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Volumn 6, Issue 5, 2014, Pages 515-527

Potential strategies for increasing drug-discovery productivity

Author keywords

[No Author keywords available]

Indexed keywords

ABIRATERONE ACETATE; BEDAQUILINE; BOCEPREVIR; CABOZANTINIB; CRIZOTINIB; CROFELEMER; GEFITINIB; HOMOHARRINGTONINE; ICATIBANT; IMATINIB; INGENOL MEBUTATE; IVACAFTOR; LINACLOTIDE; LOMITAPIDE; LORCASERIN; MARAVIROC; MIRABEGRON; PERAMPANEL; PLERIXAFOR; RETIGABINE; ROFLUMILAST; RUXOLITINIB; TERIFLUNOMIDE; VEMURAFENIB; VISMODEGIB;

EID: 84896947917     PISSN: 17568919     EISSN: 17568927     Source Type: Journal    
DOI: 10.4155/fmc.14.7     Document Type: Review
Times cited : (20)

References (87)
  • 2
    • 84866739808 scopus 로고    scopus 로고
    • Drug discovery in pharmaceutical industry: Productivity challenges and trends
    • Khanna I. Drug discovery in pharmaceutical industry: productivity challenges and trends. Drug Discov. Today 17(19-20), 1088-1102 (2012).
    • (2012) Drug Discov. Today , vol.17 , Issue.19-20 , pp. 1088-1102
    • Khanna, I.1
  • 4
    • 34447561049 scopus 로고    scopus 로고
    • Why has R and D productivity declined in the pharmaceutical industry?
    • Ruffolo RR. Why has R and D productivity declined in the pharmaceutical industry? Expert Opin. Drug Discov. 1(2), 99-102 (2006).
    • (2006) Expert Opin. Drug Discov. , vol.1 , Issue.2 , pp. 99-102
    • Ruffolo, R.R.1
  • 5
    • 77649234756 scopus 로고    scopus 로고
    • How to improve R and D productivity: The pharmaceutical industrys grand challenge
    • Paul SM, Mytelka DS, Dunwiddie CT et al. How to improve R and D productivity: the pharmaceutical industrys grand challenge. Nat. Rev. Drug Discov. 9(3), 203-214 (2010). n Gives an economic model of R and D productivity based on comprehensive, industry-wide data.
    • (2010) Nat. Rev. Drug Discov. , vol.9 , Issue.3 , pp. 203-214
    • Paul, S.M.1    Mytelka, D.S.2    Dunwiddie, C.T.3
  • 6
    • 84860690620 scopus 로고    scopus 로고
    • Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival
    • Morgan P, Van Der Graaf PH, Arrowsmith J et al. Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival. Drug Discov. Today 17(9-10), 419-424 (2012).
    • (2012) Drug Discov. Today , vol.17 , Issue.9-10 , pp. 419-424
    • Morgan, P.1    Van Der Graaf, P.H.2    Arrowsmith, J.3
  • 7
    • 44649123594 scopus 로고    scopus 로고
    • A case study of lean drug discovery: From project driven research to innovation studios and process factories
    • Ullman F, Boutellier R. A case study of lean drug discovery: from project driven research to innovation studios and process factories. Drug Discov. Today 13(11-12), 543-550 (2008).
    • (2008) Drug Discov. Today , vol.13 , Issue.11-12 , pp. 543-550
    • Ullman, F.1    Boutellier, R.2
  • 8
    • 67349164247 scopus 로고    scopus 로고
    • Making medicinal chemistry more effective - Application of Lean Sigma to improve processes, speed and quality
    • Andersson S, Armstrong A, Bjore A et al. Making medicinal chemistry more effective - application of Lean Sigma to improve processes, speed and quality. Drug Discov. Today 14(11-12), 598-604 (2009).
    • (2009) Drug Discov. Today , vol.14 , Issue.11-12 , pp. 598-604
    • Andersson, S.1    Armstrong, A.2    Bjore, A.3
  • 9
    • 84863393476 scopus 로고    scopus 로고
    • Hypothesis driven drug design: Improving quality and effectiveness of the design-make- test-analyze cycle
    • Plowright AT, Johnstone C, Kihlberg J, Pettersson J, Robb G, Thompson RA. Hypothesis driven drug design: improving quality and effectiveness of the design-make- test-analyze cycle. Drug Discov. Today 17(1-2), 56-62 (2012).
    • (2012) Drug Discov. Today , vol.17 , Issue.1-2 , pp. 56-62
    • Plowright, A.T.1    Johnstone, C.2    Kihlberg, J.3    Pettersson, J.4    Robb, G.5    Thompson, R.A.6
  • 10
    • 84868123881 scopus 로고    scopus 로고
    • What is the most important approach in current drug discovery: Doing the right things or doing things right?
