Screening with X-rays

In the October Nature Biotechnology, Nienaber et al. demonstrate that drug or inhibitor leads can be identified by high throughput X-ray crystallography (Nat. Biotech. 2000, 18:1105-1108). Pre-formed protein crystals are soaked in solvents containing mixtures of 100 compounds before the crystals are examined by X-ray crystallography. Nienaber et al. look for changes in the electron-density map caused by ligand binding. The compounds in each mixture are chosen to be diverse in shape so that they

By | October 10, 2000

In the October Nature Biotechnology, Nienaber et al. demonstrate that drug or inhibitor leads can be identified by high throughput X-ray crystallography (Nat. Biotech. 2000, 18:1105-1108). Pre-formed protein crystals are soaked in solvents containing mixtures of 100 compounds before the crystals are examined by X-ray crystallography. Nienaber et al. look for changes in the electron-density map caused by ligand binding. The compounds in each mixture are chosen to be diverse in shape so that they can be differentiated readily, and the technique allows the site and orientation of binding to be identified. Nienaber et al. use this method to screen thousands of compounds per day in a successful search for a high affinity inhibitor of the anti-cancer target urokinase.

Advertisement

Popular Now

  1. The Meaning of Pupil Dilation
    Daily News The Meaning of Pupil Dilation

    Scientists are using pupil measurements to study a wide range of psychological processes and to get a glimpse into the mind.

  2. Exercise-Induced Muscle Factor Promotes Memory
  3. Illustrating #FieldworkFails
  4. Transmissible Cancers Plague Mollusks
Biosearch Technologies