Fragment-Based Lead Discovery

被引:19
作者
Congreve, Miles [1 ]
Murray, Christopher W. [1 ]
Carr, Robin [1 ]
Rees, David C. [1 ]
机构
[1] Astex Therapeut, Cambridge CB4 0QA, England
来源
ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 42 | 2007年 / 42卷
关键词
D O I
10.1016/S0065-7743(07)42028-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
[No abstract available]
引用
收藏
页码:431 / 448
页数:18
相关论文
共 57 条
  • [41] Discovery of thrombin inhibitor fragments from chemical microarray screening
    Neumann, T
    Junker, HD
    Keil, O
    Burkert, K
    Ottleben, H
    Gamer, J
    Sekul, R
    Deppe, H
    Feurer, A
    Tomandl, D
    Metz, G
    [J]. LETTERS IN DRUG DESIGN & DISCOVERY, 2005, 2 (08) : 590 - 594
  • [42] The reversed binding of β-phenethylamine inhibitors of DPP-IV:: X-ray structures and properties of novel fragment and elaborated inhibitors
    Nordhoff, S
    Cerezo-Gálvez, S
    Feurer, A
    Hill, O
    Matassa, VG
    Metz, G
    Rummey, C
    Thiemann, M
    Edwards, PJ
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (06) : 1744 - 1748
  • [43] In silico fragment-based discovery of indolin-2-one analogues as potent DNA gyrase inhibitors
    Oblak, M
    Grdadolnik, SG
    Kotnik, M
    Jerala, R
    Filipic, M
    Solmajer, T
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (23) : 5207 - 5210
  • [44] An inhibitor of Bcl-2 family proteins induces regression of solid tumours
    Oltersdorf, T
    Elmore, SW
    Shoemaker, AR
    Armstrong, RC
    Augeri, DJ
    Belli, BA
    Bruncko, M
    Deckwerth, TL
    Dinges, J
    Hajduk, PJ
    Joseph, MK
    Kitada, S
    Korsmeyer, SJ
    Kunzer, AR
    Letai, A
    Li, C
    Mitten, MJ
    Nettesheim, DG
    Ng, S
    Nimmer, PM
    O'Connor, JM
    Oleksijew, A
    Petros, AM
    Reed, JC
    Shen, W
    Tahir, SK
    Thompson, CB
    Tomaselli, KJ
    Wang, BL
    Wendt, MD
    Zhang, HC
    Fesik, SW
    Rosenberg, SH
    [J]. NATURE, 2005, 435 (7042) : 677 - 681
  • [45] Identification of selective, nonpeptidic nitrile inhibitors of cathepsin S using the substrate activity screening method
    Patterson, Andrew W.
    Wood, Warren J. L.
    Hornsby, Michael
    Lesley, Scott
    Spraggon, Glen
    Ellman, Jonathan A.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (21) : 6298 - 6307
  • [46] Solution nuclear magnetic resonance spectroscopy techniques for probing intermolecular interactions
    Pellecchia, M
    [J]. CHEMISTRY & BIOLOGY, 2005, 12 (09): : 961 - 971
  • [47] Integrating fragment assembly and biophysical methods in the chemical advancement of small-molecule antagonists of IL-2: An approach for inhibiting protein-protein interactions
    Raimundo, BC
    Oslob, JD
    Braisted, AC
    Hyde, J
    McDowell, RS
    Randal, M
    Waal, ND
    Wilkinson, J
    Yu, CH
    Arkin, MR
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (12) : 3111 - 3130
  • [48] Fragment-based lead discovery
    Rees, DC
    Congreve, M
    Murray, CW
    Carr, R
    [J]. NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (08) : 660 - 672
  • [49] In silico fragment-based discovery of DPP-IV S1 pocket binders
    Rummey, C
    Nordhoff, S
    Thiemann, M
    Metz, G
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (05) : 1405 - 1409
  • [50] Discovery of potent inhibitors of dihydroneopterin aldolase using crystaLEAD high-throughput X-ray crystallographic screening and structure-directed lead optimization
    Sanders, WJ
    Nienaber, VL
    Lerner, CG
    McCall, JO
    Merrick, SM
    Swanson, SJ
    Harlan, JE
    Stoll, VS
    Stamper, GF
    Betz, SF
    Condroski, KR
    Meadows, RP
    Severin, JM
    Walter, KA
    Magdalinos, P
    Jakob, CG
    Wagner, R
    Beutel, BA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 (07) : 1709 - 1718