    • Elebring T, Gill A, Plowright AT. What is the most important approach in current drug discovery: doing the right things or doing things right? Drug Discov. Today 17(21-22), 1166-1169 (2012).
    • (2012) Drug Discov. Today , vol.17 , Issue.21-22 , pp. 1166-1169
    • Elebring, T.1    Gill, A.2    Plowright, A.T.3
  • 11
    • 78651365936 scopus 로고    scopus 로고
    • Creativity, innovation and lean sigma: A controversial combination?
    • Johnstone C, Pairaudeau G, Pettersson JA. Creativity, innovation and lean sigma: a controversial combination? Drug Discov. Today 16(1-2), 50-57 (2011).
    • (2011) Drug Discov. Today , vol.16 , Issue.1-2 , pp. 50-57
    • Johnstone, C.1    Pairaudeau, G.2    Pettersson, J.A.3
  • 13
    • 12344297509 scopus 로고    scopus 로고
    • Drug discovery information integration: Virtual humans for pharmacokinetics
    • Leahy DE. Drug discovery information integration: virtual humans for pharmacokinetics. Drug Discov. Today 2(2), 78-84 (2004).
    • (2004) Drug Discov. Today , vol.2 , Issue.2 , pp. 78-84
    • Leahy, D.E.1
  • 14
    • 84861620361 scopus 로고    scopus 로고
    • Medicinal chemistry matters - A call for discipline in our discipline
    • Johnstone C. Medicinal chemistry matters - a call for discipline in our discipline. Drug Discov. Today 17(11-12), 538-543 (2012).
    • (2012) Drug Discov. Today , vol.17 , Issue.11-12 , pp. 538-543
    • Johnstone, C.1
  • 15
    • 13844276627 scopus 로고    scopus 로고
    • Target-based drug discovery: Is something wrong?
    • Sams-Dodd F. Target-based drug discovery: is something wrong? Drug Discov. Today 10(2), 139-147 (2005).
    • (2005) Drug Discov. Today , vol.10 , Issue.2 , pp. 139-147
    • Sams-Dodd, F.1
  • 16
    • 84874732406 scopus 로고    scopus 로고
    • Is poor research the cause of the declining productivity of the pharmaceutical industry? An industry in need of a paradigm shift
    • Sams-Dodd F. Is poor research the cause of the declining productivity of the pharmaceutical industry? An industry in need of a paradigm shift. Drug Discov. Today 18(5-6), 211-217 (2013).
    • (2013) Drug Discov. Today , vol.18 , Issue.5-6 , pp. 211-217
    • Sams-Dodd, F.1
  • 17
    • 29144508395 scopus 로고    scopus 로고
    • Finding new drug targets in the 21st century
    • Lindsay MA. Finding new drug targets in the 21st century. Drug Discov. Today 10(23-24), 1683-1687 (2005).
    • (2005) Drug Discov. Today , vol.10 , Issue.23-24 , pp. 1683-1687
    • Lindsay, M.A.1
  • 18
    • 33646517064 scopus 로고    scopus 로고
    • Drug discovery: Selecting the optimal approach
    • Sams-Dodd F. Drug discovery: selecting the optimal approach. Drug Discov. Today 11(9-10), 465-472 (2006).
    • (2006) Drug Discov. Today , vol.11 , Issue.9-10 , pp. 465-472
    • Sams-Dodd, F.1
  • 19
    • 79959929769 scopus 로고    scopus 로고
    • How were new medicines discovered?
    • Swinney DC, Anthony J. How were new medicines discovered? Nat. Rev. Drug Discov. 10(7), 507-519 (2011).
    • (2011) Nat. Rev. Drug Discov. , vol.10 , Issue.7 , pp. 507-519
    • Swinney, D.C.1    Anthony, J.2
  • 20
    • 36549010477 scopus 로고    scopus 로고
    • Unfinished business: Target-based drug discovery
    • Brown D. Unfinished business: target-based drug discovery. Drug Discov. Today 12(23-24), 1007-1012 (2007).
    • (2007) Drug Discov. Today , vol.12 , Issue.23-24 , pp. 1007-1012
    • Brown, D.1
  • 21
    • 33646467664 scopus 로고    scopus 로고
    • Strategies to optimize the validity of disease models in the drug discovery process
    • Sams-Dodd F. Strategies to optimize the validity of disease models in the drug discovery process. Drug Discov. Today 11(7-8), 355-363 (2006).
    • (2006) Drug Discov. Today , vol.11 , Issue.7-8 , pp. 355-363
    • Sams-Dodd, F.1
  • 22
    • 84861490509 scopus 로고    scopus 로고
    • Modern phenotypic drug discovery is a viable, neoclassic pharma strategy
    • Lee JA, Uhlik MT, Moxham CM, Tomandl D, Sall DJ. Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. J. Med. Chem. 55(10), 4527-4538 (2012).
