Details of the Target

General Information of Target

Target ID LDTP02923
Target Name Endoglin (ENG)
Gene Name ENG
Gene ID 2022
Synonyms
END; Endoglin; CD antigen CD105
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDRGTLPLAVALLLASCSLSPTSLAETVHCDLQPVGPERGEVTYTTSQVSKGCVAQAPNA
ILEVHVLFLEFPTGPSQLELTLQASKQNGTWPREVLLVLSVNSSVFLHLQALGIPLHLAY
NSSLVTFQEPPGVNTTELPSFPKTQILEWAAERGPITSAAELNDPQSILLRLGQAQGSLS
FCMLEASQDMGRTLEWRPRTPALVRGCHLEGVAGHKEAHILRVLPGHSAGPRTVTVKVEL
SCAPGDLDAVLILQGPPYVSWLIDANHNMQIWTTGEYSFKIFPEKNIRGFKLPDTPQGLL
GEARMLNASIVASFVELPLASIVSLHASSCGGRLQTSPAPIQTTPPKDTCSPELLMSLIQ
TKCADDAMTLVLKKELVAHLKCTITGLTFWDPSCEAEDRGDKFVLRSAYSSCGMQVSASM
ISNEAVVNILSSSSPQRKKVHCLNMDSLSFQLGLYLSPHFLQASNTIEPGQQSFVQVRVS
PSVSEFLLQLDSCHLDLGPEGGTVELIQGRAAKGNCVSLLSPSPEGDPRFSFLLHFYTVP
IPKTGTLSCTVALRPKTGSQDQEVHRTVFMRLNIISPDLSGCTSKGLVLPAVLGITFGAF
LIGALLTAALWYIYSHTRSPSKREPVVAVAAPASSESSSTNHSIGSTQSTPCSTSSMA
Target Type
Clinical trial
Target Bioclass
Cytokine and receptor
Subcellular location
Cell membrane
Function
Vascular endothelium glycoprotein that plays an important role in the regulation of angiogenesis. Required for normal structure and integrity of adult vasculature. Regulates the migration of vascular endothelial cells. Required for normal extraembryonic angiogenesis and for embryonic heart development. May regulate endothelial cell shape changes in response to blood flow, which drive vascular remodeling and establishment of normal vascular morphology during angiogenesis. May play a critical role in the binding of endothelial cells to integrins and/or other RGD receptors. Acts as a TGF-beta coreceptor and is involved in the TGF-beta/BMP signaling cascade that ultimately leads to the activation of SMAD transcription factors. Required for GDF2/BMP9 signaling through SMAD1 in endothelial cells and modulates TGFB1 signaling through SMAD3.
TTD ID
T22350
Uniprot ID
P17813
DrugMap ID
TTB30LE
Ensemble ID
ENST00000344849.4
HGNC ID
HGNC:3349
ChEMBL ID
CHEMBL3712885

