Kinases and cancer drug targets

Protein kinases switch other proteins on and off by adding phosphate groups, and when they are stuck in the on position they can drive cancer. Imatinib (Gleevec), which blocks the BCR-ABL kinase in leukemia, showed that drugs designed against a specific kinase can work. This collection shows kinases with the drugs that target them, along with other famous cancer targets such as Ras, p53, MDM2, BCL-2 and PARP.

Open Protein kinase A with ATP and a peptide inhibitor in 3D

29 structures

• Protein kinase A with ATP and a peptide inhibitor1ATP
  PKA was the first protein kinase structure solved and became the model for the whole family.
• Mouse Abl kinase with imatinib (Gleevec)1IEP
• Human Abl kinase with imatinib2HYY
• Abl kinase with nilotinib3CS9
• Abl kinase with dasatinib2GQG
• KIT kinase with imatinib1T46
• EGFR kinase with erlotinib1M17
• EGFR kinase with lapatinib1XKK
• EGFR G719S mutant with gefitinib (Iressa)2ITO
• EGFR kinase with osimertinib4ZAU
• Cyclin A bound to cyclin-dependent kinase 21FIN
• BRAF V600E with vemurafenib3OG7
• BRAF V600E with dabrafenib4XV2
• BRAF with sorafenib1UWH
• BRAF bound to MEK14MNE
• ALK kinase with crizotinib2XP2
• BTK kinase with ibrutinib5P9J
• PI3K alpha lipid kinase with an inhibitor4JPS
• mTOR kinase4JSV
• H-Ras bound to a GTP analog5P21
• KRas bound to GDP4OBE
• KRas G12C with sotorasib (AMG 510)6OIM
  Sotorasib was the first approved drug to target a mutant Ras protein.
• MDM2 bound to a p53 peptide1YCR
• MDM2 with nutlin-3a4HG7
• BCL-2 with venetoclax6O0K
• PARP1 catalytic domain with olaparib7KK4
• Human ABL1 kinase (AlphaFold)P00519 (AlphaFold)
• Human BRAF kinase (AlphaFold)P15056 (AlphaFold)
• Human KRas (AlphaFold)P01116 (AlphaFold)

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