References
1. Manning G, Whyte DB, Martinez R, Hunter T, Sudarsanam S (2002) The protein kinase
complement of the human genome. Science 298:1912–1934
2. Roskoski R (2018) FDA-approved protein kinase inhibitors. http://www.brimr.org/PKI/PKIs.
htm
3. Monoclonal antibodies approved by the EMA and FDA for therapeutic use. http://www.actip.
org/products/monoclonal-antibodies-approved-by-the-ema-and-fda-for-therapeutic-use/
4. Giordano S (2008) Curr Med Chem 15:422–432
5. Serrano C, George S (2014) Recent advances in the treatment of gastrointestinal stromal tumors.
Ther Adv Med Oncol 6:115–127
6. Yan L, Rosen N, Arteaga C (2011) Targeted cancer therapies. Chin J Cancer 30:1–4
7. Jänne PA, Gray N, Settleman J (2009) Factors underlying sensitivity of cancers to smallmolecule kinase inhibitors. Nat Rev Drug Discov 8:709–723
8. Knight ZA, Shokat KM (2005) Features of selective kinase inhibitors. Chem Biol 12:621–637
9. Schwartz PA, Murray BW (2011) Protein kinase biochemistry and drug discovery. Bioorg
Chem 39:192–210
10. Morphy R (2010) Selectively nonselective kinase inhibition: striking the right balance. J Med
Chem 53:1413–1437
11. Zhao Y, Adjei AA (2014) The clinical development of MEK inhibitors. Nat Rev Clin Oncol
11:385–400
12. Vogelstein B, Papadopoulos N, Velculescu VE, Zhou S, Diaz Jr LA, Kinzler KW (2013)
Cancer genome landscapes. Science 339:1546–1558
13. Sullivan I, Planchard D (2017) Next-generation EGFR tyrosine kinase inhibitors for treating
EGFR-mutant lung Cancer beyond first line. Front Med. https://doi.org/10.3389/fmed.2016.
00076
14. Holderfield M, Deuker MM, McCormick F, McMahon M (2014) Targeting RAF kinases for
cancer therapy: BRAF mutated melanoma and beyond. Nat Rev Cancer 14:455–467
15. Knighton DR et al (1991) Crystal structure of the catalytic subunit of cyclic adenosine
monophosphate-dependent protein kinase. Science 253:407–414
16. Kornev AP, Haste NM, Taylor SS, Ten Eyck LF (2006) Surface comparison of active and
inactive protein kinases identifies a conserved activation mechanism. PNAS 103:17783–17788
17. McClendona CL, Kornevc AP, Gilsonb M, Taylor SS (2014) Dynamic architecture of a protein
kinase. PNAS 111:E4623–E4631
18. Brewer MR, Yun CH, Lai D, Lemmon MA, Eck MJ, Pao W (2013) Mechanism for activation of
mutated epidermal growth factor receptors in lung cancer. PNAS 110:E3595–E3604
19. Fratev FF, Jónsdóttir SO (2009) An in silico study of the molecular basis of B-RAF activation
and conformational stability. BMC Struct Biol 9:1–17
20. Echeverria I, Liu Y, Gabelli SB, Amzel LM (2015) Oncogenic mutations weaken the interactions that stabilize the p110a-p85a heterodimer in phosphatidylinositol 3-kinase α. FEBS J
