Details of the Target

General Information of Target

Target ID LDTP10987
Target Name Tumor susceptibility gene 101 protein (TSG101)
Gene Name TSG101
Gene ID 7251
Synonyms
Tumor susceptibility gene 101 protein; ESCRT-I complex subunit TSG101
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLA
ISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMG
LTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRG
RTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLD
SKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKG
QVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTE
SLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQN
FEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCS
TPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDF
QLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPE
HRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTE
FLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQ
DLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHL
PLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELT
RYDCEVNVPVLGSSTLLQGGDLLRALDQAT
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Ubiquitin-conjugating enzyme family, UEV subfamily
Subcellular location
Cytoplasm
Function
Component of the ESCRT-I complex, a regulator of vesicular trafficking process. Binds to ubiquitinated cargo proteins and is required for the sorting of endocytic ubiquitinated cargos into multivesicular bodies (MVBs). Mediates the association between the ESCRT-0 and ESCRT-I complex. Required for completion of cytokinesis; the function requires CEP55. May be involved in cell growth and differentiation. Acts as a negative growth regulator. Involved in the budding of many viruses through an interaction with viral proteins that contain a late-budding motif P-[ST]-A-P. This interaction is essential for viral particle budding of numerous retroviruses. Required for the exosomal release of SDCBP, CD63 and syndecan. It may also play a role in the extracellular release of microvesicles that differ from the exosomes.
TTD ID
T01283
Uniprot ID
Q99816
DrugMap ID
TTHU7JA
Ensemble ID
ENST00000251968.4
HGNC ID
HGNC:15971
ChEMBL ID
CHEMBL6157

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.W117R .
HCT116 SNV: p.H267R .
HCT15 SNV: p.K243N .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
YN-1
 Probe Info  		100.00  LDD0444  [3]
STPyne
 Probe Info  		K237(4.08); K257(0.90); K294(5.63); K361(6.34)  LDD0277  [4]
ONAyne
 Probe Info  		K294(7.03)  LDD0275  [4]
Probe 1
 Probe Info  		Y42(17.84)  LDD3495  [5]
HPAP
 Probe Info  		3.15  LDD0063  [6]
HHS-475
 Probe Info  		Y63(0.84)  LDD0264  [7]
HHS-465
 Probe Info  		Y63(6.91)  LDD2237  [8]
DBIA
 Probe Info  		C73(0.60)  LDD0812  [9]
CY4
 Probe Info  		R368(0.00); R374(0.00)  LDD0247  [2]
IA-alkyne
 Probe Info  		C87(0.00); C73(0.00)  LDD0036  [10]
1c-yne
 Probe Info  		N.A.  LDD0228  [11]
AOyne
 Probe Info  		15.00  LDD0443  [12]
HHS-482
 Probe Info  		Y63(1.35)  LDD2239  [8]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C191
 Probe Info  		12.21  LDD1868  [13]
FFF probe11
