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Determining Target Structure

Drugs bind targets. The structure of a drug and its target are therefore closely related. If one understands the structure of the target, then important elements of the drug can generally be inferred. For this reason, the discovery team seeks out as much information on [Pg.214]

This section deals exclusively with protein targets enzymes and receptors. Is not the structure of oligonucleotides also important It certainly is. The difference between proteins and oligonucleotides, especially DNA, is that proteins are far less predictable in terms of structure. An essentially universal structure like the double helix of DNA has no parallel in the world of proteins. Considerable research effort is expended on determining the three-dimensional structure of target proteins. [Pg.215]


For each key atom, i, in each reaction stage, j, determine the difference in oxidation number of that atom with respect to what it is in the final target structure. Hence,... [Pg.117]

Many of the more critical target structures in sabotage operations are made of steel. Plastic explosives are the best for steel cutting. They are easier to place and permit the use of a simple rule of thumb for determining the amount of explosive needed rather than working out a complicated mathematical formula. Also, if the proper techniques are used much less explosive is required to do the job than demolitions formulas call for. [Pg.24]

Historically, the major focus of peptidomimetic design has evolved from receptor-targeted drug discovery research and has not been directly impacted by an experimentally-determined 3D structure of... [Pg.563]

In 1991, we first introduced the one-bead one-compound (OBOC ) combinatorial library method.1 Since then, it has been successfully applied to the identification of ligands for a large number of biological targets.2,3 Using well-established on-bead binding or functional assays, the OBOC method is highly efficient and practical. A random library of millions of beads can be rapidly screened in parallel for a specific acceptor molecule (receptor, antibody, enzyme, virus, etc.). The amount of acceptor needed is minute compared to solution phase assay in microtiter plates. The positive beads with active compounds are easily isolated and subjected to structural determination. For peptides that contain natural amino acids and have a free N-terminus, we routinely use an automatic protein sequencer with Edman chemistry, which converts each a-amino acid sequentially to its phenylthiohydantoin (PTH) derivatives, to determine the structure of peptide on the positive beads. [Pg.271]

The primary method for determining protein structure is x-ray crystallography. Unfortunately, the receptors most frequently targeted by the pharmaceutical industry are embedded in cell membranes. The cell membrane plays a vital role in determining the overall shape of a membrane-bound receptor. Crystallization is performed in the absence of membrane lipids, so x-ray information is not representative of the true receptor structure. Therefore, reliable structural information on receptors is difficult to obtain. [Pg.95]


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Target structure

Target structure determination

Target structure determination

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