Hinge region binding elements

Figure 2.18 Identified inhibitors of TGFpRl identified through inhibitor hybridisation. The red region shows the selectivity pocket fragment, the hinge region binding element is black and the solvent channel unit is coloured blue.

Indirubin-3 -monoxime has been demonstrated to be ATP competitive and to bind in the ATP binding site (X-ray crystal structure of protein-Hgand complex solved). The crystal structure is shown in Fig. 6. The key hinge region binding interestingly involves all three of the key H-bonding elements ... 

SHRs are built in a modular structure with similar structure elements. They contain a DNA-binding domain (DBD), a hinge region with a nuclear location signal (NLS), a ligand-binding domain (LBD) and several transcriptional activation functions (Fig. 1). 

The core of all eukaryotic Ser/Thr- and Tyr-specific protein kinases adopt a common fold illustrated in Fig. 7.3 for the tyrosine kinase domain of the insulin receptor. The structure comprises two lobes that are conneded by a hinge region. The N-terminal lobe contains five / -structures and one a-helix, named C-helix. In contrast, the larger C-terminal lobe is mostly a-helical. It comprises a four-helix bundle, additional a-he-lices, and two short yS-strands. ATP and 1 or 2 metal ions are bound at the interface of the two lobes, while the binding site for the peptide substrate is located mostly in the C-terminal lobe. The following structural elements have been found to be critical for catalysis and for protein kinase control ... 

Figure 2. Model for Ferritin mRNA Translational Control Iron releases IRP-l/IRP-2 from suppressing ferritin mRNA translation at the Iron responsive Element stemloops (IREs) specific to the L- and H- mRNA 5 cap sites. In the diagram, IRP-I and IRP-2 are depicted as two domains separated by a hinge region (line). Our preliminary data suggests that the RNA binding protein (Poly C-binding proteins, CP-1 and CP-2) interact with the ferritin mRNA acute box(AB) domain (box) downstream from the IRE (Thomson et al. In revision).

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