Kinase inhibition through Ready-to-go cell lines

Overview of the kinase family

Kinases are a large family of enzymes with over 500 encoded in the human genome and all share a highly conserved kinase domain. Dependent on the substrate they act upon they can be broadly classified into 3 categories: protein kinases, carbohydrate kinases and lipid kinases. Due to the diverse roles that kinases play in the cell they are implicated in a number of diseases including cancer:

Protein kinases

• can phosphorylate substrate proteins on serine, threonine, tyrosines or histidine residues. Mitogen-activated protein kinases such as RAF kinases involved in the MAPK signaling pathways and cyclin dependent kinases (CDKs) involved in cell cycle regulation are prime examples of pathways implicated in cancers.

Lipid kinases

• alter the localization and reactivity of lipids through phosphorylation. A well-known example of a lipid kinase is phosphoinositide 3-kinase which is implicated in a number of cancers, mainly through alterations to its catalytic subunit - PIK3CA.

Carbohydrate kinases

• such as hexokinase play important roles in the majority of metabolic pathways.
• Available knockout cell lines

Examples of available knockouts by kinase sub-family

AGC Subfamily

CAMK Subfamily

CK1 Subfamily

CMGC Subfamily

STE Subfamily

TK Subfamily

TKL Subfamily