    • (2012) J. Med. Chem. , vol.55 , Issue.10 , pp. 4527-4538
    • Lee, J.A.1    Uhlik, M.T.2    Moxham, C.M.3    Tomandl, D.4    Sall, D.J.5
  • 23
    • 0028605318 scopus 로고
    • A protein kinase involved in the regulation of inflammatory cytokine biosynthesis
    • Lee JC, Laydon JT, McDonnell PC et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature 372(6508), 739-746 (1994).
    • (1994) Nature , vol.372 , Issue.6508 , pp. 739-746
    • Lee, J.C.1    Laydon, J.T.2    McDonnell, P.C.3
  • 24
    • 17044373269 scopus 로고    scopus 로고
    • Finding the target after screening the phenotype
    • Hart CP. Finding the target after screening the phenotype. Drug Discov. Today 10(7), 513-519 (2005).
    • (2005) Drug Discov. Today , vol.10 , Issue.7 , pp. 513-519
    • Hart, C.P.1
  • 25
    • 84875458314 scopus 로고    scopus 로고
    • Target identification and mechanism of action in chemical biology and drug discovery
    • Schenone M, Dancik V, Wagner BK, Clemons PA. Target identification and mechanism of action in chemical biology and drug discovery. Nat. Chem. Biol. 9(4), 232-240 (2013).
    • (2013) Nat. Chem. Biol. , vol.9 , Issue.4 , pp. 232-240
    • Schenone, M.1    Dancik, V.2    Wagner, B.K.3    Clemons, P.A.4
  • 26
    • 84874630073 scopus 로고    scopus 로고
    • Target identification for small bioactive molecules: Finding the needle in the haystack
    • Ziegler S, Pries V, Hedberg C, Waldmann H. Target identification for small bioactive molecules: finding the needle in the haystack. Angew. Chem. Int. Ed. 52(10), 2744-2792 (2013).
    • (2013) Angew. Chem. Int. Ed. , vol.52 , Issue.10 , pp. 2744-2792
    • Ziegler, S.1    Pries, V.2    Hedberg, C.3    Waldmann, H.4
  • 27
    • 79958078949 scopus 로고    scopus 로고
    • Discovery and characterization of small molecule inhibitors of the BET family bromodomains
    • Chung CW, Coste H, White JH et al. Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J. Med. Chem. 54(11), 3827-3838 (2011).
    • (2011) J. Med. Chem. , vol.54 , Issue.11 , pp. 3827-3838
    • Chung, C.W.1    Coste, H.2    White, J.H.3
  • 28
    • 68949119585 scopus 로고    scopus 로고
    • The topology of drug-target interaction networks: Implicit dependence on drug properties and target families
    • Mestres J, Gregori-Puigjane E, Valverde S, Sole RV. The topology of drug-target interaction networks: implicit dependence on drug properties and target families. Mol. Biosyst. 5(9), 1051-1057 (2009).
    • (2009) Mol. Biosyst. , vol.5 , Issue.9 , pp. 1051-1057
    • Mestres, J.1    Gregori-Puigjane, E.2    Valverde, S.3    Sole, R.V.4
  • 29
    • 84876933802 scopus 로고    scopus 로고
    • Shifting from the single to the multitarget paradigm in drug discovery
    • Medina-Franco JL, Giulianotti MA, Welmaker GS, Houghten RA. Shifting from the single to the multitarget paradigm in drug discovery. Drug Discov. Today 18(9-10), 495-501 (2013).
    • (2013) Drug Discov. Today , vol.18 , Issue.9-10 , pp. 495-501
    • Medina-Franco, J.L.1    Ma, G.2    Welmaker, G.S.3    Houghten, R.A.4
  • 30
    • 84877947846 scopus 로고    scopus 로고
    • Human disease and drug pharmacology, complex as real life
    • Viayna E, Sola I, Di Pietro O, Munoz-Torrero D. Human disease and drug pharmacology, complex as real life. Curr. Med. Chem. 20(13), 1623-1634 (2013).
    • (2013) Curr. Med. Chem. , vol.20 , Issue.13 , pp. 1623-1634
    • Viayna, E.1    Sola, I.2    Di Pietro, O.3    Munoz-Torrero, D.4
  • 31
    • 27144443099 scopus 로고    scopus 로고
    • Drug discovery: Playing dirty
    • Frantz S. Drug discovery: playing dirty. Nature 437(7061), 942-943 (2005).
    • (2005) Nature , vol.437 , Issue.7061 , pp. 942-943
    • Frantz, S.1
  • 33
    • 35148824614 scopus 로고    scopus 로고
    • Network pharmacology
    • Hopkins AL. Network pharmacology. Nat. Biotechnol. 25(10), 1110-1111 (2007).
    • (2007) Nat. Biotechnol. , vol.25 , Issue.10 , pp. 1110-1111
    • Hopkins, A.L.1
  • 34
    • 54249155522 scopus 로고    scopus 로고
    • Network pharmacology: The next paradigm in drug discovery
    • Hopkins AL. Network pharmacology: the next paradigm in drug discovery. Nat. Chem. Biol. 4(11), 682-690 (2008).
