메뉴 건너뛰기




Volumn 49, Issue 5, 2010, Pages 822-829

An efficient and information-rich biochemical method design for fragment library screening on ion channels

Author keywords

5 HT3; Cys loop; Fragment; High throughput; Library; Ligand; Screen; Therapeutic

Indexed keywords

G PROTEIN COUPLED RECEPTOR; ION CHANNEL; LIGAND GATED ION CHANNEL; MEMBRANE PROTEIN; RADIOLIGAND; UNCLASSIFIED DRUG; VOLTAGE GATED ION CHANNEL;

EID: 78349241041     PISSN: 07366205     EISSN: None     Source Type: Journal    
DOI: 10.2144/000113538     Document Type: Article
Times cited : (15)

References (26)
  • 1
    • 33847381100 scopus 로고    scopus 로고
    • A decade of fragment-based drug design: Strategic advances and lessons learned
    • Hajduk, P.J. and J. Greer. 2007. A decade of fragment-based drug design: strategic advances and lessons learned. Nat. Rev. Drug Discov. 6:211-219.
    • (2007) Nat. Rev. Drug Discov. , vol.6 , pp. 211-219
    • Hajduk, P.J.1    Greer, J.2
  • 2
    • 67651004682 scopus 로고    scopus 로고
    • Fragment-based drug discovery
    • Warr, W.A. 2009. Fragment-based drug discovery. J. Comput. Aided Mol. Des. 23:453-458.
    • (2009) J. Comput. Aided Mol. Des. , vol.23 , pp. 453-458
    • Warr, W.A.1
  • 3
    • 46849089254 scopus 로고    scopus 로고
    • Recent developments in fragment-based drug discovery
    • Congreve, M., G. Chessari, D. Tisi, and A.J. Woodhead. 2008. Recent developments in fragment-based drug discovery. J. Med. Chem. 51:3661-3680.
    • (2008) J. Med. Chem. , vol.51 , pp. 3661-3680
    • Congreve, M.1    Chessari, G.2    Tisi, D.3    Woodhead, A.J.4
  • 4
    • 67649494337 scopus 로고    scopus 로고
    • Transforming fragments into candidates: Small becomes big in medicinal chemistry
    • de Kloe, G.E., D. Bailey, R. Leurs, and I.J. de Esch. 2009. Transforming fragments into candidates: small becomes big in medicinal chemistry. Drug Discov. Today 14:630-646.
    • (2009) Drug Discov. Today , vol.14 , pp. 630-646
    • De Kloe, G.E.1    Bailey, D.2    Leurs, R.3    De Esch, I.J.4
  • 5
    • 67650999672 scopus 로고    scopus 로고
    • Lessons for fragment library design: Analysis of output from multiple screening campaigns
    • Chen, I.-J. and R.E. Hubbard. 2009. Lessons for fragment library design: analysis of output from multiple screening campaigns. J. Comput. Aided Mol. Des. 23:603-620.
    • (2009) J. Comput. Aided Mol. Des. , vol.23 , pp. 603-620
    • Chen, I.-J.1    Hubbard, R.E.2
  • 6
    • 33845364148 scopus 로고    scopus 로고
    • Fragment-based drug design: How big is too big?
    • Hajduk, P.J. 2006. Fragment-based drug design: how big is too big? J. Med. Chem. 49:6972-6976.
    • (2006) J. Med. Chem. , vol.49 , pp. 6972-6976
    • Hajduk, P.J.1
  • 7
    • 27644555726 scopus 로고    scopus 로고
    • Substrate activity screening: A fragment-based method for the rapid identification of nonpeptidic protease inhibitors
    • Wood, W.J., A.W. Patterson, H. Tsuruoka, R.K. Jain, and J.A. Ellman. 2005. Substrate activity screening: a fragment-based method for the rapid identification of nonpeptidic protease inhibitors. J. Am. Chem. Soc. 127:15521-15527.
    • (2005) J. Am. Chem. Soc. , vol.127 , pp. 15521-15527
    • Wood, W.J.1    Patterson, A.W.2    Tsuruoka, H.3    Jain, R.K.4    Ellman, J.A.5
  • 8
    • 0029836953 scopus 로고    scopus 로고
    • Discovering high-affinity ligands for proteins: SAR by NMR
    • Shuker, S.B., P.J. Hajduk, R.P. Meadows, and S.W. Fesik. 1996. Discovering high-affinity ligands for proteins: SAR by NMR. Science 274:1531-1534.
    • (1996) Science , vol.274 , pp. 1531-1534
    • Shuker, S.B.1    Hajduk, P.J.2    Meadows, R.P.3    Fesik, S.W.4
  • 10
    • 65249093007 scopus 로고    scopus 로고
    • Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. in silico docking, pharmacological screening, and X-ray analysis
    • Ulens, C., A. Akdemir, A. Jongejan, R. van Elk, S. Bertrand, A. Perrakis, R. Leurs, A.B. Smit, et al. 2009. Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. in silico docking, pharmacological screening, and X-ray analysis. J. Med. Chem. 52:2372-2383.
    • (2009) J. Med. Chem. , vol.52 , pp. 2372-2383
    • Ulens, C.1    Akdemir, A.2    Jongejan, A.3    Van Elk, R.4    Bertrand, S.5    Perrakis, A.6    Leurs, R.7    Smit, A.B.8
  • 12
