Ligand-binding Pockets

The structures of enzyme active sites, and other ligand binding pockets on enzymes, are ideally suited for high-affinity interactions with drug-like inhibitors. 

Mutations in Drug Targets Leading to Changes in the Ligand Binding Pocket... 

A., Gustafsson, J.A. and Carlquist, M. (2003) The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands. The Journal of Biological Chemistry, 278, 38821-38828. 

Kuang D, Yao Y, Wang M, Pattabiramann N, Kotra L, et al. 2003. Molecular similarities in the ligand binding pockets of an odorant receptor and the metabotropic glutamate receptors. J Biol Chem 278(43) 42551-42559. 

Yao Y, Pattabiraman N, Michne WE, Huang X-P, Hampson DR. 2003. Molecular modeling and mutagenesis of the ligand binding pocket of the mGluR3 subtype of metabotropic glutamate receptor. J Neurochem 86 947-957. 

FIGURE 5.6 A transmembrane olfactory receptor. The sections shown as cylinders reside in the cell wall. These are the seven transmembrane hydrophobic domains. Loops on top (and the N-terminus) are outside the cell, those at the bottom (and the C-terminus) are inside the cell. For clarity, the cylinders are spread out but, in the cell, they are bundled into a ligand-binding pocket. The residues shown as black dots are especially diverse among known odorant receptors. This diversity enables the receptor family to interact with many different odor molecules. (From Buck, 1996.)... 

Chikhi R, Sael L, Kihara D (2010) Real-time ligand binding pocket database search using local surface descriptors. Proteins 78 2007-2028... 

The scope of the AD was further broadened by the discovery that ally] 4-methoxy-benzoates are excellent substrates for this reaction [8]. The 4-methoxybenzoyl substituent is supposed to interact with the aryl groups of the ligand-binding pocket and to suppress acyl migration from... 

---