    • (2008) Nat. Chem. Biol. , vol.4 , Issue.11 , pp. 682-690
    • Hopkins, A.L.1
  • 35
    • 77955333346 scopus 로고    scopus 로고
    • Rational approaches to targeted polypharmacology: Creating and navigating protein-ligand interaction networks
    • Metz JT, Hajduk PJ. Rational approaches to targeted polypharmacology: creating and navigating protein-ligand interaction networks. Curr. Opin. Chem. Biol. 14(4), 498-504 (2010).
    • (2010) Curr. Opin. Chem. Biol. , vol.14 , Issue.4 , pp. 498-504
    • Metz, J.T.1    Hajduk, P.J.2
  • 36
    • 84867338003 scopus 로고    scopus 로고
    • Discovery and preclinical validation of drug indications using compendia of public gene expression data
    • Sirota M, Dudley JT, Kim J et al. Discovery and preclinical validation of drug indications using compendia of public gene expression data. Sci. Transl. Med. 3(96), 96ra77 (2011).
    • (2011) Sci. Transl. Med. , vol.3 , Issue.96
    • Sirota, M.1    Dudley, J.T.2    Kim, J.3
  • 38
    • 77954052283 scopus 로고    scopus 로고
    • Systems approaches to polypharmacology and drug discovery
    • Boran AD, Iyengar R. Systems approaches to polypharmacology and drug discovery. Curr. Opin. Drug Discov. Devel. 13(3), 297-309 (2010).
    • (2010) Curr. Opin. Drug Discov. Devel. , vol.13 , Issue.3 , pp. 297-309
    • Boran, A.D.1    Iyengar, R.2
  • 39
    • 84855882587 scopus 로고    scopus 로고
    • Novel computational approaches to polypharmacology as a means to define responses to individual drugs
    • Xie L, Xie L, Kinnings SL, Bourne PE. Novel computational approaches to polypharmacology as a means to define responses to individual drugs. Annu. Rev. Pharmacol. Toxicol. 52, 361-379 (2012).
    • (2012) Annu. Rev. Pharmacol. Toxicol. , vol.52 , pp. 361-379
    • Xie, L.1    Xie, L.2    Kinnings, S.L.3    Bourne, P.E.4
  • 41
    • 27144449695 scopus 로고    scopus 로고
    • Designed multiple ligands. An emerging drug discovery paradigm
    • Morphy R, Rankovic Z. Designed multiple ligands. An emerging drug discovery paradigm. J. Med. Chem. 48(21), 6523-6543 (2005).
    • (2005) J. Med. Chem. , vol.48 , Issue.21 , pp. 6523-6543
    • Morphy, R.1    Rankovic, Z.2
  • 42
    • 65549171659 scopus 로고    scopus 로고
    • Designing multiple ligands - Medicinal chemistry strategies and challenges
    • Morphy R, Rankovic Z. Designing multiple ligands - medicinal chemistry strategies and challenges. Curr. Pharm. Des. 15(6), 587-600 (2009).
    • (2009) Curr. Pharm. Des. , vol.15 , Issue.6 , pp. 587-600
    • Morphy, R.1    Rankovic, Z.2
  • 43
    • 33746862160 scopus 로고    scopus 로고
    • The physicochemical challenges of designing multiple ligands
    • Morphy R, Rankovic Z. The physicochemical challenges of designing multiple ligands. J. Med. Chem. 49(16), 4961-4970 (2006).
    • (2006) J. Med. Chem. , vol.49 , Issue.16 , pp. 4961-4970
    • Morphy, R.1    Rankovic, Z.2
  • 44
    • 79951997039 scopus 로고    scopus 로고
    • THRX-198321 is a bifunctional muscarinic receptor antagonist and beta2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent manner
    • Steinfeld T, Hughes AD, Klein U, Smith JA, Mammen M. THRX-198321 is a bifunctional muscarinic receptor antagonist and beta2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent manner. Mol. Pharmacol. 79(3), 389-399 (2011).
    • (2011) Mol. Pharmacol. , vol.79 , Issue.3 , pp. 389-399
    • Steinfeld, T.1    Hughes, A.D.2    Klein, U.3    Smith, J.A.4    Mammen, M.5
  • 45
    • 77649204688 scopus 로고    scopus 로고
    • Selectively nonselective kinase inhibition: Striking the right balance
    • Morphy R. Selectively nonselective kinase inhibition: striking the right balance. J. Med. Chem. 53(4), 1413-1437 (2010).
    • (2010) J. Med. Chem. , vol.53 , Issue.4 , pp. 1413-1437
    • Morphy, R.1
  • 46
    • 33749238553 scopus 로고    scopus 로고
    • Discovery and development of sorafenib: A multikinase inhibitor for treating cancer
    • Wilhelm S, Carter C, Lynch M et al. Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat. Rev. Drug Discov. 5(10), 835-844 (2006).
