Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D
A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P 1′, P 2–P 4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of sel...
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| Published in | Bioorganic & medicinal chemistry letters Vol. 8; no. 22; pp. 3203 - 3206 |
|---|---|
| Main Authors | , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford
Elsevier Ltd
17.11.1998
Elsevier |
| Subjects | |
| Online Access | Get full text |
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| Abstract | A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P
1′, P
2–P
4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of selective inhibitors for each enzyme.
Selective inhibitors of plasmepsin II and cathepsin D were identified from an encoded 18,900-member combinatorial library. |
|---|---|
| AbstractList | A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P
1′, P
2–P
4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of selective inhibitors for each enzyme.
Selective inhibitors of plasmepsin II and cathepsin D were identified from an encoded 18,900-member combinatorial library. A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P1, P2-P4 surrogates. Evaluation of this encoded library against two aspartyl proteases, plasmepsin II and cathepsin D, led to the identification of selective inhibitors for each enzyme. |
| Author | Tao, Shewei Goldberg, Daniel E. Johnson, Theodore O. Orlowski, Marc Gluzman, Ilya Y. Lauri, Giorgio Carroll, Carolyn DiIanni Dolle, Roland E. |
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| Cites_doi | 10.1021/ja00125a022 10.1002/med.2610130605 10.1172/JCI117140 10.1002/j.1460-2075.1994.tb06263.x 10.1128/AAC.16.6.710 10.1016/S0960-894X(98)00419-3 |
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| Keywords | Aminoalcohol Enzyme Plasmepsin II Combinatorial chemistry Enzyme inhibitor Non peptide compound Selectivity In vitro Peptidases Structure activity relation Chemical compound library Hydrolases Aspartic endopeptidases Cathepsin D Solid phase Piperazine derivatives Chemical synthesis |
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| References | Baldwin, Bhat, Gulnik, Hosur, Sowder, Cachau, Collins, Silvia, Erickson (BIB5) 1993; 90 Francis, Gluzman, Oksman, Knickerbocker, Mueller, Sherman, Russell, Goldberg (BIB2) 1994; 13 BIB6 BIB4 Abdel-Meguid (BIB1) 1993; 13 Gluzman, Francis, Oksman, Smith, Duffin, Goldberg, Rich, Agarwal (BIB8) 1994; 93 Carroll, Patel, Johnson, Guo, Orlowski, He, Cavallaro, Guo, Oksman, Gluzman, Connelly, Chelsky, Goldberg, Dolle (BIB3) 1998; 8 Baldwin, Burbaum, Henderson, Ohlmeyer (BIB7) 1995; 117 Desjardin, Canfield, Haynes, Chulay (BIB9) 1979; 16 Baldwin (10.1016/S0960-894X(98)00554-X_BIB7) 1995; 117 Carroll (10.1016/S0960-894X(98)00554-X_BIB3) 1998; 8 Gluzman (10.1016/S0960-894X(98)00554-X_BIB8_1) 1994; 93 Baldwin (10.1016/S0960-894X(98)00554-X_BIB5) 1993; 90 Francis (10.1016/S0960-894X(98)00554-X_BIB2) 1994; 13 Rich (10.1016/S0960-894X(98)00554-X_BIB8_2) 1986; 22 Desjardin (10.1016/S0960-894X(98)00554-X_BIB9) 1979; 16 Abdel-Meguid (10.1016/S0960-894X(98)00554-X_BIB1) 1993; 13 |
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1′, P
2–P
4... A structure-based 18,900-member combinatorial library was synthesized containing a statine template and three cyclic diamino acids as potential P1, P2-P4... |
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| SubjectTerms | Amides - pharmacology Amino Acids - pharmacology Analytical, structural and metabolic biochemistry Aspartic Acid Endopeptidases - antagonists & inhibitors Biological and medical sciences Cathepsin D - antagonists & inhibitors Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Humans Hydrolases Protease Inhibitors - pharmacology Protozoan Proteins Structure-Activity Relationship |
| Title | Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D |
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