 Probe Info  		12.82  LDD0472  [14]
FFF probe13
 Probe Info  		20.00  LDD0475  [14]
FFF probe2
 Probe Info  		20.00  LDD0463  [14]
FFF probe3
 Probe Info  		20.00  LDD0465  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C73(0.60)  LDD0812  [9]
 LDCM0216  AC100 HEK-293T C73(0.77)  LDD0814  [9]
 LDCM0217  AC101 HEK-293T C73(0.90)  LDD0815  [9]
 LDCM0218  AC102 HEK-293T C73(0.94)  LDD0816  [9]
 LDCM0219  AC103 HEK-293T C73(0.71)  LDD0817  [9]
 LDCM0220  AC104 HEK-293T C73(0.74)  LDD0818  [9]
 LDCM0221  AC105 HEK-293T C73(0.93)  LDD0819  [9]
 LDCM0222  AC106 HEK-293T C73(0.95)  LDD0820  [9]
 LDCM0223  AC107 HEK-293T C73(0.86)  LDD0821  [9]
 LDCM0224  AC108 HEK-293T C73(1.11)  LDD0822  [9]
 LDCM0225  AC109 HEK-293T C73(0.85)  LDD0823  [9]
 LDCM0227  AC110 HEK-293T C73(0.50)  LDD0825  [9]
 LDCM0228  AC111 HEK-293T C73(0.22)  LDD0826  [9]
 LDCM0229  AC112 HEK-293T C73(0.46)  LDD0827  [9]
 LDCM0230  AC113 HEK-293T C73(0.94)  LDD0828  [9]
 LDCM0231  AC114 HEK-293T C73(1.18)  LDD0829  [9]
 LDCM0232  AC115 HEK-293T C73(1.05)  LDD0830  [9]
 LDCM0233  AC116 HEK-293T C73(0.84)  LDD0831  [9]
 LDCM0234  AC117 HEK-293T C73(0.74)  LDD0832  [9]
 LDCM0235  AC118 HEK-293T C73(0.90)  LDD0833  [9]
 LDCM0236  AC119 HEK-293T C73(0.74)  LDD0834  [9]
 LDCM0238  AC120 HEK-293T C73(0.73)  LDD0836  [9]
 LDCM0239  AC121 HEK-293T C73(0.89)  LDD0837  [9]
 LDCM0240  AC122 HEK-293T C73(0.67)  LDD0838  [9]
 LDCM0241  AC123 HEK-293T C73(0.60)  LDD0839  [9]
 LDCM0242  AC124 HEK-293T C73(0.82)  LDD0840  [9]
 LDCM0243  AC125 HEK-293T C73(0.70)  LDD0841  [9]
 LDCM0244  AC126 HEK-293T C73(0.59)  LDD0842  [9]
 LDCM0245  AC127 HEK-293T C73(0.32)  LDD0843  [9]
 LDCM0279  AC2 HEK-293T C73(1.11)  LDD0877  [9]
 LDCM0290  AC3 HEK-293T C73(0.91)  LDD0888  [9]
 LDCM0301  AC4 HEK-293T C73(0.70)  LDD0899  [9]
 LDCM0312  AC5 HEK-293T C73(0.87)  LDD0910  [9]
 LDCM0320  AC57 HEK-293T C73(1.11)  LDD0918  [9]
 LDCM0321  AC58 HEK-293T C73(1.24)  LDD0919  [9]
 LDCM0322  AC59 HEK-293T C73(1.07)  LDD0920  [9]
 LDCM0324  AC60 HEK-293T C73(0.79)  LDD0922  [9]
 LDCM0325  AC61 HEK-293T C73(1.06)  LDD0923  [9]
 LDCM0326  AC62 HEK-293T C73(0.93)  LDD0924  [9]
 LDCM0327  AC63 HEK-293T C73(0.75)  LDD0925  [9]
 LDCM0328  AC64 HEK-293T C73(1.36)  LDD0926  [9]
 LDCM0329  AC65 HEK-293T C73(0.98)  LDD0927  [9]
 LDCM0330  AC66 HEK-293T C73(0.94)  LDD0928  [9]
 LDCM0331  AC67 HEK-293T C73(0.85)  LDD0929  [9]
 LDCM0365  AC98 HEK-293T C73(0.93)  LDD0963  [9]
 LDCM0366  AC99 HEK-293T C73(1.13)  LDD0964  [9]
 LDCM0156  Aniline NCI-H1299 11.77  LDD0403  [1]
 LDCM0369  CL100 HEK-293T C73(0.95)  LDD0967  [9]
 LDCM0371  CL102 HEK-293T C73(0.89)  LDD1575  [15]
 LDCM0372  CL103 HEK-293T C73(0.90)  LDD1576  [15]
 LDCM0375  CL106 HEK-293T C73(1.04)  LDD1579  [15]
 LDCM0376  CL107 HEK-293T C73(1.24)  LDD1580  [15]
 LDCM0380  CL110 HEK-293T C73(1.07)  LDD1584  [15]
 LDCM0381  CL111 HEK-293T C73(1.00)  LDD1585  [15]
 LDCM0384  CL114 HEK-293T C73(1.05)  LDD1588  [15]
 LDCM0385  CL115 HEK-293T C73(1.10)  LDD1589  [15]
 LDCM0388  CL118 HEK-293T C73(0.91)  LDD1592  [15]
 LDCM0389  CL119 HEK-293T C73(0.98)  LDD1593  [15]