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2780 SNV: p.W272C .
BXPC3 SNV: p.K216N .
HEL Substitution: p.H108Y .
HEL9217 Substitution: p.H108Y .
KYSE510 SNV: p.P293S .
P31FUJ SNV: p.R222G .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
OPA-S-S-alkyne
 Probe Info  		K285(0.18); K556(2.03); K402(2.25); K513(4.09)  LDD3494  [2]
BTD
 Probe Info  		C207(1.93)  LDD1700  [3]
AHL-Pu-1
 Probe Info  		C652(10.38)  LDD0171  [4]
Acrolein
 Probe Info  		C30(0.00); C582(0.00); H227(0.00)  LDD0222  [5]
DBIA
 Probe Info  		C582(0.96)  LDD0078  [6]
IPM
 Probe Info  		N.A.  LDD0025  [7]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
Methacrolein
 Probe Info  		C30(0.00); C582(0.00)  LDD0218  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C207(1.20); C582(1.25)  LDD2142  [3]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C207(1.79); C582(1.26)  LDD2112  [3]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C30(0.54); C207(0.39)  LDD2095  [3]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C207(0.98)  LDD2130  [3]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C30(1.01); C207(0.96); C582(0.82); C549(0.91)  LDD2117  [3]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C207(1.19); C582(1.48); C549(1.08)  LDD2152  [3]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C582(1.52); C549(0.96)  LDD2103  [3]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C207(0.47); C549(0.83)  LDD2132  [3]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C207(0.54)  LDD2131  [3]
 LDCM0026  4SU-RNA+native RNA DM93 C652(10.38)  LDD0171  [4]
 LDCM0545  Acetamide MDA-MB-231 C30(0.71); C207(0.58)  LDD2138  [3]
 LDCM0520  AKOS000195272 MDA-MB-231 C207(0.98); C582(0.77); C549(1.01)  LDD2113  [3]
 LDCM0020  ARS-1620 HCC44 C582(0.96)  LDD0078  [6]
 LDCM0498  BS-3668 MDA-MB-231 C207(0.58)  LDD2091  [3]
 LDCM0108  Chloroacetamide HeLa C30(0.00); C582(0.00); H227(0.00)  LDD0222  [5]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C582(6.50); C549(2.15); C207(1.66); C30(1.17)  LDD1702  [3]
 LDCM0022  KB02 42-MG-BA C207(2.14)  LDD2244  [8]
 LDCM0023  KB03 MDA-MB-231 C582(9.44); C207(5.02)  LDD1701  [3]
 LDCM0024  KB05 COLO792 C207(4.59); C516(2.28)  LDD3310  [8]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C582(1.34); C549(0.80)  LDD2102  [3]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C207(0.78)  LDD2121  [3]
 LDCM0109  NEM HeLa N.A.  LDD0225  [5]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C207(0.65); C582(0.41)  LDD2089  [3]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C207(1.02); C549(1.01)  LDD2093  [3]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C207(0.69); C549(1.16)  LDD2094  [3]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C207(1.01); C582(0.89); C549(1.00)  LDD2097  [3]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C549(1.27)  LDD2098  [3]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C30(0.96); C207(1.29); C582(0.87); C549(0.94)  LDD2099  [3]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C207(0.64); C582(0.96)  LDD2100  [3]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C207(1.71); C582(1.05)  LDD2101  [3]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C207(0.96)  LDD2104  [3]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C582(0.91); C549(0.82)  LDD2105  [3]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C207(0.71); C582(0.80)  LDD2107  [3]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C207(1.82); C582(1.06)  LDD2108  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C207(1.07); C582(0.79); C549(0.64)  LDD2109  [3]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C30(1.02); C207(0.92); C549(0.73)  LDD2111  [3]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C207(0.87); C582(0.89); C549(0.51)  LDD2114  [3]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C582(0.75)  LDD2115  [3]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C207(1.41)  LDD2118  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C30(0.87); C207(1.62); C582(2.55); C549(1.36)  LDD2119  [3]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C207(0.77); C549(0.68)  LDD2120  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C30(1.06); C207(0.82); C582(0.81)  LDD2123  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C30(1.03); C207(0.81); C582(0.78); C549(0.59)  LDD2125  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C30(1.38); C207(0.93)  LDD2127  [3]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C207(0.71)  LDD2128  [3]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C207(0.92); C582(1.20); C549(0.76)  LDD2129  [3]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C207(0.83); C582(0.77)  LDD2133  [3]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C30(0.54); C207(0.77); C582(0.54); C549(0.73)  LDD2134  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C207(1.11); C582(1.00)  LDD2135  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C30(0.95); C207(0.98); C582(1.00); C549(0.76)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C30(1.13); C207(0.92); C582(0.87); C549(0.66)  LDD2137  [3]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C207(1.93)  LDD1700  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C207(0.68); C582(0.61); C549(0.59)  LDD2140  [3]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C207(1.16); C582(0.70)  LDD2141  [3]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C207(0.94); C549(0.84)  LDD2143  [3]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C207(2.05); C582(3.66)  LDD2144  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C207(0.82)  LDD2146  [3]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C207(2.35); C549(1.35)  LDD2147  [3]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C30(0.85); C207(0.67); C582(0.62); C549(0.59)  LDD2148  [3]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C207(0.43); C549(0.84)  LDD2150  [3]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C582(1.47)  LDD2153  [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
E3 ubiquitin-protein ligase TRIM21 (TRIM21) TRIM/RBCC family P19474
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Integrin alpha-5 (ITGA5) Integrin alpha chain family P08648
Integrin beta-1 (ITGB1) Integrin beta chain family P05556
Galectin-3 (LGALS3) . P17931
Cytokine and receptor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transforming growth factor beta-1 proprotein (TGFB1) TGF-beta family P01137
Endoglin (ENG) . P17813
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leucine-rich alpha-2-glycoprotein (LRG1) . P02750

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Trc105 Monoclonal antibody D00YQI
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Carotuximab . DB06322

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 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
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 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
5 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.
6 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.
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 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