A SOLUTION-PHASE SCREENING-PROCEDURE FOR THE ISOLATION OF ACTIVE COMPOUNDS FROM A LIBRARY OF MOLECULES

A SOLUTION-PHASE SCREENING-PROCEDURE FOR THE ISOLATION OF ACTIVE COMPOUNDS FROM A LIBRARY OF MOLECULES
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DOI:
10.1002/anie.199420611
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发表时间:
1994-11-02
期刊:
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH
影响因子:
--
通讯作者:
REBEK, J
REBEK, J
中科院分区:
其他
文献类型:
--
作者:
CARELL, T;WINTNER, EA;REBEK, J

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图1.相对于不含添加的库材料的空白(X.A,=100%),在存在添加的库的情况下,胰酶活性A。每一条代表四次测量的平均胰酶活性。A)胰酶活性[“/o],初始文库A1和A7(在50mLDMSO中各有2.5毫克)分别由核心分子I和2构建。和19个氨基酸构建块[是。B)胰酶活性[‘%I,6个亚库EUR31-B6(每50mLDMSO中各2.5mgDMSO),由19个氨基酸组成的核心分子1和15构成(不含S-Trt-Cys)。B1:省略G1组,B2:省略G2组,83:省略G3组,84:省略G4组。B5:省略G5组。B6:省略G6组。组G1-G6列于表1。c)Trqpsin活性[%i,其中9个亚库C1-C9(在50毫升DMSO中各1.5毫克)由核心分子1构建而成,其中8个构建块来自G1-G3组(表1)中的氨基酸(表1)。C1:省略arg,cz。Lys省略:C3他省略:C4:Leo省略:C5:Ile省略:C6:省略:C7:Glyomomed。C8.A h省略;C9:val省略。D)胰酶活性[“h],有六个亚基膜d1-d6(每例0。J nigiii 50mLofDMSO)。有关他们的组成的说明,请参阅正文和
Fig. 1. Trypsin activity A, in the presence of added libraries relative to that of a blank (X. A,= 100%) containing no added library material. Each bar represents average trypsin activity For four measurements. a) Trypsin activity ["/o] with the initial libraries A1 and A7 (in each case 2.5 mg in 50 mL of DMSO) constructed from the core molecules I and 2. respectively. and 19 amino acid building blocks [IS. b) Trypsin activity ['% I with the six sublibraries€ 31-B6 (in each case 2.5 mg in 50 mL of DMSO) constructed from core molecule 1 and 15 of the 19 amino acid building blocks (\* ithout S-Trt-Cys). B1: group GI omitted, B2: group G2 omitted: 83: group G3 omitted; 84: group G4 omitted. B5: group G5 omitted. B6: Group G6 omitted. Groups GI-G6 are listed in Table 1. c) Trqpsin activity [% I with the nine sublibraries C1-C9 (in each case 1.5 mg in 50 mL of DMSO) constructed from the core molecule 1 end eight of the nine building blocks from the amino acids in groups Gl-G3 (Table 1). C1: Arg omitted, CZ. Lys omitted: C3 His omitted: C4: Leo omitted: C5: Ile omitted: C6: Proomitted: C7: Glyomitted. C8. A h omitted; C9: Val omitted. d) Trypsin activity [" h] with the six sublibraries D1-D6 (in each case0. j nigiii 50mLofDMSO). Foradescriptionoftheircompositionssee text and