Medicinal Chemistry

the coenzyme can stabilize the anion by resonance delocalization on the heterocyclic ring (see figure 8.6). Additionally, flavin ...

8.2.2.1 Physicochemical Properties of Acetylcholinesterase The purification of AChE and the elucidation of its physicochemical p ...

As classical competitive enzyme inhibitors, they have a high affinity for the active site but are not substrates. The enzyme is ...

ACh receptors are destroyed by endocytosis via coated pits and proteolysis in lysosomes. In myasthenia gravis, the receptors are ...

disease. Dementia is a nonspecific term applied to any chronic, progressive, non-reversible neurodegenerative process that resul ...

inactive compounds; however, insects do not have the hydrolases that would deactivate the insecticide. Because of this double sa ...

8.2.3 Enzyme Targets: Adenosine Triphosphatase Adenosine triphosphatase (ATPase, E.C. 3.6.1.3) comprises a group of extremely wi ...

Na+–K+exchange, which occurs before each heart contraction. The inhibition of Na+ extrusion increases the Na+concentration, whic ...

The activity of a compound depends to a very great extent on the position of the 23-carbonyl oxygen, which is held quite rigidl ...

In the red blood cell this reaction plays an important role in CO 2 transport from the tissues to the lungs. In the kidney, the ...

they are much weaker carbonic anhydrase inhibitors than acetazolamide, and may have another mode of action in addition to carbon ...

It was previously thought that 5-FU inhibits the enzyme by classical competitive inhibition. However, it was found that 5-FU is ...

orienting the amino group of the substrate and decreasing the energy of the transition state. Monoamine oxidase has some importa ...

Propargylamines.The propargylamines are Kcatinhibitors or suicide substrates of MAO, forming covalent derivatives with the flavi ...

protein molecule—to control the activity of its catalytic subunit. Not surprisingly, kinases are widely studied as druggable tar ...

There are some conditions, such as cancer, in which it would be desirable to “turn on” apoptosis, hastening the death of the mal ...

502 Table 8.2 Caspases Relevant to Drug Design Caspace Alternate nonmenclature Function Substrates Caspase-1 ICE Processing of i ...

from one of the procaspase units of the homodimer, and a small unit from the other procaspase. The activated caspases kill cells ...

juice to its sailors to prevent scurvy. (This is the origin of the slang word “limey” for the British.) The use of fish-liver oi ...

the vitamin, with the result that FAD carries a pair of electrons and two hydrogens. The monoamine oxidases (see section 8.2.6) ...