    • (2006) Nat. Rev. Drug Discov. , vol.5 , Issue.10 , pp. 835-844
    • Wilhelm, S.1    Carter, C.2    Lynch, M.3
  • 47
    • 84859124139 scopus 로고    scopus 로고
    • Crizotinib: A novel and first-in-class multitargeted tyrosine kinase inhibitor for the treatment of anaplastic lymphoma kinase rearranged non-small cell lung cancer and beyond
    • Ou SH. Crizotinib: a novel and first-in-class multitargeted tyrosine kinase inhibitor for the treatment of anaplastic lymphoma kinase rearranged non-small cell lung cancer and beyond. Drug Des. Devel. Ther. 5, 471-485 (2011).
    • (2011) Drug Des. Devel. Ther. , vol.5 , pp. 471-485
    • Ou, S.H.1
  • 48
    • 70449634957 scopus 로고    scopus 로고
    • Predicting new molecular targets for known drugs
    • Keiser MJ, Setola V, Irwin JJ et al. Predicting new molecular targets for known drugs. Nature 462(7270), 175-181 (2009).
    • (2009) Nature , vol.462 , Issue.7270 , pp. 175-181
    • Keiser, M.J.1    Setola, V.2    Irwin, J.J.3
  • 50
    • 33646122469 scopus 로고    scopus 로고
    • Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: Mechanisms leading to optimal efficacy and safety
    • Swinney DC. Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and safety. Curr. Top. Med. Chem. 6(5), 461-478 (2006).
    • (2006) Curr. Top. Med. Chem. , vol.6 , Issue.5 , pp. 461-478
    • Swinney, D.C.1
  • 51
    • 0033797928 scopus 로고    scopus 로고
    • Comparative pharmacodynamics and pharmacokinetics of candesartan and losartan in man
    • Fuchs B, Breithaupt-Grogler K, Belz GG et al. Comparative pharmacodynamics and pharmacokinetics of candesartan and losartan in man. J. Pharm. Pharmacol. 52(9), 1075-1083 (2000).
    • (2000) J. Pharm. Pharmacol. , vol.52 , Issue.9 , pp. 1075-1083
    • Fuchs, B.1    Breithaupt-Grogler, K.2    Belz, G.G.3
  • 52
    • 33748325882 scopus 로고    scopus 로고
    • Drug-target residence time and its implications for lead optimization
    • Copeland RA, Pompliano DL, Meek TD. Drug-target residence time and its implications for lead optimization. Nat. Rev. Drug Discov. 5(9), 730-739 (2006).
    • (2006) Nat. Rev. Drug Discov. , vol.5 , Issue.9 , pp. 730-739
    • Copeland, R.A.1    Pompliano, D.L.2    Meek, T.D.3
  • 53
    • 77955329488 scopus 로고    scopus 로고
    • Drug-target residence time: Critical information for lead optimization
    • Lu H, Tonge PJ. Drug-target residence time: critical information for lead optimization. Curr. Opin. Chem. Biol. 14(4), 467-474 (2010).
    • (2010) Curr. Opin. Chem. Biol. , vol.14 , Issue.4 , pp. 467-474
    • Lu, H.1    Tonge, P.J.2
  • 54
    • 84877785836 scopus 로고    scopus 로고
    • A comprehensive analysis of the influence of drug binding kinetics on drug action at molecular and systems levels
    • Yin N, Pei J, Lai L. A comprehensive analysis of the influence of drug binding kinetics on drug action at molecular and systems levels. Mol. BioSyst. 9, 1381-1389 (2013).
    • (2013) Mol. BioSyst. , vol.9 , pp. 1381-1389
    • Yin, N.1    Pei, J.2    Lai, L.3
  • 55
    • 84859388604 scopus 로고    scopus 로고
    • Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target
    • Miller DC, Lunn G, Jones P, Sabnis Y, Davies NL, Driscoll P. Investigation of the effect of molecular properties on the binding kinetics of a ligand to its biological target. Med. Chem. Commun. 3, 449-452 (2012).
    • (2012) Med. Chem. Commun. , vol.3 , pp. 449-452
    • Miller, D.C.1    Lunn, G.2    Jones, P.3    Sabnis, Y.4    Davies, N.L.5    Driscoll, P.6
  • 56
    • 84880148746 scopus 로고    scopus 로고
    • Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics
    • Jin M, Petronella BA, Cooke A et al. Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics. ACS Med. Chem. Lett. 4(7), 627-631 (2013).
    • (2013) ACS Med. Chem. Lett. , vol.4 , Issue.7 , pp. 627-631
    • Jin, M.1    Petronella, B.A.2    Cooke, A.3
  • 58
    • 21144439000 scopus 로고    scopus 로고
    • Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib
    • Kwak EL, Sordella R, Bell DW et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc. Natl Acad. Sci. USA 102(21), 7665-7670 (2005).
