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Volumn 7, Issue 7, 2006, Pages 1023-1027

Target-assisted selection of galactosyltransferase binders from dynamic combinatorial libraries. An unexpected solution with restricted amounts of the enzyme

Author keywords

Cabohydrates; Combinatorial chemistry; Enzyme inhibitors; Molecular recognition; Self assembly

Indexed keywords

ALDEHYDE; ALPHA 1,3 GALACTOSYLTRANSFERASE; AMIDE; DIAMINE DERIVATIVE; GALACTOSE; NUCLEOTIDE;

EID: 33745930819     PISSN: 14394227     EISSN: 14397633     Source Type: Journal    
DOI: 10.1002/cbic.200600022     Document Type: Article
Times cited : (34)

References (56)
  • 2
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    • (Eds.: B. Ernst, G. W. Hart, P. Sinäy), Wiley-VCH, Weinheim
    • a) X. Qian, M. M. Palcic in Carbohydrates in Chemistry and Biology, (Eds.: B. Ernst, G. W. Hart, P. Sinäy), Wiley-VCH, Weinheim; 2000, 3, 293;
    • (2000) Carbohydrates in Chemistry and Biology , vol.3 , pp. 293
    • Qian, X.1    Palcic, M.M.2
  • 4
    • 33745920887 scopus 로고    scopus 로고
    • c) For an up-to-date 3D structure database of glycosyltransferases see www. cermav.cnrs.fr/cgi-bin/rxgt/rxgt.cgi
  • 23
    • 33745891022 scopus 로고    scopus 로고
    • note
    • In this paper, the term "imines" will designate the totality of the assembled members of the library (imines, hemi-aminals, aminals and their protonated species).
  • 28
    • 33745901751 scopus 로고    scopus 로고
    • note
    • [5] affinity systems.
  • 29
    • 29144498663 scopus 로고    scopus 로고
    • However, for a self-screening process in which only catalytic amounts of the target protein are present, see R. Larsson, Z. Pei, O. Ramström, Angew. Chem. 2004, 116, 3802;
    • (2004) Angew. Chem. , vol.116 , pp. 3802
    • Larsson, R.1    Pei, Z.2    Ramström, O.3
  • 31
    • 33745909535 scopus 로고    scopus 로고
    • note
    • When taking a good affinity constant for a binder (1 μM), one calculates that the amount of the amplified amine would be approximately in the range of the detection limit of our system (around 20 pmol), with the enzyme at a concentration of 2 μM.
  • 32
    • 33745878365 scopus 로고    scopus 로고
    • note
    • The term "amplification" for a library member designates its concentration in the presence of the target divided by its concentration in the absence of the target.
  • 33
    • 33745903240 scopus 로고    scopus 로고
    • note
    • 3CN reduction of imines in an aqueous medium.
  • 34
    • 0037008717 scopus 로고    scopus 로고
    • In the course of these studies, information was published on the 3D structure of the α-1,3-galactosyltransferase enzyme, substrates binding and catalytic mechanism, E. Boix, Y. Zhang, G. J. Swaminathan, K. Brew, K. R. Acharya, J. Biol. Chem. 2002, 277, 28310.
    • (2002) J. Biol. Chem. , vol.277 , pp. 28310
    • Boix, E.1    Zhang, Y.2    Swaminathan, G.J.3    Brew, K.4    Acharya, K.R.5
  • 35
    • 0032556891 scopus 로고    scopus 로고
    • D. Butler, Nature 1998, 391, 320;
    • (1998) Nature , vol.391 , pp. 320
    • Butler, D.1
  • 52
    • 33745923308 scopus 로고    scopus 로고
    • note
    • LC-MS or LC-evaporative light scattering (ELS) methods of detection were not adapted or not sensitive enough for our compounds.
  • 53
    • 33745915658 scopus 로고    scopus 로고
    • note
    • We previously checked that the commercial enzyme was still active after 14 days in a Tris-acetate buffer containing glycerol. Attempts to concentrate the commercial preparation of the enzyme lead to a very significant decrease in the enzyme activity.
  • 54
    • 33745887902 scopus 로고    scopus 로고
    • note
    • Because of the UV-detection method, the product distribution was established by using independently prepared reference compounds and was quantified by using the HPLC-UV profile, each peak area being corrected by the molar extinction coefficient of the corresponding amine at 254 nm.
  • 56
    • 33745900594 scopus 로고    scopus 로고
    • note
    • 50 measurements.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.