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Titolo:
STRUCTURAL-ANALYSIS OF RICIN AND IMPLICATIONS FOR INHIBITOR DESIGN
Autore:
ROBERTUS JD; YAN XJ; ERNST S; MONZINGO A; WORLEY S; DAY P; HOLLIS T; SVINTH M;
Indirizzi:
UNIV TEXAS,DEPT CHEM & BIOCHEM AUSTIN TX 78712
Titolo Testata:
Toxicon
fascicolo: 11-12, volume: 34, anno: 1996,
pagine: 1325 - 1334
SICI:
0041-0101(1996)34:11-12<1325:SORAIF>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
TOXIN-A CHAIN; 3-DIMENSIONAL STRUCTURE; ENZYMATIC INACTIVATION; GLUTAMIC ACID-177; AMP NUCLEOSIDASE; ACTIVE-SITE; PROTEIN; RIBOSOMES; 2.5-A; MUTAGENESIS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
J.D. Robertus et al., "STRUCTURAL-ANALYSIS OF RICIN AND IMPLICATIONS FOR INHIBITOR DESIGN", Toxicon, 34(11-12), 1996, pp. 1325-1334

Abstract

Ricin is a potent cytotoxin with experimental and clinical uses; it has also been used as a poison. There is considerable interest in identifying or designing inhibitors of the toxin that could be administeredas antidotes. The X-ray structure of ricin A-chain is known and a plausible mechanism of action has been proposed. This provides a structural and chemical framework around which inhibitors could be designed; such a structure-based project is underway. Computer programs such as DOCK, GRID, SYBYL, and CHEMX have been used to map the ricin A-chain binding site and to search for potential inhibitors. Inhibitor candidates can be assayed kinetically in a protein synthesis assay and binding can be observed crystallographically. Taken together, a workable search algorithm has been developed and initial tests indicate that at least one ricin A-chain inhibitor, pteroic acid, has been identified. Copyright (C) 1996 Elsevier Science Ltd

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Documento generato il 18/09/20 alle ore 17:19:59