Related Experiment Video
Updated: Jun 21, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
Published on: August 29, 2015
Recent progress towards the identification of selective inhibitors of serine/threonine protein kinases
1Smithkline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA. Jerry_L_Adams@sbphrd.com
Abstract:
Protein serine/threonine kinases figure prominently among the molecular targets currently being pursued by the pharmaceutical industry. Given the conserved tertiary structure and catalytic mechanism of the mammalian kinase superfamily, it is not surprising that the discovery of selective inhibitors has proven to be difficult. However, in the last two years, progress has accelerated and approaches that target the ATP binding site and antisense RNA have matured to the point of advancing compounds into clinical trials. The development of a structural basis for understanding the selectivity of the pyridinylimidazole class of p38 MAP kinase inhibitors has been a major advance in this area.
Related Concept Videos
Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
The JAK-STAT Signaling Pathway
Protein-protein Interfaces

