TY - JOUR
T1 - Screening a fragment cocktail library using ultrafiltration
AU - Shibata, Sayaka
AU - Zhang, Zhongsheng
AU - Korotkov, Konstantin V.
AU - Delarosa, Jaclyn
AU - Napuli, Alberto
AU - Kelley, Angela M.
AU - Mueller, Natasha
AU - Ross, Jennifer
AU - Zucker, Frank H.
AU - Buckner, Frederick S.
AU - Merritt, Ethan A.
AU - Verlinde, Christophe L.M.J.
AU - Van Voorhis, Wesley C.
AU - Hol, Wim G.J.
AU - Fan, Erkang
N1 - Funding Information:
We thank Eric T. Larson for his critical review of the manuscript. This work was supported by National Institutes of Health grants P50GM64655 (SGPP), P01AI067921 (MSGPP), and AI34501.
PY - 2011/9
Y1 - 2011/9
N2 - Ultrafiltration provides a generic method to discover ligands for protein drug targets with millimolar to micromolar K d, the typical range of fragment-based drug discovery. This method was tailored to a 96-well format, and cocktails of fragment-sized molecules, with molecular masses between 150 and 300 Da, were screened against medical structural genomics target proteins. The validity of the method was confirmed through competitive binding assays in the presence of ligands known to bind the target proteins.
AB - Ultrafiltration provides a generic method to discover ligands for protein drug targets with millimolar to micromolar K d, the typical range of fragment-based drug discovery. This method was tailored to a 96-well format, and cocktails of fragment-sized molecules, with molecular masses between 150 and 300 Da, were screened against medical structural genomics target proteins. The validity of the method was confirmed through competitive binding assays in the presence of ligands known to bind the target proteins.
KW - Compound library
KW - Fragment-based drug discovery
KW - Screening
KW - Ultrafiltration
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U2 - 10.1007/s00216-011-5225-7
DO - 10.1007/s00216-011-5225-7
M3 - Article
C2 - 21750879
AN - SCOPUS:80052579105
SN - 1618-2642
VL - 401
SP - 1589
EP - 1595
JO - Analytical and Bioanalytical Chemistry
JF - Analytical and Bioanalytical Chemistry
IS - 5
ER -