1ux2: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 5: | Line 5: | ||
==Overview== | ==Overview== | ||
Nicotinic acetylcholine receptors are prototypes for the pharmaceutically, important family of pentameric ligand-gated ion channels. Here we present, atomic resolution structures of nicotine and carbamylcholine binding to, AChBP, a water-soluble homolog of the ligand binding domain of nicotinic, receptors and their family members, GABAA, GABAC, 5HT3 serotonin, and, glycine receptors. Ligand binding is driven by enthalpy and is accompanied, by conformational changes in the ligand binding site. Residues in the, binding site contract around the ligand, with the largest movement in the, C loop. As expected, the binding is characterized by substantial aromatic, and hydrophobic contributions, but additionally there are close contacts, between protein oxygens and positively charged groups in the ... | Nicotinic acetylcholine receptors are prototypes for the pharmaceutically, important family of pentameric ligand-gated ion channels. Here we present, atomic resolution structures of nicotine and carbamylcholine binding to, AChBP, a water-soluble homolog of the ligand binding domain of nicotinic, receptors and their family members, GABAA, GABAC, 5HT3 serotonin, and, glycine receptors. Ligand binding is driven by enthalpy and is accompanied, by conformational changes in the ligand binding site. Residues in the, binding site contract around the ligand, with the largest movement in the, C loop. As expected, the binding is characterized by substantial aromatic, and hydrophobic contributions, but additionally there are close contacts, between protein oxygens and positively charged groups in the ligands. The, higher affinity of nicotine is due to a main chain hydrogen bond with the, B loop and a closer packing of the aromatic groups. These structures will, be useful tools for the development of new drugs involving nicotinic, acetylcholine receptor-associated diseases. | ||
==About this Structure== | ==About this Structure== | ||
1UX2 is a | 1UX2 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Lymnaea_stagnalis Lymnaea stagnalis] with NAG, SO4, NH4 and EPE as [http://en.wikipedia.org/wiki/ligands ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UX2 OCA]. | ||
==Reference== | ==Reference== | ||
| Line 30: | Line 30: | ||
[[Category: pentamer]] | [[Category: pentamer]] | ||
''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 14:34:08 2007'' | ||
