Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …

The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

INTRODUCTION Molecularly targeted drugs such as imatinib and crizotinib have
revolutionized the treatment of certain blood and lung cancers because of their remarkable …

Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1
oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have …

Cyclins and cyclin-dependent protein kinases (CDKs) are important proteins that are
required for the regulation and expression of the large number of components necessary for …

Because dysregulation and mutations of protein kinases play causal roles in human
disease, this family of enzymes has become one of the most important drug targets over the …

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 …

Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …

Highlights•A dramatic increase in the approval of small molecule kinase inhibitors
(SMKIs).•The molecular weight of most approved SMKIs is in the range of 400–600.•The …

ERK1 and ERK2 are key protein kinases that contribute to the Ras-Raf-MEK-ERK MAP
kinase signalling module. This pathway participates in the control of numerous processes …