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Volumn 131, Issue 9, 2009, Pages 3342-3348

Discovery of inhibitors of aberrant gene transcription from libraries of DNA binding molecules: Inhibition of LEF-1-mediated gene transcription and oncogenic transformation

Author keywords

[No Author keywords available]

Indexed keywords

ASSAYS; BINDING ENERGY; COMPLEXATION; DNA; GENES; LEAD COMPOUNDS; MOLECULES; TISSUE CULTURE; TRANSCRIPTION FACTORS;

EID: 71749120003     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja809083d     Document Type: Article
Times cited : (32)

References (48)
  • 8
    • 0026416047 scopus 로고
    • Approximately 50% of the Western population develop colorectal adenomas by the age of 70 a
    • Approximately 50% of the Western population develop colorectal adenomas by the age of 70 (a) Ransohoff, D.; Lang, C. N. Engl. J. Med. 1991, 325, 37-41.
    • (1991) N. Engl. J. Med. , vol.325 , pp. 37-41
    • Ransohoff, D.1    Lang, C.2
  • 43
    • 0036850867 scopus 로고    scopus 로고
    • It is possible that a single uniquely active compound in a mixture may be missed by screening even such small mixtures 10 or 15 compounds. However, because two of the subunits of each compound in a given mixture are the same same B and C subunits, it is more likely that each compound in a mixture exhibits a progressive range of related binding affinities and selectivities rather than exhibiting a unique behavior. As such, the screening of mixtures containing such common elements not only minimize the chances of missing a uniquely active compound, but it can often provide a first level SAR that distinguishes it from randomly combined 10-15 compound mixtures that are commonly used to expedite HTS. For our purposes and as shown herein, the approach provided useful lead structures utilizing equipment, reagent amounts, and time accessible in any academic laboratory. For more detailed documentation of testing such mixtures, see. a
    • It is possible that a single uniquely active compound in a mixture may be missed by screening even such small mixtures (10 or 15 compounds). However, because two of the subunits of each compound in a given mixture are the same (same B and C subunits), it is more likely that each compound in a mixture exhibits a progressive range of related binding affinities and selectivities rather than exhibiting a unique behavior. As such, the screening of mixtures containing such common elements not only minimize the chances of missing a uniquely active compound, but it can often provide a first level SAR that distinguishes it from randomly combined 10-15 compound mixtures that are commonly used to expedite HTS. For our purposes and as shown herein, the approach provided useful lead structures utilizing equipment, reagent amounts, and time accessible in any academic laboratory. For more detailed documentation of testing such mixtures, see. (a) Ambroise, Y.; Yuspan, B.; Ginsberg, M. H.; Boger, D. L. Chem. Biol. 2002, 9, 1219-1226.
    • (2002) Chem. Biol. , vol.9 , pp. 1219-1226
    • Ambroise, Y.1    Yuspan, B.2    Ginsberg, M.H.3    Boger, D.L.4
  • 46
    • 84925570808 scopus 로고    scopus 로고
    • This library is available upon request for screening
    • This library is available upon request for screening.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.