Abstract Phosphoinositide-dependent kinase-1 (PDK1) is a critical enzyme in the PI3K/AKT
pathway and to the activation of AGC family protein kinases, including S6K, SGK, and PKC …

In this work, we describe the use of the rule of 3 fragment-based strategies from biochemical
screening data of 1100 in-house, small, low molecular weight fragments. The sequential …

Fragment screening of phosphoinositide-dependent kinase-1 (PDK1) in a biochemical
kinase assay afforded hits that were characterized and prioritized based on ligand efficiency …

A dynamic, focused screening strategy that utilized a limited but diversified set of target-
specific compounds was explored as an efficient means for the identification of inhibitors of …

3-Phosphoinositide-dependent protein kinase-1 (PDK1) has been recognized as a
promising anticancer target. Thus, it is interesting to identify new inhibitors of PDK1 for …

In this Letter is described the structure-based design of potent dihydro-pyrazoloquinazolines
as PDK1 inhibitors. Starting from low potency HTS hits with the aid of X-ray crystallography …

Phosphoinositide-dependent protein kinase-1 (PDK1) is a master regulator of the AGC
family of kinases and an integral component of the PI3K/AKT/mTOR pathway. As this …

Warburg effect, a preference of aerobic glycolysis for energy production even in the
presence of adequate oxygen, is one of the most prominent distinctions of cancer cells from …

We report the use of a fragment-based lead discovery method, Tethering with extenders, to
discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With …

Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based
screening approach. Computational modeling of the fragments bound to the active site led to …