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Titolo:
Cantharimides: A new class of modified cantharidin analogues inhibiting protein phosphatases 1 and 2A
Autore:
McCluskey, A; Walkom, C; Bowyer, MC; Ackland, SP; Gardiner, E; Sakoff, JA;
Indirizzi:
Univ Newcastle, Med Chem Grp, Sch Biol & Chem Sci, Callaghan, NSW 2308, Australia Univ Newcastle Callaghan NSW Australia 2308 allaghan, NSW 2308, Australia Univ Newcastle, Sch Sci & Technol, Callaghan, NSW 2308, Australia Univ Newcastle Callaghan NSW Australia 2308 allaghan, NSW 2308, Australia Newcastle Mater Misericordiae Hosp, Dept Med Oncol, Newcastle, NSW 2298, Australia Newcastle Mater Misericordiae Hosp Newcastle NSW Australia 2298 Australia
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 22, volume: 11, anno: 2001,
pagine: 2941 - 2946
SICI:
0960-894X(20011119)11:22<2941:CANCOM>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
SER-THR PHOSPHATASES; PP1; PP2A; DERIVATIVES; DESIGN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: McCluskey, A Univ Newcastle, Med Chem Grp, Sch Biol & Chem Sci, Callaghan,NSW 2308, Australia Univ Newcastle Callaghan NSW Australia 2308 2308, Australia
Citazione:
A. McCluskey et al., "Cantharimides: A new class of modified cantharidin analogues inhibiting protein phosphatases 1 and 2A", BIOORG MED, 11(22), 2001, pp. 2941-2946

Abstract

Cantharidin and its analogues have been of considerable interest as potentinhibitors of the serine/threonine protein phosphatases 1 and 2A (PP1 and PP2A). However, limited modifications to the parent compounds is tolerated. As part of an ongoing study we have developed a new series of cantharidin analogues, the cantharimides. Inhibition studies indicate that cantharimides possessing a D- or L-histidine, are more potent inhibitors of PP1 and PP2A (PP1 IC50 = 3.22 +/- 0.7 muM; PP2A IC50 = 0.81 +/- 0.1 muM and PP1 IC50 =2.82 +/- 0.6 muM; PP2A IC50 = 1.35 +/- 0.3 muM, respectively) than norcantharidin (PP1 IC50 = 5.31 +/- 0.76 muM; PP2A IC50 = 2.9 +/- 1.04 muM) and essentially equipotent with cantharidin (PP1 IC50 = 3.6 +/- 0.42 muM; PP2A IC50 = 0.36 +/- 0.08 muM). Cantharimides with non-polar or acidic amino acid residues are only poor inhibitors of PP1 and PP2A. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/06/20 alle ore 01:58:08