    • (2005) Proc. Natl Acad. Sci. USA , vol.102 , Issue.21 , pp. 7665-7670
    • Kwak, E.L.1    Sordella, R.2    Bell, D.W.3
  • 59
    • 84867621201 scopus 로고    scopus 로고
    • Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker
    • Solca F, Dahl G, Zoephel A et al. Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker. J. Pharmacol. Exp. Ther. 343(2), 342-350 (2012).
    • (2012) J. Pharmacol. Exp. Ther. , vol.343 , Issue.2 , pp. 342-350
    • Solca, F.1    Dahl, G.2    Zoephel, A.3
  • 61
    • 15744391870 scopus 로고    scopus 로고
    • The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor
    • Watson C, Jenkinson S, Kazmierski W, Kenakin T. The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. Mol. Pharmacol. 67(4), 1268-1282 (2005).
    • (2005) Mol. Pharmacol. , vol.67 , Issue.4 , pp. 1268-1282
    • Watson, C.1    Jenkinson, S.2    Kazmierski, W.3    Kenakin, T.4
  • 62
    • 28244469774 scopus 로고    scopus 로고
    • Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human
    • Napier C, Sale H, Mosley M et al. Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human. Biochem. Pharmacol. 71(1-2), 163-172 (2005).
    • (2005) Biochem. Pharmacol. , vol.71 , Issue.1-2 , pp. 163-172
    • Napier, C.1    Sale, H.2    Mosley, M.3
  • 63
    • 46849116601 scopus 로고    scopus 로고
    • Putative allosteric MEK1 and MEK2 inhibitors
    • Price S. Putative allosteric MEK1 and MEK2 inhibitors. Expert Opin. Ther. Pat. 18(6), 603-627 (2008).
    • (2008) Expert Opin. Ther. Pat. , vol.18 , Issue.6 , pp. 603-627
    • Price, S.1
  • 64
    • 84884127318 scopus 로고    scopus 로고
    • Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAFdriven cancers
    • doi:10.1038/ nature12441 (Epub ahead of print)
    • Hatzivassiliou G, Haling JR, Chen H et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAFdriven cancers. Nature doi:10.1038/ nature12441 (2013) (Epub ahead of print).
    • (2013) Nature
    • Hatzivassiliou, G.1    Haling, J.R.2    Chen, H.3
  • 65
    • 80053287704 scopus 로고    scopus 로고
    • Monitoring Gq-coupled receptor response through inositol phosphate quantification with the IP-One assay
    • Trinquet E, Bouhelal R, Dietz M. Monitoring Gq-coupled receptor response through inositol phosphate quantification with the IP-One assay. Expert Opin. Drug Discov. 6(10), 981-994 (2011).
    • (2011) Expert Opin. Drug Discov. , vol.6 , Issue.10 , pp. 981-994
    • Trinquet, E.1    Bouhelal, R.2    Dietz, M.3
  • 66
    • 77956486698 scopus 로고    scopus 로고
    • Label-free whole-cell assays: Expanding the scope of GPCR screening
    • Scott CW, Peters MF. Label-free whole-cell assays: expanding the scope of GPCR screening. Drug Discov. Today 15(17-18), 704-716 (2010).
    • (2010) Drug Discov. Today , vol.15 , Issue.17-18 , pp. 704-716
    • Scott, C.W.1    Peters, M.F.2
  • 67
    • 84881271660 scopus 로고    scopus 로고
    • Emerging paradigms in GPCR allostery: Implications for drug discovery
    • Wootten D, Christopoulos A, Sexton PM. Emerging paradigms in GPCR allostery: implications for drug discovery. Nat. Rev. Drug Discov. 12(8), 630-644 (2013).
    • (2013) Nat. Rev. Drug Discov. , vol.12 , Issue.8 , pp. 630-644
    • Wootten, D.1    Christopoulos, A.2    Sexton, P.M.3
  • 68
    • 0028081040 scopus 로고
    • Synthesis and quantitative structure-activity relationships of anticonvulsant 2, 3,6-triaminopyridines
    • Seydel JK, Schaper KJ, Coats EA et al. Synthesis and quantitative structure-activity relationships of anticonvulsant 2,3,6-triaminopyridines. J. Med. Chem. 37(19), 3016-3022 (1994).
    • (1994) J. Med. Chem. , vol.37 , Issue.19 , pp. 3016-3022
    • Seydel, J.K.1    Schaper, K.J.2    Coats, E.A.3
  • 69
    • 3242656529 scopus 로고    scopus 로고
    • A novel extract SB-300 from the stem bark latex of Croton lechleri inhibits CFTR-mediated chloride secretion in human colonic epithelial cells
    • Fischer H, Machen TE, Widdicombe JH et al. A novel extract SB-300 from the stem bark latex of Croton lechleri inhibits CFTR-mediated chloride secretion in human colonic epithelial cells. J. Ethnopharmacol. 93(2), 351-357 (2004).
