What is the example for transition state analogue?

Examples of drugs that are transition state analog inhibitors include flu medications such as the neuraminidase inhibitor oseltamivir and the HIV protease inhibitors saquinavir in the treatment of AIDS.

What is the purpose of transition state analogues?

Transition-state analogs have been used for generating catalytic antibodies, antibodies that catalyze chemical reactions. Enzymes lower activation energy and accelerate catalysis by tightly binding to the transition state.

Is transition state analog reversible?

6.1 Reversible Transition State Analog Inhibitors Peptidyl trifluoromethyl ketones are examples of reversible, transition state analog inhibitors of serine proteases.

Which of the following would be the characteristics of a good transition state analog for a serine protease?

What would be the characteristics of a good transition state analog for a serine protease? The analog would have a tetrahedral carbon. The analog would have oxygens or nitrogens to hydrogen-bond to the active site His residue and to other active site species.

What does it mean to bind a substrate in the transition state?

enzymes
By binding substrates to their active sites, enzymes stabilize the structure of the transition state. This in turn lowers of the free energy of the transition state, which in turn decreases the rate of the chemical reaction. Enzymes do not however change the Gibbs free energy of the chemical reaction.

Why are transition state analogs better than substrate analogs?

Transition state analogs typically bind to enzyme active sites much more tightly than substrate analogs because the enzyme binds the substrate in the transition state more strongly than one in the ground state, as explained by the thermodynamic cycle as previously described.

Are transition-state analogs stable?

The transition state structure has a lifetime on the fsec timescale and has equal probability of partitioning to reactant or product., Transition state analogue—a chemically stable molecule with features of bond lengths, angles and electron density at the van der Waals surface to resemble the actual transition state …