This animation illustrates how a small molecule binds to a protein. As a result of the binding, the protein alters its shape and becomes inactivated.
A molecular menagerie of small molecules is displayed, with two particular molecules singled out for attention: rapamycin and furrowstatin, which are discussed in the remainder of Dr. Schreiber's lectures on chemical genetics.
Microarray technology is useful for screening many small molecules at once. Automated devices have made it possible for thousands of different small molecules to be printed as an array of spots on a glass slide. A single type of protein which has been tagged with a fluorescent marker can then...
Rapamycin is a small molecule originally isolated from nature. It has antibiotic and immunosuppressive properties. It also allows two proteins which do not normally interact to bind together in the cell, which causes problems in the nutrient-sensing pathway.
After a chemical biologist has made many novel small molecules by diversity-oriented synthesis, the next step is to find those that are useful. Molecules need to be "screened." Conceptually, screening is like using proteins as a custom filter to catch potentially useful small molecules.
One technique for discovering small molecules of biological relevance is to expose cultured cells to a variety of small molecules and look for changes in the cells' appearance, behavior or other measurable qualities.
The hypothetical relationship of chemical space and biological space is plotted on a three-dimensional graph, giving a glimpse of the future direction of research at the intersections of various disciplines.
In diversity-oriented synthesis, many combinations of chemical building blocks undergo relatively few reaction steps to form a vast variety of different molecules. In this example, 45 x 45 x 45 combinations yield more than 88,000 novel molecules.