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Titolo:
The design, synthesis, and biological evaluation of analogues of the serine-threonine protein phosphatase 1 and 2A selective inhibitor microcystin LA: Rational modifications imparting PP1 selectivity
Autore:
Aggen, JB; Humphrey, JM; Gauss, CM; Huang, HB; Nairn, AC; Chamberlain, AR;
Indirizzi:
Univ Calif Irvine, Dept Chem, Irvine, CA 92697 USA Univ Calif Irvine Irvine CA USA 92697 ne, Dept Chem, Irvine, CA 92697 USA Chu Tzi Coll Med, Inst Biochem, Iwaki, Fukushima 970, Japan Chu Tzi Coll Med Iwaki Fukushima Japan 970 m, Iwaki, Fukushima 970, Japan Rockefeller Univ, New York, NY 10021 USA Rockefeller Univ New York NY USA10021 eller Univ, New York, NY 10021 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 3, volume: 7, anno: 1999,
pagine: 543 - 564
SICI:
0968-0896(199903)7:3<543:TDSABE>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEPHAROSE AFFINITY-CHROMATOGRAPHY; NATURAL PRODUCT INHIBITORS; REVERSE-TURN CONSTRAINTS; PHASE PEPTIDE-SYNTHESIS; L-ALANINE DERIVATIVES; AMINO-ACIDS; SERINE/THREONINE PHOSPHATASES; OKADAIC ACID; CALYCULIN-A; D-PRO;
Keywords:
microcystin; inhibitor; PP1; PP2A; selective;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
94
Recensione:
Indirizzi per estratti:
Indirizzo: Chamberlain, AR Univ Calif Irvine, Dept Chem, Irvine, CA 92697 USA Univ Calif Irvine Irvine CA USA 92697 rvine, CA 92697 USA
Citazione:
J.B. Aggen et al., "The design, synthesis, and biological evaluation of analogues of the serine-threonine protein phosphatase 1 and 2A selective inhibitor microcystin LA: Rational modifications imparting PP1 selectivity", BIO MED CH, 7(3), 1999, pp. 543-564

Abstract

Based on the results from previously reported molecular modeling analyses of the interactions between the inhibitor microcystin and the serine-threonine protein phosphatases 1 and 2A, we have designed analogues of microcystin LA with structural modifications intended to impart PP1 selectivity. The synthesis of several first generation analogues followed by inhibition assays revealed that all three are PP1-selective, as predicted. Although the observed selectivities are modest, one of the designed analogues is more selective for PP1 than any known small molecule inhibitor. (C) 1999 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 21:59:20