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DrugBank target: P62942

DrugBank target: P62942 (FKB1A_HUMAN)     

Example drug-target structure: 1bkf

( There are 43 structures corresponding to this UniProt sequence in the PDB. Click the orange, plus icon above for a list. )

Peptidyl-prolyl cis-trans isomerase FKBP1A

12 kDa FK506-binding protein, Calstabin-1, FK506-binding protein 1A, Immunophilin FKBP12, Rotamase, PPIase FKBP1A, 12 kDa FKBP, FKBP-12, FKBP-1A.

Function

Keeps in an inactive conformation TGFBR1, the TGF-beta type I serine/threonine kinase receptor, preventing TGF-beta receptor activation in absence of ligand. Recruites SMAD7 to ACVR1B which prevents the association of SMAD2 and SMAD3 with the activin receptor complex, thereby blocking the activin signal. May modulate the RYR1 calcium channel activity. PPIases accelerate the folding of proteins. It catalyzes the cis-trans isomerization of proline imidic peptide bonds in oligopeptides..

Enzyme

5.2.1.8   [EC->PDB]   [IntEnz]   [ExPASy]   [KEGG]  

Catalytic activity

Peptidylproline (omega=180) = peptidylproline (omega=0).

Schematic diagram of Pfam domains in target sequence plus wiring diagram of PDB structure containing drug molecule

1bkf

Key:    PfamA domain  Secondary structure  Bound drug molecule

Sequence length: 107 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 3 drugs for this target protein:

 

Generic name: DB00864 tacrolimus
FK5
Formula: C44H69No12
Structure: There are 18 PDB structures containing this molecule of which 4 are bound to the above target protein.
 
Generic name: DB00337 pimecrolimus
Formula: C43H68Clno11
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00877 sirolimus
Formula: C51H79No13
Structure: There are no structures of this molecule in the PDB.

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