    • (2004) J. Ethnopharmacol. , vol.93 , Issue.2 , pp. 351-357
    • Fischer, H.1    Machen, T.E.2    Widdicombe, J.H.3
  • 70
    • 19944429772 scopus 로고    scopus 로고
    • A Diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis
    • Andries K, Verhasselt P, Guillemont J et al. A Diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 307(5707), 223-227 (2005).
    • (2005) Science , vol.307 , Issue.5707 , pp. 223-227
    • Andries, K.1    Verhasselt, P.2    Guillemont, J.3
  • 71
    • 17644395643 scopus 로고    scopus 로고
    • Phase I/II trial of adding semisynthetic homoharringtonine in chronic myeloid leukemia patients who have achieved partial or complete cytogenetic response on imatinib
    • Marin D, Kaeda JS, Andreasson C et al. Phase I/II trial of adding semisynthetic homoharringtonine in chronic myeloid leukemia patients who have achieved partial or complete cytogenetic response on imatinib. Cancer 103(9), 1850-1855 (2005).
    • (2005) Cancer , vol.103 , Issue.9 , pp. 1850-1855
    • Marin, D.1    Kaeda, J.S.2    Andreasson, C.3
  • 72
    • 0026579123 scopus 로고
    • 3-carboxy-5-methyl-N-4- (trifluoromethyl)phenyl]-4- isoxazolecarboxamide, new prodrug for the antiarthritic agent 2-cyano-3-hydroxy-N-4- (trifluoromethyl)phenyl]-2-butenamide
    • Patterson JW, Cheung PS, Ernest MJ. 3-carboxy-5-methyl-N-4- (trifluoromethyl)phenyl]-4- isoxazolecarboxamide, new prodrug for the antiarthritic agent 2-cyano-3-hydroxy-N-4- (trifluoromethyl)phenyl]-2- butenamide. J. Med. Chem. 35, 507-510 (1992).
    • (1992) J. Med. Chem. , vol.35 , pp. 507-510
    • Patterson, J.W.1    Cheung, P.S.2    Ernest, M.J.3
  • 73
    • 23744432856 scopus 로고    scopus 로고
    • PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC
    • Hampson P, Chahal H, Khanim F et al. PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood 106(4), 1362-1368 (2005).
    • (2005) Blood , vol.106 , Issue.4 , pp. 1362-1368
    • Hampson, P.1    Chahal, H.2    Khanim, F.3
  • 74
    • 0025969299 scopus 로고
    • Hoe 140 a new potent and long acting bradykininantagonist: In vitro studies
    • Hock FJ, Wirth K, Albus U et al. Hoe 140 a new potent and long acting bradykininantagonist: in vitro studies. Br. J. Pharmacol. 102(3), 769-773 (1991).
    • (1991) Br. J. Pharmacol. , vol.102 , Issue.3 , pp. 769-773
    • Hock, F.J.1    Wirth, K.2    Albus, U.3
  • 75
    • 84868481873 scopus 로고    scopus 로고
    • Vemurafenib: The first drug approved for BRAF-mutant cancer
    • Bollag G, Tsai J, Zhang J et al. Vemurafenib: the first drug approved for BRAF-mutant cancer. Nat. Rev. Drug Discov. 11, 873-886 (2012).
    • (2012) Nat. Rev. Drug Discov. , vol.11 , pp. 873-886
    • Bollag, G.1    Tsai, J.2    Zhang, J.3
  • 76
    • 33749241866 scopus 로고    scopus 로고
    • Discovery of (1R,5S)-N-3-amino-1- (cyclobutylmethyl)-2,3-dioxopropyl]- 3-2(S)-(1,1-dimethylethyl)amino]carbonyl] amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo3.1.0]hexan-2(S)- carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: A potential therapeutic agent for the treatment of hepatitis C infection
    • Venkatraman S, Bogen SL, Arasappan A et al. Discovery of (1R,5S)-N-3-amino-1- (cyclobutylmethyl)-2,3-dioxopropyl]- 3-2(S)-(1,1- dimethylethyl)amino]carbonyl] amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo3.1.0]hexan-2(S)- carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection. J. Med. Chem. 49(20), 6074-6086 (2006).
    • (2006) J. Med. Chem. , vol.49 , Issue.20 , pp. 6074-6086
    • Venkatraman, S.1    Bogen, S.L.2    Arasappan, A.3
  • 77
    • 0029058770 scopus 로고
    • Novel steroidal inhibitors of human cytochrome P45017.alpha.-hydroxylase- C17,20-lyase): Potential agents for the treatment of prostatic cancer
    • Potter GA, Barrie SE, Jarman M, Rowlands MG. Novel steroidal inhibitors of human cytochrome P45017.alpha.-hydroxylase- C17,20-lyase): potential agents for the treatment of prostatic cancer. J. Med. Chem. 38, 2463-2471 (1995).
