Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

In contrast to the traditional mechanism of drug action that relies on the reversible,
noncovalent interaction of a ligand with its biological target, a targeted covalent inhibitor …

In the history of therapeutics, covalent drugs occupy a very distinct category. While
representing a significant fraction of the drugs on the market, very few have been …

Highlights•Summarized the diverse types of warheads across the human
kinome.•Highlighted facile covalent reactive functional groups which bind protein …

CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-
transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability …

We combine molecular dynamics, statistical mechanics, and hybrid quantum
mechanics/molecular mechanics simulations to describe mechanistically the severe acute …

The calmodulin-activated α-kinase, eukaryotic elongation factor 2 kinase (eEF-2K), serves
as a master regulator of translational elongation by specifically phosphorylating and …

Eukaryotic elongation factor-2 kinase (eEF-2K) is an unusual alpha kinase commonly
upregulated in various human cancers, including breast, pancreatic, lung, and brain tumors …

Abweichend vom üblichen Arzneimittelwirkmechanismus einer reversiblen, nichtkovalenten
Wechselwirkung eines Liganden mit seinem biologischen Zielmolekül wird ein …

The α-kinase, eEF2K, phosphorylates the threonine 56 residue of eEF2 to inhibit global
peptide elongation (protein translation). As a master regulator of protein synthesis, in …