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When Tsg binds in the vWC1 position this causes dissociation of Sog from collagen IV releasing the complex from the matrix.
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Resveratrol binds in the T4 binding pocket of tetrameric TTR, resulting in increased fluorescence quantum yield in a concentration-dependent manner.
This result appears surprising as KorA binds in the -10 region of the promoter, precisely overlapping the RNAP binding site [ 18].
Protein crystallography revealed that this moiety binds in the S1′ pocket of the enzyme.
Potency versus aggrecanase was optimized by modification of the benzyloxyarylsulfonamide group that binds in the S1′ pocket.
Oral bioavailability was found to be dependent on metabolic clearance and cellular permeability, and was optimized through modulation of the sidechain that binds in the S3sp subsite.
Optimization of the alkyne and tetrahydropyridine portions of the pharmacophore provided potent CatS inhibitors (IC50 = 40 300 nM), and an X-ray structure of 32 revealed that the arylalkyne moiety binds in the S1 pocket of the enzyme.
c-MYC-fwd2 binds in the 5'UTR upstream of the ATG and c-MYC-fwd, also used for expression construct cloning, binds to the ATG start codon region.
The indole anchor of (S -YH239 bindS -YH239 Trp23 pocket of MDM2.
(a) Model of C12M01 bound in the MAP4K4 binding site with extended P-loop conformation.
Many small molecules bind in the T4 binding pocket of TTR and prevent its aggregation and amyloidogenesis cascade by stabilizing the native tetramer [ 27– 29].
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