1prg: Difference between revisions
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==Overview== | ==Overview== | ||
The peroxisome proliferator-activated receptor-gamma (PPAR-gamma) is a, ligand-dependent transcription factor that is important in adipocyte, differentiation and glucose homeostasis and which depends on interactions, with co-activators, including steroid receptor co-activating factor-1, (SRC-1). Here we present the X-ray crystal structure of the human, apo-PPAR-gamma ligand-binding domain (LBD), at 2.2 A resolution; this, structure reveals a large binding pocket, which may explain the diversity, of ligands for PPAR-gamma. We also describe the ternary complex containing, the PPAR-gamma LBD, the antidiabetic ligand rosiglitazone (BRL49653), and, 88 amino acids of human SRC-1 at 2.3 A resolution. Glutamate and lysine, residues that are highly conserved in LBDs of nuclear receptors form a, .. | The peroxisome proliferator-activated receptor-gamma (PPAR-gamma) is a, ligand-dependent transcription factor that is important in adipocyte, differentiation and glucose homeostasis and which depends on interactions, with co-activators, including steroid receptor co-activating factor-1, (SRC-1). Here we present the X-ray crystal structure of the human, apo-PPAR-gamma ligand-binding domain (LBD), at 2.2 A resolution; this, structure reveals a large binding pocket, which may explain the diversity, of ligands for PPAR-gamma. We also describe the ternary complex containing, the PPAR-gamma LBD, the antidiabetic ligand rosiglitazone (BRL49653), and, 88 amino acids of human SRC-1 at 2.3 A resolution. Glutamate and lysine, residues that are highly conserved in LBDs of nuclear receptors form a, 'charge clamp' that contacts backbone atoms of the LXXLL helices of SRC-1., These results, together with the observation that two consecutive LXXLL, motifs of SRC-1 make identical contacts with both subunits of a PPAR-gamma, homodimer, suggest a general mechanism for the assembly of nuclear, receptors with co-activators. | ||
==About this Structure== | ==About this Structure== | ||
1PRG is a | 1PRG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Structure known Active Sites: LLL and LND. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1PRG OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transcription factor]] | [[Category: transcription factor]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:56:41 2007'' | ||