    • (1995) J. Med. Chem. , vol.38 , pp. 2463-2471
    • Potter, G.A.1    Barrie, S.E.2    Jarman, M.3    Rowlands, M.G.4
  • 78
    • 0035084103 scopus 로고    scopus 로고
    • Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro
    • Hatzelmann A, Schudt C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J. Pharmacol. Exp. Ther. 297(1), 267-279 (2001).
    • (2001) J. Pharmacol. Exp. Ther. , vol.297 , Issue.1 , pp. 267-279
    • Hatzelmann, A.1    Schudt, C.2
  • 79
    • 0035866584 scopus 로고    scopus 로고
    • A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors
    • Robl JA, Sulsky R, Sun C et al. A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors. J. Med. Chem. 44(6), 851-856 (2001).
    • (2001) J. Med. Chem. , vol.44 , Issue.6 , pp. 851-856
    • Robl, J.A.1    Sulsky, R.2    Sun, C.3
  • 80
    • 83355166909 scopus 로고    scopus 로고
    • Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth
    • Yakes FM, Chen J, Tan J et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol. Cancer. Ther. 10(12), 2298-2308 (2011).
    • (2011) Mol. Cancer. Ther. , vol.10 , Issue.12 , pp. 2298-2308
    • Yakes, F.M.1    Chen, J.2    Tan, J.3
  • 81
    • 84870989558 scopus 로고    scopus 로고
    • Discovery of 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2- dihydropyridin-3-yl) benzonitrile (Perampanel): A novel, noncompetitive a-amino-3-hydroxy-5-methyl-4- isoxazolepropanoic acid (AMPA) receptor Antagonist
    • Hibi S, Ueno K, Nagato S et al. Discovery of 2-(2-oxo-1-phenyl-5-pyridin- 2-yl-1,2- dihydropyridin-3-yl)benzonitrile (Perampanel): a novel, noncompetitive a-amino-3-hydroxy-5-methyl-4- isoxazolepropanoic acid (AMPA) receptor Antagonist. J. Med. Chem. 55, 10584-10600 (2012).
    • (2012) J. Med. Chem. , vol.55 , pp. 10584-10600
    • Hibi, S.1    Ueno, K.2    Nagato, S.3
  • 82
    • 78049283798 scopus 로고    scopus 로고
    • Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit
    • Busby RW, Bryant AP, Bartolini WP et al. Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit. Eur. J. Pharmacol. 649(1), 328-335 (2010).
    • (2010) Eur. J. Pharmacol. , vol.649 , Issue.1 , pp. 328-335
    • Busby, R.W.1    Bryant, A.P.2    Bartolini, W.P.3
  • 83
    • 77950800340 scopus 로고    scopus 로고
    • Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective beta3- adrenergic receptor agonists
    • Maruyama T, Onda K, Hayakawa M et al. Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective beta3- adrenergic receptor agonists. Chem. Pharm. Bull. (Tokyo) 58(4), 533-545 (2010).
    • (2010) Chem. Pharm. Bull. (Tokyo) , vol.58 , Issue.4 , pp. 533-545
    • Maruyama, T.1    Onda, K.2    Hayakawa, M.3
  • 84
    • 13944263169 scopus 로고    scopus 로고
    • Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity
    • Smith BM, Smith JM, Tsai JH et al. Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity. Bioorg. Med. Chem. Lett. 15(5), 1467-1470 (2005).
    • (2005) Bioorg. Med. Chem. Lett. , vol.15 , Issue.5 , pp. 1467-1470
    • Smith, B.M.1    Smith, J.M.2    Tsai, J.H.3
  • 85
    • 73249114731 scopus 로고    scopus 로고
    • Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770
    • Van Goor F, Hadida S, Grootenhuis PDJ et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. Proc. Natl Acad. Sci. USA 106(44), 18825-18830 (2009).
    • (2009) Proc. Natl Acad. Sci. USA , vol.106 , Issue.44 , pp. 18825-18830
    • Van Goor, F.1    Hadida, S.2    Pdj, G.3
  • 86
    • 77958029696 scopus 로고    scopus 로고
    • Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway
    • Castanedo GM, Wang S, Robarge KD et al. Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway. Bioorg. Med. Chem. Lett. 20, 6748-6753 (2010).
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 6748-6753
    • Castanedo, G.M.1    Wang, S.2    Robarge, K.D.3
  • 87
    • 77950684805 scopus 로고    scopus 로고
    • Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms
    • Quintás-Cardama A, Vaddi K, Liu P et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115, 3109-3117 (2010).
    • (2010) Blood , vol.115 , pp. 3109-3117
    • Quintás-Cardama, A.1    Vaddi, K.2    Liu, P.3


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