J. Richard CroutEnzymes As Targets for Drug DesignCrout JR (1989): Enzyme inhibitors as drugs. In: Enzymes as Targets for Drug Design , Palfreyman MG, McCann PP, Lovenberg W, Temple JG Jr and Sjoerdsma A, eds. San Diego: Academic Press....
The significance of enzymes as targets of drug action is discussed. New approaches to the rational design of enzyme inhibitors are characterized by a pronounced shift of emphasis toward the targets of drug action, as the structure and function of an increasing number of enzymes are described in ...
Design of suicide substrates: an approach to the development of highly selective enzyme inhibitors as drugs The concept that a pharmacologically important target enzyme can generate, via its normal catalytic mechanism, an irreversible inhibitor from an innocuous substrate analogue and hence commit suicide...
enzyme inhibitors repress an organism’s vital physiological functions. Many toxic substances, including pesticides, such nerve gases as lewisite, and such respiratory toxins as cyanides and hydrogen sulfide, have a toxic effect owing to the inhibition of enzymes, for example, the enzyme cholinesteras...
The majority of enzyme inhibitor drugs are reversible in that removal of the inhibitor (e.g., by dialysis) fully restores the enzymatic activity. Such inhibitors bind to their target enzyme through a combination of noncovalent interactions, such as hydrogen bonding or ionic, hydrophobic, and Van ...
The actions of many drugs involve enzyme inhibition. This is exemplified by the inhibitors of monoamine oxidases (MAO) and the cholinsterases (ChE) that have been used for several pharmacological purposes. This review describes key principles and approaches for the reliable determination of enzyme ...
Irreversible enzyme inhibitors have the ability to permanently change the structure of the protein, and the process cannot be undone. Reversible enzyme inhibition can temporarily block the action of an enzyme but will not be permanent in nature. This process can occur in a number of ways, ...
We propose a new molecular therapeutic strategy for genetic metabolic diseases of administering competitive inhibitors as 'chemical chaperons' at sub–inhibitory intracellular concentrations. This is a preview of subscription content, access via your institution Access options Subscription info for Chinese ...
Structure-based drug design and in vitro testing reveal new inhibitors of enoyl-acyl carrier protein reductases The need for new antibacterial agents is increasingly becoming of great importance as bacterial resistance to current drugs is quickly spreading. Enoyl-acy... Ghattas, Mohammad A.Eissa, Ne...
2.8.3Cardiovascular drugs Several groups ofcardiovascular drugsare commonly used for the therapeutic treatment ofheart disorders, such as beta-blockers [ATE,metoprolol(MET), PRP], angiotensin-converting-enzyme (ACE) inhibitors,angiotensin II receptor antagonists[sartans i.e.,Valsartan(VAL)] andcalcium...