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Some molecules slow or stop an enzyme by binding to and blocking the site where its substrates normally bind: its 'active site'.
The X-linked inhibitor of apoptosis protein (XIAP) is overexpressed in several malignant cells where it prevents apoptosis by binding to, and blocking, the activation of caspase-3, -7, and -9.
C/EBPβ-Ala217 binding to, and blocking, RSK phosphorylation results in decreased phosphorylation of C/EBPβ on Thr217, and presumably, other target survival proteins by activated RSK.
C/EBPβ-Ala217 binding to, and blocking, RSK phosphorylation (Figure 5A) results in decreased phosphorylation of C/EBPβ on Thr217, and presumably, other target survival proteins by activated RSK [5][10][11].
Adding tamoxifen inhibited the stimulating effect of the estrogens by binding to and blocking the ER.
For instance, the Dickkopf family of secreted Wnt antagonists moderate Wnt activity by binding to and blocking Lrp5/6 (Mao et al., 2001).
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However, both Trx1 and sCD30 can influence the ability of CD30R to mediate the activation of intracellular signaling by selectively inhibiting interaction with CD30L (Fig. 1 and Online Resource 1): Trx1 by catalytically changing RCD30 structure and sCD30 by closely binding to CD30L and blocking its binding to RCD30.
Treatment with specific integrin blocking antibodies revealed that blocking ITGA5 impaired adhesion to FN, blocking ITGAV and ITGB5 reduced the binding to VTN, and blocking ITGA6 inhibited binding to LN.
Poxviruses have developed a family of secreted TNFRs which are thought to act in vivo by binding to TNF and blocking its activity.
Previous studies have shown that TRB3 is a pseudokinase that impaires insulin signaling by binding to Akt and blocking its activation32.
Vincristine is a dimeric Catharanthus alkaloid derived from the Madagascan periwinkle that acts by binding to tubulin and blocking metaphase in actively dividing cells.
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