    • 34548205436 scopus 로고    scopus 로고
    • Molecular pharmacology of the glycine receptor chloride channel
    • Webb, T.I. and J.W. Lynch. 2007. Molecular pharmacology of the glycine receptor chloride channel. Curr. Pharm. Des. 13:2350-2367.
    • (2007) Curr. Pharm. Des. , vol.13 , pp. 2350-2367
    • Webb, T.I.1    Lynch, J.W.2
  • 13
    • 20044396748 scopus 로고    scopus 로고
    • A receptor channel pharmacology
    • Johnston, G.A. 2005. GABAA receptor channel pharmacology. Curr. Pharm. Des. 11:1867-1885.
    • (2005) Curr. Pharm. Des. , vol.11 , pp. 1867-1885
    • Johnston, G.A.1
  • 14
    • 58049133111 scopus 로고    scopus 로고
    • A receptors: Subtypes provide diversity of function and pharmacology
    • Olsen, R.W. and W. Sieghart. 2009. GABAA receptors: subtypes provide diversity of function and pharmacology. Neuropharmacology 56:141-148.
    • (2009) Neuropharmacology , vol.56 , pp. 141-148
    • Olsen, R.W.1    Sieghart, W.2
  • 16
    • 70349647710 scopus 로고    scopus 로고
    • Correction for interference by test samples in high-throughput assays
    • Shapiro, A.B., G.K. Walkup, and T.A. Keating. 2009. Correction for interference by test samples in high-throughput assays. J. Biomol. Screen. 14:1008-1016.
    • (2009) J. Biomol. Screen. , vol.14 , pp. 1008-1016
    • Shapiro, A.B.1    Walkup, G.K.2    Keating, T.A.3
  • 17
    • 0027522536 scopus 로고
    • Further concerns over Cheng-Prusoff analysis
    • Leff, P. and I.G. Dougall. 1993. Further concerns over Cheng-Prusoff analysis. Trends Pharmacol. Sci. 14:110-112.
    • (1993) Trends Pharmacol. Sci. , vol.14 , pp. 110-112
    • Leff, P.1    Dougall, I.G.2
  • 18
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng, Y. and W.H. Prusoff. 1973. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 22:3099-3108.
    • (1973) Biochem. Pharmacol. , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2
  • 19
    • 36549033318 scopus 로고    scopus 로고
    • Integration of fragment screening and library design
    • Siegal, G., E. Ab, and J. Schultz. 2007. Integration of fragment screening and library design. Drug Discov. Today 12:1032-1039.
    • (2007) Drug Discov. Today , vol.12 , pp. 1032-1039
    • Siegal, G.1    Ab, E.2    Schultz, J.3
  • 20
    • 0037153217 scopus 로고    scopus 로고
    • A new approach to finding natural chemical structure classes
    • Xu, J. 2002. A new approach to finding natural chemical structure classes. J. Med. Chem. 45:5311-5320.
    • (2002) J. Med. Chem. , vol.45 , pp. 5311-5320
    • Xu, J.1
  • 21
    • 78049403279 scopus 로고    scopus 로고
    • Ligand binding assays at equilibrium: Validation and interpretation
    • Feb 2. [Epub ahead of print]
    • Hulme, E.C. and M.A. Trevethick. 2010. Ligand binding assays at equilibrium: validation and interpretation. Br. J. Pharmacol. Feb 2. [Epub ahead of print].
    • (2010) Br. J. Pharmacol.
    • Hulme, E.C.1    Trevethick, M.A.2
  • 22
    • 67651005599 scopus 로고    scopus 로고
    • Structural models in the assessment of protein druggability based on HTS data
    • Gupta, A., A.K. Gupta, and K. Seshadri. 2009. Structural models in the assessment of protein druggability based on HTS data. J. Comput. Aided Mol. Des. 23:583-592.
    • (2009) J. Comput. Aided Mol. Des. , vol.23 , pp. 583-592
    • Gupta, A.1    Gupta, A.K.2    Seshadri, K.3
  • 24
    • 36248944181 scopus 로고    scopus 로고
    • An integrated approach to fragment-based lead generation: Philosophy, strategy and case studies from AstraZeneca's drug discovery programmes
    • Albert, J.S., N. Blomberg, A.L. Breeze, A.J. Brown, J.N. Burrows, P.D. Edwards, R.H. Folmer, S. Geschwindner, et al. 2007. An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes. Curr. Top. Med. Chem. 7:1600-1629.
    • (2007) Curr. Top. Med. Chem. , vol.7 , pp. 1600-1629
    • Albert, J.S.1    Blomberg, N.2    Breeze, A.L.3    Brown, A.J.4    Burrows, J.N.5    Edwards, P.D.6    Folmer, R.H.7    Geschwindner, S.8
  • 25
    • 42149155410 scopus 로고    scopus 로고
    • C receptors
    • Thompson, A.J. and S.C. Lummis. 2008. Antimalarial drugs inhibit human 5-HT3 and GABAA but not GABAC receptors. Br. J. Pharmacol. 153:1686-1696.
    • (2008) Br. J. Pharmacol. , vol.153 , pp. 1686-1696
    • Thompson, A.J.1    Lummis, S.C.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.