General Information of Target

Target ID LDTP04939
Target Name Transforming growth factor beta-2 proprotein (TGFB2)
Gene Name TGFB2
Gene ID 7042
Synonyms
Transforming growth factor beta-2 proprotein; Cetermin; Glioblastoma-derived T-cell suppressor factor; G-TSF) [Cleaved into: Latency-associated peptide; LAP; Transforming growth factor beta-2; TGF-beta-2)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MHYCVLSAFLILHLVTVALSLSTCSTLDMDQFMRKRIEAIRGQILSKLKLTSPPEDYPEP
EEVPPEVISIYNSTRDLLQEKASRRAAACERERSDEEYYAKEVYKIDMPPFFPSENAIPP
TFYRPYFRIVRFDVSAMEKNASNLVKAEFRVFRLQNPKARVPEQRIELYQILKSKDLTSP
TQRYIDSKVVKTRAEGEWLSFDVTDAVHEWLHHKDRNLGFKISLHCPCCTFVPSNNYIIP
NKSEELEARFAGIDGTSTYTSGDQKTIKSTRKKNSGKTPHLLLMLLPSYRLESQQTNRRK
KRALDAAYCFRNVQDNCCLRPLYIDFKRDLGWKWIHEPKGYNANFCAGACPYLWSSDTQH
SRVLSLYNTINPEASASPCCVSQDLEPLTILYYIGKTPKIEQLSNMIVKSCKCS
Target Type
Clinical trial
Target Bioclass
Cytokine and receptor
Family
TGF-beta family
Subcellular location
Secreted; Secreted, extracellular space, extracellular matrix
Function
[Transforming growth factor beta-2 proprotein]: Precursor of the Latency-associated peptide (LAP) and Transforming growth factor beta-2 (TGF-beta-2) chains, which constitute the regulatory and active subunit of TGF-beta-2, respectively.; [Latency-associated peptide]: Required to maintain the Transforming growth factor beta-2 (TGF-beta-2) chain in a latent state during storage in extracellular matrix. Associates non-covalently with TGF-beta-2 and regulates its activation via interaction with 'milieu molecules', such as LTBP1 and LRRC32/GARP, that control activation of TGF-beta-2.; [Transforming growth factor beta-2]: Multifunctional protein that regulates various processes such as angiogenesis and heart development. Activation into mature form follows different steps: following cleavage of the proprotein in the Golgi apparatus, Latency-associated peptide (LAP) and Transforming growth factor beta-2 (TGF-beta-2) chains remain non-covalently linked rendering TGF-beta-2 inactive during storage in extracellular matrix. At the same time, LAP chain interacts with 'milieu molecules', such as LTBP1 and LRRC32/GARP, that control activation of TGF-beta-2 and maintain it in a latent state during storage in extracellular milieus. Once activated following release of LAP, TGF-beta-2 acts by binding to TGF-beta receptors (TGFBR1 and TGFBR2), which transduce signal.
TTD ID
T14143
Uniprot ID
P61812
DrugMap ID
TTY9TWO
Ensemble ID
ENST00000366929.4
HGNC ID
HGNC:11768
ChEMBL ID
CHEMBL3217393

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CORL23 SNV: p.F152I .
DU145 SNV: p.K175N DBIA    Probe Info 
HEC1 SNV: p.C318Y .
KASUMI1 SNV: p.P113L .
LNCaP clone FGC SNV: p.I370V DBIA    Probe Info 
MCC26 SNV: p.Y352S DBIA    Probe Info 
TKKK SNV: p.E90K .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K173(4.22); K81(6.32)  LDD0277  [1]
DBIA
 Probe Info 
C89(1.54)  LDD3311  [2]
BTD
 Probe Info 
C89(1.11)  LDD1700  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 42-MG-BA C89(1.90)  LDD2244  [2]
 LDCM0023  KB03 42-MG-BA C89(3.33)  LDD2661  [2]
 LDCM0024  KB05 G361 C89(1.54)  LDD3311  [2]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C89(1.00)  LDD2101  [3]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C89(0.75)  LDD2111  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C89(1.83)  LDD2125  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C89(0.69)  LDD2127  [3]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C89(0.51)  LDD2134  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C89(0.69)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C89(0.72)  LDD2137  [3]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C89(1.11)  LDD1700  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C89(0.54)  LDD2146  [3]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C89(0.76)  LDD2148  [3]

References

1 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
2 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
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