Details of the Target

General Information of Target

Target ID LDTP02503
Target Name Transforming growth factor beta-3 proprotein (TGFB3)
Gene Name TGFB3
Gene ID 7043
Synonyms
Transforming growth factor beta-3 proprotein [Cleaved into: Latency-associated peptide; LAP; Transforming growth factor beta-3; TGF-beta-3)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKMHLQRALVVLALLNFATVSLSLSTCTTLDFGHIKKKRVEAIRGQILSKLRLTSPPEPT
VMTHVPYQVLALYNSTRELLEEMHGEREEGCTQENTESEYYAKEIHKFDMIQGLAEHNEL
AVCPKGITSKVFRFNVSSVEKNRTNLFRAEFRVLRVPNPSSKRNEQRIELFQILRPDEHI
AKQRYIGGKNLPTRGTAEWLSFDVTDTVREWLLRRESNLGLEISIHCPCHTFQPNGDILE
NIHEVMEIKFKGVDNEDDHGRGDLGRLKKQKDHHNPHLILMMIPPHRLDNPGQGGQRKKR
ALDTNYCFRNLEENCCVRPLYIDFRQDLGWKWVHEPKGYYANFCSGPCPYLRSADTTHST
VLGLYNTLNPEASASPCCVPQDLEPLTILYYVGRTPKVEQLSNMVVKSCKCS
Target Type
Clinical trial
Target Bioclass
Other
Family
TGF-beta family
Subcellular location
Secreted; Secreted, extracellular space, extracellular matrix
Function
Transforming growth factor beta-3 proprotein: Precursor of the Latency-associated peptide (LAP) and Transforming growth factor beta-3 (TGF-beta-3) chains, which constitute the regulatory and active subunit of TGF-beta-3, respectively.; [Latency-associated peptide]: Required to maintain the Transforming growth factor beta-3 (TGF-beta-3) chain in a latent state during storage in extracellular matrix. Associates non-covalently with TGF-beta-3 and regulates its activation via interaction with 'milieu molecules', such as LTBP1 and LRRC32/GARP, that control activation of TGF-beta-3. Interaction with integrins results in distortion of the Latency-associated peptide chain and subsequent release of the active TGF-beta-3.; Transforming growth factor beta-3: Multifunctional protein that regulates embryogenesis and cell differentiation and is required in various processes such as secondary palate 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-3 (TGF-beta-3) chains remain non-covalently linked rendering TGF-beta-3 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-3 and maintain it in a latent state during storage in extracellular milieus. TGF-beta-3 is released from LAP by integrins: integrin-binding results in distortion of the LAP chain and subsequent release of the active TGF-beta-3. Once activated following release of LAP, TGF-beta-3 acts by binding to TGF-beta receptors (TGFBR1 and TGFBR2), which transduce signal.
TTD ID
T22978
Uniprot ID
P10600
DrugMap ID
TTWOMY8
Ensemble ID
ENST00000238682.8
HGNC ID
HGNC:11769
ChEMBL ID
CHEMBL3712903

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
IM95 Deletion: p.E313del
Insertion: p.E58Ter		 .
KMS11 SNV: p.T29P .
LN18 SNV: p.H64P; p.E216G .
RL952 SNV: p.T205A .
SUPT1 SNV: p.L51F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C307(4.81)  LDD3493  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 AU565 C307(4.17)  LDD2265  [1]
 LDCM0023  KB03 AU565 C307(2.97)  LDD2682  [1]
 LDCM0024  KB05 ZR-75-1 C307(4.81)  LDD3493  [1]

References

1 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