 LDCM0393  CL122 HEK-293T C73(0.89)  LDD1597  [15]
 LDCM0394  CL123 HEK-293T C73(0.85)  LDD1598  [15]
 LDCM0396  CL125 HEK-293T C73(0.91)  LDD0994  [9]
 LDCM0397  CL126 HEK-293T C73(0.85)  LDD0995  [9]
 LDCM0398  CL127 HEK-293T C73(1.23)  LDD0996  [9]
 LDCM0399  CL128 HEK-293T C73(1.12)  LDD0997  [9]
 LDCM0401  CL14 HEK-293T C73(1.03)  LDD1605  [15]
 LDCM0402  CL15 HEK-293T C73(1.10)  LDD1606  [15]
 LDCM0407  CL2 HEK-293T C73(0.84)  LDD1611  [15]
 LDCM0414  CL26 HEK-293T C73(1.06)  LDD1618  [15]
 LDCM0415  CL27 HEK-293T C73(0.89)  LDD1619  [15]
 LDCM0418  CL3 HEK-293T C73(1.10)  LDD1622  [15]
 LDCM0428  CL39 HEK-293T C73(0.93)  LDD1632  [15]
 LDCM0441  CL50 HEK-293T C73(0.98)  LDD1645  [15]
 LDCM0454  CL62 HEK-293T C73(0.98)  LDD1657  [15]
 LDCM0455  CL63 HEK-293T C73(0.94)  LDD1658  [15]
 LDCM0467  CL74 HEK-293T C73(1.01)  LDD1670  [15]
 LDCM0480  CL86 HEK-293T C73(0.93)  LDD1683  [15]
 LDCM0481  CL87 HEK-293T C73(0.85)  LDD1684  [15]
 LDCM0486  CL91 HEK-293T C73(0.98)  LDD1084  [9]
 LDCM0487  CL92 HEK-293T C73(0.66)  LDD1085  [9]
 LDCM0488  CL93 HEK-293T C73(0.96)  LDD1086  [9]
 LDCM0489  CL94 HEK-293T C73(0.89)  LDD1087  [9]
 LDCM0490  CL95 HEK-293T C73(0.69)  LDD1088  [9]
 LDCM0491  CL96 HEK-293T C73(0.86)  LDD1089  [9]
 LDCM0492  CL97 HEK-293T C73(0.86)  LDD1090  [9]
 LDCM0493  CL98 HEK-293T C73(0.88)  LDD1091  [9]
 LDCM0494  CL99 HEK-293T C73(0.73)  LDD1092  [9]
 LDCM0495  E2913 HEK-293T C73(0.96)  LDD1698  [15]
 LDCM0468  Fragment33 HEK-293T C73(0.99)  LDD1671  [15]
 LDCM0427  Fragment51 HEK-293T C73(1.03)  LDD1631  [15]
 LDCM0116  HHS-0101 DM93 Y63(0.84)  LDD0264  [7]
 LDCM0117  HHS-0201 DM93 Y63(0.44)  LDD0265  [7]
 LDCM0118  HHS-0301 DM93 Y63(0.36)  LDD0266  [7]
 LDCM0119  HHS-0401 DM93 Y63(0.23)  LDD0267  [7]
 LDCM0120  HHS-0701 DM93 Y63(0.81)  LDD0268  [7]
 LDCM0014  Panhematin K562 3.15  LDD0063  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Rho-associated protein kinase 1 (ROCK1) AGC Ser/Thr protein kinase family Q13464
Tyrosine-protein phosphatase non-receptor type 23 (PTPN23) Protein-tyrosine phosphatase family Q9H3S7
Kinesin-like protein KIFC3 (KIFC3) Kinesin family Q9BVG8
E3 ubiquitin-protein ligase LNX (LNX1) . Q8TBB1
E3 ubiquitin-protein ligase LRSAM1 (LRSAM1) . Q6UWE0
E3 ubiquitin-protein ligase MGRN1 (MGRN1) . O60291
Probable E3 ubiquitin-protein ligase TRIML2 (TRIML2) . Q8N7C3
Tripartite motif-containing protein 54 (TRIM54) . Q9BYV2
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
ADP-ribosylation factor-binding protein GGA3 (GGA3) GGA protein family Q9NZ52
SNARE-associated protein Snapin (SNAPIN) SNAPIN family O95295
CD2-associated protein (CD2AP) . Q9Y5K6
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein PKNOX2 (PKNOX2) TALE/MEIS homeobox family Q96KN3
Protein capicua homolog (CIC) . Q96RK0
Other
Click To Hide/Show 39 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apoptosis-stimulating of p53 protein 1 (PPP1R13B) ASPP family Q96KQ4
Neutrophil gelatinase-associated lipocalin (LCN2) Lipocalin family P80188
Coiled-coil domain-containing protein 88B (CCDC88B) CCDC88 family A6NC98
