The BRAF kinase is mutated, typically Val 600→Glu (V600E), to induce an active oncogenic
state in a large fraction of melanomas, thyroid cancers, hairy cell leukaemias and, to a …

Cullin-RING ligases are multisubunit E3 ubiquitin ligases that recruit substrate-specific
adaptors to catalyze protein ubiquitylation. Cul3-based Cullin-RING ligases are uniquely …

Protein kinases have emerged as one of the most successful families of drug targets. To
date, most selective kinase inhibitors have been discovered serendipitously either through …

Growth factor signaling pathways are tightly regulated by phosphorylation and include many
important kinase targets of interest for drug discovery. Small molecule inhibitors of the bone …

Activation of the ERK pathway is a hallmark of cancer, and targeting of upstream signaling
partners led to the development of approved drugs. Recently, SCH772984 has been shown to …

Bone morphogenetic protein (BMP) receptor kinases are tightly regulated to control development
and tissue homeostasis. Mutant receptor kinase domains escape regulation leading to …

Drugs that function through covalent bond formation represent a considerable fraction of our
repository of effective medicines but safety concerns and the complexity of developing …

Bromodomains are acetyl-lysine specific protein interaction domains that have recently emerged
as a new target class for the development of inhibitors that modulate gene transcription. …

p38α mitogen-activated protein kinase (p38α) is activated by a variety of mechanisms,
including autophosphorylation initiated by TGFβ-activated kinase 1 binding protein 1 (TAB1) …

The protein kinase DYRK1A has been suggested to act as one of the intracellular regulators
contributing to neurological alterations found in individuals with Down syndrome. For an …