The clinical and commercial success of covalent drugs has prompted a renewed and more
deliberate pursuit of covalent and irreversible mechanisms within drug discovery. A covalent …

Covalent drugs haveproved to be successful therapies for various indications, but largely
owing to safety concerns, they are rarely considered when initiating a target-directed drug …

The development of therapies for the treatment of neurological cancer faces a number of
major challenges including the synthesis of small molecule agents that can penetrate the …

Much of drug discovery today is predicated on the concept of selective targeting of particular
bioactive macromolecules by low-molecular-mass drugs. The binding of drugs to their …

Failure due to poor in vivo efficacy is a primary contributor to attrition during the development
of new chemotherapeutics. Lead optimization programs that in their quest for efficacy focus …

In the relatively young but expanding field of irreversible kinase inhibitor drug discovery,
there are two main developments that are of central importance. First, the patients have …

Malarial dihydrofolate reductase (DHFR) is the target of antifolate antimalarial drugs such as
pyrimethamine and cycloguanil, the clinical efficacy of which have been compromised by …

Although NAD+ biosynthesis is required for Sir2 functions and replicative lifespan in yeast,
alterations in NAD+ precursors have been reported to accelerate aging but not to extend …

Experimental analysis of enzymatic transition-state structures uses kinetic isotope effects
(KIEs) to report on bonding and geometry differences between reactants and the transition …

This book provides the" nuts and bolts" background for a successful study of carbohydrates-
the essential molecules that not only give you energy, but are an integral part of many …