282:3528–3542
21. Peng W, Thomas EN, Mads HC (2015) FDA-approved small-molecule kinase inhibitors.
Trends Pharmacol Sci 36:422–439
22. Wu P, Nielsen TE, Clausen MH (2016) Small-molecule kinase inhibitors: an analysis of
FDA-approved drugs. Drug Discov Today 21:5–10
23. Martin E, Mukherjee P (2012) Kinase-kernel models: accurate in silico screening of 4 million
compounds across the entire human kinome. J Chem Inf Model 52:156–170
24. Taylor SS, Kornev PA (2011) Protein kinases: evolution of dynamic regulatory proteins. Trends
Biochem Sci 36:65–77
25. Zarrinkar PP et al (2008) A quantitative analysis of kinase inhibitor selectivity. Nat Biotech
26:127–132
120
L. Schio and H. Minoux
1. Manning G, Whyte DB, Martinez R, Hunter T, Sudarsanam S (2002) The protein kinase
complement of the human genome. Science 298:1912–1934
2. Roskoski R (2018) FDA-approved protein kinase inhibitors. http://www.brimr.org/PKI/PKIs.
htm
3. Monoclonal antibodies approved by the EMA and FDA for therapeutic use. http://www.actip.
org/products/monoclonal-antibodies-approved-by-the-ema-and-fda-for-therapeutic-use/
4. Giordano S (2008) Curr Med Chem 15:422–432
5. Serrano C, George S (2014) Recent advances in the treatment of gastrointestinal stromal tumors.
Ther Adv Med Oncol 6:115–127
6. Yan L, Rosen N, Arteaga C (2011) Targeted cancer therapies. Chin J Cancer 30:1–4
7. Jänne PA, Gray N, Settleman J (2009) Factors underlying sensitivity of cancers to smallmolecule kinase inhibitors. Nat Rev Drug Discov 8:709–723
8. Knight ZA, Shokat KM (2005) Features of selective kinase inhibitors. Chem Biol 12:621–637
9. Schwartz PA, Murray BW (2011) Protein kinase biochemistry and drug discovery. Bioorg
Chem 39:192–210
10. Morphy R (2010) Selectively nonselective kinase inhibition: striking the right balance. J Med
Chem 53:1413–1437
11. Zhao Y, Adjei AA (2014) The clinical development of MEK inhibitors. Nat Rev Clin Oncol
11:385–400
12. Vogelstein B, Papadopoulos N, Velculescu VE, Zhou S, Diaz Jr LA, Kinzler KW (2013)
Cancer genome landscapes. Science 339:1546–1558
13. Sullivan I, Planchard D (2017) Next-generation EGFR tyrosine kinase inhibitors for treating
EGFR-mutant lung Cancer beyond first line. Front Med. https://doi.org/10.3389/fmed.2016.
00076
14. Holderfield M, Deuker MM, McCormick F, McMahon M (2014) Targeting RAF kinases for
cancer therapy: BRAF mutated melanoma and beyond. Nat Rev Cancer 14:455–467
15. Knighton DR et al (1991) Crystal structure of the catalytic subunit of cyclic adenosine
monophosphate-dependent protein kinase. Science 253:407–414
16. Kornev AP, Haste NM, Taylor SS, Ten Eyck LF (2006) Surface comparison of active and
inactive protein kinases identifies a conserved activation mechanism. PNAS 103:17783–17788
17. McClendona CL, Kornevc AP, Gilsonb M, Taylor SS (2014) Dynamic architecture of a protein
kinase. PNAS 111:E4623–E4631
18. Brewer MR, Yun CH, Lai D, Lemmon MA, Eck MJ, Pao W (2013) Mechanism for activation of
mutated epidermal growth factor receptors in lung cancer. PNAS 110:E3595–E3604
19. Fratev FF, Jónsdóttir SO (2009) An in silico study of the molecular basis of B-RAF activation
and conformational stability. BMC Struct Biol 9:1–17
20. Echeverria I, Liu Y, Gabelli SB, Amzel LM (2015) Oncogenic mutations weaken the interactions that stabilize the p110a-p85a heterodimer in phosphatidylinositol 3-kinase α. FEBS J
282:3528–3542
21. Peng W, Thomas EN, Mads HC (2015) FDA-approved small-molecule kinase inhibitors.
Trends Pharmacol Sci 36:422–439
22. Wu P, Nielsen TE, Clausen MH (2016) Small-molecule kinase inhibitors: an analysis of
FDA-approved drugs. Drug Discov Today 21:5–10
23. Martin E, Mukherjee P (2012) Kinase-kernel models: accurate in silico screening of 4 million
compounds across the entire human kinome. J Chem Inf Model 52:156–170
24. Taylor SS, Kornev PA (2011) Protein kinases: evolution of dynamic regulatory proteins. Trends
Biochem Sci 36:65–77
25. Zarrinkar PP et al (2008) A quantitative analysis of kinase inhibitor selectivity. Nat Biotech
26:127–132
120
L. Schio and H. Minoux