3o1d | pdb_00003o1d

Structure-function study of Gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.

spinqualitylabelsall models 3o1d, resolution 2.40Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3o1d is a 2 chain structure with sequence from Danio rerio and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: G72 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function VDRA_DANRE Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis. Publication Abstract from PubMed Derivatives of vitamin D(3) containing a second side-chain emanating at C-20 are known as gemini and act as vitamin D receptor agonists. Recently, two of these, namely Gemini-0072 and the epimeric Gemini-0097, were selected for further studies in view of their high biological activities and lack of hypercalcemic effects. We now show that the two analogs recruit coactivator SRC-1 better than the parental gemini and act as VDR superagonists. The crystal structures of complexes of zVDR with Gemini-0072 and Gemini-0097 indicate that these ligands induce an extra cavity within the ligand-binding pocket similar to gemini and that their superagonistic activity is due to an increased stabilization of helix H12. Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.,Huet T, Maehr H, Lee HJ, Uskokovic MR, Suh N, Moras D, Rochel N Medchemcomm. 2011;2(5):424-429. PMID:22180837 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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