Kinase chemogenomics: targeting the human kinome for target validation and drug discovery.
Chemogenomics is a gene family-based approach to drug discovery and target validation. This review will summarize the application of this interdisciplinary approach to the protein kinases of the human genome with emphasis upon the synergies and efficiencies to be gained. Specific examples from the SAPK-family will be discussed.
ter Haar
E
E
Vertex Pharmaceuticals, Inc., 130 Waverly Street, Cambridge, Massachusetts 02139, USA. Harbeson@vpharm.com
Walters
W P
WP
Pazhanisamy
S
S
Taslimi
P
P
Pierce
A C
AC
Bemis
G W
GW
Salituro
F G
FG
Harbeson
S L
SL
D001665:Binding Sites; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry*; D015894:Genome, Human; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D010597:Pharmacogenetics; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000737:chemistry / Q000235:genetics; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D008024:Ligands; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases