Structure of PDB 1vjy Chain A

Receptor sequence
>1vjyA (length=299) Species: 9606 (Homo sapiens) [Search protein sequence]
IARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQ
TVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIA
DLGLAVRHDSATDTIDIRVGTKRYMAPEVLDDSINMKHFESFKRADIYAM
GLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNI
PNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
3D structure
PDB1vjy Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-beta Type I Receptor Inhibitors.
ChainA
Resolution2.0 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D333 K335 N338 D351 T375
Catalytic site (residue number reindexed from 1) D133 K135 N138 D151 T171
Enzyme Commision number 2.7.11.30: receptor protein serine/threonine kinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 460 A I211 A230 K232 L260 L278 S280 Y282 H283 L340 D351 I11 A30 K32 L60 L78 S80 Y82 H83 L140 D151 MOAD: ic50=0.023uM
PDBbind-CN: -logKd/Ki=7.64,IC50=0.023uM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004675 transmembrane receptor protein serine/threonine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007178 cell surface receptor protein serine/threonine kinase signaling pathway
Cellular Component
GO:0016020 membrane

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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:1vjy, PDBe:1vjy, PDBj:1vjy
PDBsum1vjy
PubMed15317461
UniProtP36897|TGFR1_HUMAN TGF-beta receptor type-1 (Gene Name=TGFBR1)

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