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Volumn 126, Issue 40, 2004, Pages 12809-12818

In situ click chemistry: Enzyme inhibitors made to their own specifications

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLENE; BIOCHEMISTRY; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY;

EID: 5644276317     PISSN: 00027863     EISSN: None     Source Type: Journal    
DOI: 10.1021/ja046382g     Document Type: Article
Times cited : (394)

References (52)
  • 1
    • 79951847547 scopus 로고    scopus 로고
    • Nicolaou, K. C., Hanko, R., Hartwig, W., Eds.; Wiley-VCH: Weinheim, Germany
    • Nicolaou, K. C.; Hanko, R.; Hartwig, W. In Handbook of Combinatorial Chemistry; Nicolaou, K. C., Hanko, R., Hartwig, W., Eds.; Wiley-VCH: Weinheim, Germany, 2002; Vol. 1, pp 3-9.
    • (2002) Handbook of Combinatorial Chemistry , vol.1 , pp. 3-9
    • Nicolaou, K.C.1    Hanko, R.2    Hartwig, W.3
  • 8
    • 27744554825 scopus 로고    scopus 로고
    • Fixing the drugs pipeline
    • March 11
    • Fixing the drugs pipeline. The Economist, March 11, 2004; available online at http://www.economist.com/printedition/displayStory.cfm?Story_ID= 2477075.
    • (2004) The Economist
  • 10
    • 0022469902 scopus 로고
    • Rideout, D. Science 1986, 233, 561-563.
    • (1986) Science , vol.233 , pp. 561-563
    • Rideout, D.1
  • 42
    • 85039510043 scopus 로고    scopus 로고
    • note
    • -1 24). Apart from the expected entropic stabilization, the transition state may also experience stabilization through hydrogen bonding and stacking interactions with the protein.25
  • 43
    • 85039503167 scopus 로고    scopus 로고
    • note
    • The in situ screening experiments were generally performed with the following concentrations: 1 μM for the enzyme, 4.6 μM for tacrine components, and 24 μM for phenylphenanthridinium components. Because of the sensitive nature of the analysis method, the building block concentrations can be reduced to as low as 1 μM for tacrine reagents and 6 μM for phenylphenanthridinium reagents, without a significant loss of intensity of the product peak. However, lowering the phenylphenanthridinium component concentration to 1 μM dramatically decreased the reaction rate and makes the intensity of the product signal prohibitively small.
  • 44
    • 85039492202 scopus 로고    scopus 로고
    • note
    • The computation was performed at the Swiss Institute of Bioinformatics (SIB) using the BLAST network service. The SIB BLAST network service uses a server developed at SIB and the National Center for Biotechnology Information (NCBI) BLAST 2 software.
  • 48
    • 85039502697 scopus 로고    scopus 로고
    • note
    • All samples were analyzed by LC/MS-SIM with electrospray detection on a Cyclobond 1 2000 DMP column (4.6 × 100 mm, preceded by a Phenomenex C18 ODS guard column) using isocratic elution conditions.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.