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Titolo:
Ribose modified nucleosides and nucleotides as ligands for purine receptors
Autore:
Jacobson, KA; Ravi, RG; Nandanan, E; Kim, HS; Moro, S; Kim, YC; Lee, K; Barak, D; Marquez, VE; Ji, XD;
Indirizzi:
NIDDK, Mol Recognit Sect, LBC, NIH, Bethesda, MD 20902 USA NIDDK BethesdaMD USA 20902 cognit Sect, LBC, NIH, Bethesda, MD 20902 USA NCI, Med Chem Lab, Frederick, MD 21701 USA NCI Frederick MD USA 21701NCI, Med Chem Lab, Frederick, MD 21701 USA
Titolo Testata:
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
fascicolo: 4-7, volume: 20, anno: 2001,
pagine: 333 - 341
SICI:
1525-7770(2001)20:4-7<333:RMNANA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-COUPLED RECEPTORS; HUMAN P2Y(1) RECEPTOR; BIOLOGICAL-ACTIVITY; ANTAGONISTS; DERIVATIVES; AGONISTS; ANALOGS; POTENT; MUTAGENESIS; RECOGNITION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Jacobson, KA NIDDK, Mol Recognit Sect, LBC, NIH, Bethesda, MD 20902 USA NIDDK Bethesda MD USA 20902 LBC, NIH, Bethesda, MD 20902 USA
Citazione:
K.A. Jacobson et al., "Ribose modified nucleosides and nucleotides as ligands for purine receptors", NUCLEOS NUC, 20(4-7), 2001, pp. 333-341

Abstract

Molecular modeling of receptors for adenosine and nucleotide (P2) receptors with docked ligand, based on mutagenesis, was carried out. Adenosine 3',5'-bisphosphate derivatives act as selective P2Y(1) antagonists/partial agonists. The ribose moiety was replaced with carbocyclics, smaller and larger rings, conformationally constrained rings, and acyclics, producing compounds that retained receptor affinity. Conformational constraints were built into the ribose rings of nucleoside and nucleotide ligands using the methanocarba approach, i.e. fused cyclopropane and cyclopentane rings in place of ribose, suggesting a preference for the Northern (N) conformation among ligands for P2Y(1) and A(1) and A(3)ARs.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/01/20 alle ore 10:15:29