11]
C231
 Probe Info  		33.36  LDD1904  [11]
C232
 Probe Info  		54.19  LDD1905  [11]
C233
 Probe Info  		10.85  LDD1906  [11]
C234
 Probe Info  		5.78  LDD1907  [11]
C235
 Probe Info  		39.12  LDD1908  [11]
C238
 Probe Info  		11.71  LDD1911  [11]
C243
 Probe Info  		11.39  LDD1916  [11]
C246
 Probe Info  		20.68  LDD1919  [11]
C264
 Probe Info  		18.00  LDD1935  [11]
C277
 Probe Info  		8.17  LDD1947  [11]
C278
 Probe Info  		92.41  LDD1948  [11]
C280
 Probe Info  		10.06  LDD1950  [11]
C282
 Probe Info  		24.76  LDD1952  [11]
C285
 Probe Info  		38.59  LDD1955  [11]
C286
 Probe Info  		5.39  LDD1956  [11]
C287
 Probe Info  		19.43  LDD1957  [11]
C288
 Probe Info  		11.79  LDD1958  [11]
C289
 Probe Info  		87.43  LDD1959  [11]
C290
 Probe Info  		5.17  LDD1960  [11]
C293
 Probe Info  		25.63  LDD1963  [11]
C296
 Probe Info  		14.52  LDD1966  [11]
C299
 Probe Info  		6.63  LDD1968  [11]
C307
 Probe Info  		5.06  LDD1975  [11]
C310
 Probe Info  		12.13  LDD1977  [11]
C314
 Probe Info  		11.71  LDD1981  [11]
C343
 Probe Info  		15.56  LDD2005  [11]
C348
 Probe Info  		10.85  LDD2009  [11]
C349
 Probe Info  		15.35  LDD2010  [11]
C350
 Probe Info  		48.17  LDD2011  [11]
C362
 Probe Info  		99.73  LDD2023  [11]
C363
 Probe Info  		45.25  LDD2024  [11]
C364
 Probe Info  		50.21  LDD2025  [11]
C366
 Probe Info  		16.80  LDD2027  [11]
C367
 Probe Info  		11.96  LDD2028  [11]
C388
 Probe Info  		52.71  LDD2047  [11]
C390
 Probe Info  		21.86  LDD2049  [11]
C407
 Probe Info  		12.30  LDD2064  [11]
C413
 Probe Info  		11.96  LDD2069  [11]
FFF probe11
 Probe Info  		15.93  LDD0471  [12]
FFF probe13
 Probe Info  		20.00  LDD0475  [12]
FFF probe14
 Probe Info  		20.00  LDD0477  [12]
FFF probe2
 Probe Info  		20.00  LDD0463  [12]
JN0003
 Probe Info  		20.00  LDD0469  [12]
VE-P
 Probe Info  		N.A.  LDD0396  [13]
OEA-DA
 Probe Info  		4.19  LDD0046  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 CDX: HA1; Afatinib resistant C235(1.22)  LDD2346  [4]
 LDCM0023  KB03 CDX: HA1; Afatinib resistant C235(1.77)  LDD2763  [4]
 LDCM0024  KB05 MV4-11 C235(2.69)  LDD3338  [4]
 LDCM0014  Panhematin HEK-293T 3.32  LDD0062  [6]
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 2.22  LDD0123  [5]

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
Tyrosine--tRNA ligase, cytoplasmic (YARS1) Class-I aminoacyl-tRNA synthetase family P54577
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Membrane-associated progesterone receptor component 2 (PGRMC2) Cytochrome b5 family O15173
Endophilin-B1 (SH3GLB1) Endophilin family Q9Y371
Transmembrane protein 242 (TMEM242) TMEM242 family Q9NWH2
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FAM209A (FAM209A) FAM209 family Q5JX71
Junctional sarcoplasmic reticulum protein 1 (JSRP1) . Q96MG2
Sprouty-related, EVH1 domain-containing protein 1 (SPRED1) . Q7Z699

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 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151
3 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
4 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
5 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.
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 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
8 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
9 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.
10 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.
11 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
12 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.
13 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
14 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570