Lipopolysaccharide-induced tumor necrosis factor-alpha factor (LITAF) CDIP1/LITAF family Q99732
Protein chibby homolog 1 (CBY1) Chibby family Q9Y3M2
Death domain-associated protein 6 (DAXX) DAXX family Q9UER7
Protein FAM110A (FAM110A) FAM110 family Q9BQ89
Protein FAM9B (FAM9B) FAM9 family Q8IZU0
Golgi membrane protein 1 (GOLM1) GOLM family Q8NBJ4
HAUS augmin-like complex subunit 1 (HAUS1) HAUS1 family Q96CS2
Protein INCA1 (INCA1) INCA family Q0VD86
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cuticular Ha4 (KRT34) Intermediate filament family O76011
Keratin, type I cuticular Ha5 (KRT35) Intermediate filament family Q92764
Keratin, type I cytoskeletal 16 (KRT16) Intermediate filament family P08779
Keratin, type I cytoskeletal 18 (KRT18) Intermediate filament family P05783
Keratin, type II cytoskeletal 75 (KRT75) Intermediate filament family O95678
Harmonin-binding protein USHBP1 (USHBP1) MCC family Q8N6Y0
Marginal zone B- and B1-cell-specific protein (MZB1) MZB1 family Q8WU39
Synaptonemal complex central element protein 1 (SYCE1) SYCE family Q8N0S2
Tuftelin-interacting protein 11 (TFIP11) TFP11/STIP family Q9UBB9
Vacuolar protein sorting-associated protein 28 homolog (VPS28) VPS28 family Q9UK41
Vacuolar protein sorting-associated protein 37A (VPS37A) VPS37 family Q8NEZ2
Vacuolar protein sorting-associated protein 37B (VPS37B) VPS37 family Q9H9H4
Vacuolar protein sorting-associated protein 37C (VPS37C) VPS37 family A5D8V6
LIM domain-containing protein ajuba (AJUBA) Zyxin/ajuba family Q96IF1
BAG family molecular chaperone regulator 4 (BAG4) . O95429
Centrosomal protein of 55 kDa (CEP55) . Q53EZ4
Hematopoietic SH2 domain-containing protein (HSH2D) . Q96JZ2
Hepatocyte growth factor-regulated tyrosine kinase substrate (HGS) . O14964
Leukocyte receptor cluster member 8 (LENG8) . Q96PV6
Mediator of DNA damage checkpoint protein 1 (MDC1) . Q14676
PDZ and LIM domain protein 7 (PDLIM7) . Q9NR12
Protein hinderin (KIAA1328) . Q86T90
Ras GTPase-activating-like protein IQGAP1 (IQGAP1) . P46940
Tax1-binding protein 1 (TAX1BP1) . Q86VP1
TNFAIP3-interacting protein 1 (TNIP1) . Q15025
YLP motif-containing protein 1 (YLPM1) . P49750
ZW10 interactor (ZWINT) . O95229

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fgi-101-1a6 Antibody D03RCB

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 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.
3 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.
4 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
5 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.
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 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 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.
9 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
10 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
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 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.
13 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
14 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.
15 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402