Chemical probes are powerful reagents with increasing impacts on biomedical research.
However, probes of poor quality or that are used incorrectly generate misleading results. To …

Despite the success of protein kinase inhibitors as approved therapeutics, drug discovery
has focused on a small subset of kinase targets. Here we provide a thorough characterization …

Stimulation of resting CD4 + T lymphocytes leads to rapid proliferation and differentiation
into effector (Teff) or inducible regulatory (Treg) subsets with specific functions to promote or …

Ruthenium alkylidene 1 has been utilized in the tandem ring opening−ring closing metathesis
of cyclic olefins. This reaction produces a bicyclic molecule from a cyclic olefin. Reactivity …

Chemical probes are urgently needed to functionally annotate hitherto-untargeted kinases
and stimulate new drug discovery efforts to address unmet medical needs. The size of the …

A genomic signature designed to assess the activity of the estrogen-related receptor alpha (ERRα)
was used to profile more than 800 breast tumors, revealing a shorter disease-free …

Protein kinases are highly tractable targets for drug discovery. However, the biological
function and therapeutic potential of the majority of the 500+ human protein kinases remains …

The identification of nonporphyrin ligands for the orphan nuclear receptor Rev-erbα will
enable studies of its role as a heme sensor and regulator of metabolic and circadian signaling. …

X-ray crystal structures of the ligand binding domain (LBD) of the estrogen-related receptor-γ
(ERRγ) were determined that describe this receptor in three distinct states: unliganded, …

To catalyze research on historically untargeted protein kinases, we created the PKIS, an
annotated set of 367 small molecule kinase inhibitors. The set has been widely distributed to …