Target name

P36897: TGF-beta receptor type-1


  Protein function

Transmembrane serine/threonine kinase forming with the TGF-beta type II serine/threonine kinase receptor, TGFBR2, the non-promiscuous receptor for the TGF-beta cytokines TGFB1, TGFB2 and TGFB3. Transduces the TGFB1, TGFB2 and TGFB3 signal from the cell surface to the cytoplasm and is thus regulating a plethora of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. The formation of the receptor complex composed of 2 TGFBR1 and 2 TGFBR2 molecules symmetrically bound to the cytokine dimer results in the phosphorylation and the activation of TGFBR1 by the constitutively active TGFBR2. Activated TGFBR1 phosphorylates SMAD2 which dissociates from the receptor and interacts with SMAD4. The SMAD2-SMAD4 complex is subsequently translocated to the nucleus where it modulates the transcription of the TGF-beta-regulated genes. This constitutes the canonical SMAD-dependent TGF-beta signaling cascade. Also involved in non-canonical, SMAD-independent TGF-beta signaling pathways. For instance, TGFBR1 induces TRAF6 autoubiquitination which in turn results in MAP3K7 ubiquitination and activation to trigger apoptosis. Also regulates epithelial to mesenchymal transition through a SMAD-independent signaling pathway through PARD6A phosphorylation and activation.

  Database links

Uniprot primary ID P36897
PDB ID 1RW8 1PY5 3KFD 1VJY 2PJY 2X7O 2L5S 4X2N 1B6C 4X2J 2WOU 4X2G 1IAS 4X0M 3TZM 4X2K 1TBI 3GXL 3FAA 2WOT 3KCF 3HMM
DrugBank ID
BioGrid ID 112904
GuidetoPHARMACOLOGY ID 1788
PharmGKB ID PA36485
KEGG ID hsa:7046
DIP ID DIP-5935N
STRING ID 9606.ENSP00000364133
IntAct ID P36897
DMDM 547777
BRENDA 2.7.10.2 2.7.11.30
Reactome R-HSA-3304356 R-HSA-3315487 R-HSA-3645790 R-HSA-3656532 R-HSA-3656535 R-HSA-2173789 R-HSA-2173788 R-HSA-2173791
SignaLink P36897
BioCyc
Entrez Gene (Gene ID) 7046
BindingDB P36897

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.886 0.005 0.954 0.000 0.920 0.000 0.920 0.000 0.970 0.000 0.849 0.003 Download
Estate fingerprints 0.854 0.005 0.806 0.005 0.830 0.000 0.834 0.005 0.900 0.000 0.660 0.005 Download
MACCS fingerprints 0.860 0.000 0.832 0.000 0.846 0.005 0.849 0.003 0.924 0.005 0.689 0.003 Download
Daylight fingerprints 0.839 0.003 0.935 0.005 0.887 0.005 0.880 0.000 0.943 0.005 0.777 0.005 Download
ECFP2 fingerprints 0.939 0.003 0.921 0.005 0.930 0.000 0.930 0.000 0.980 0.000 0.866 0.005 Download
ECFP4 fingerprints 0.950 0.000 0.990 0.005 0.970 0.000 0.970 0.000 0.986 0.005 0.938 0.004 Download
ECFP6 fingerprints 0.948 0.004 0.992 0.000 0.970 0.000 0.970 0.000 0.980 0.000 0.942 0.004 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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