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Inhibition of the Chk1 kinase by small molecules binding to its active site is a strategy of great therapeutic interest for oncology.
Curcumin was reported to inhibit P-12-LOX via binding to its active site [28, 29].
Curcumin was reported to inhibit this enzyme via binding to its active site.
Rivaroxaban inhibits coagulation factor Xa directly by binding to its active centre.
BA inhibits the activity of serine proteases, including prostate-specific antigen (PSA), presumably by binding to its active site (Bone et al, 1987; Gallardo-Williams et al, 2003).
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Pro-uPA is converted to its active form after binding to its specific surface receptor, uPAR [ 1, 2].
Colonic tumour cells possess a cell surface protease capable of binding 9-aminoacridine to its active centre, thus locating cells when viewed under a fluorescence microscope.
By binding with TF, fVII is changed to its active form, fVIIa, and subsequently triggers the extrinsic coagulation cascade by activating factor X (Furie and Furie, 1988).
TSP-1 can convert latent TGF-β to its active form by binding to LAP, thereby releasing the active TGF-β from LAP.
According to our model, its binding to the active site of PTP-SL is assisted by hydrophobic (stacking) interactions with the highly conserved residue Y313PTP-SL which in turn is stabilized through hydrophobic forces between its aromatic ring and the aliphatic portion of the side chain of R312PTP-SL.
Despite this difference, its binding to the active sites is coordinated by three conserved histidine residues, [ 36].
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