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Titolo:
Development of a synthetic cyclized peptide derived from alpha-fetoproteinthat prevents the growth of human breast cancer
Autore:
Mesfin, FB; Andersen, TT; Jacobson, HI; Zhu, S; Bennett, JA;
Indirizzi:
Albany Med Coll, Ctr Cardiovasc Sci, Albany, NY 12208 USA Albany Med CollAlbany NY USA 12208 Cardiovasc Sci, Albany, NY 12208 USA Albany Med Coll, Ctr Immunol & Microbial Dis, Albany, NY 12208 USA Albany Med Coll Albany NY USA 12208 & Microbial Dis, Albany, NY 12208 USA Albany Med Ctr, Ctr Canc, Albany, NY USA Albany Med Ctr Albany NY USAAlbany Med Ctr, Ctr Canc, Albany, NY USA
Titolo Testata:
JOURNAL OF PEPTIDE RESEARCH
fascicolo: 3, volume: 58, anno: 2001,
pagine: 246 - 256
SICI:
1397-002X(200109)58:3<246:DOASCP>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
SOLID-PHASE SYNTHESIS; ALZHEIMERS-DISEASE; 6-AMINOQUINOLYL-N-HYDROXYSUCCINIMIDYL CARBAMATE; BETA-A4 PEPTIDES; AMINO-ACIDS; AGGREGATION; ESTRADIOL; ESTROGEN; SECONDARY; STABILITY;
Keywords:
alpha-fetoprotein; antibreast cancer peptides; anti-estrogens; cyclic peptide;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
Recensione:
Indirizzi per estratti:
Indirizzo: Andersen, TT Albany Med Coll, Ctr Cardiovasc Sci, Mail Code 8,47 New Scotland Ave, Albany, NY 12208 USA Albany Med Coll Mail Code 8,47 New Scotland Ave Albany NY USA 12208
Citazione:
F.B. Mesfin et al., "Development of a synthetic cyclized peptide derived from alpha-fetoproteinthat prevents the growth of human breast cancer", J PEPT RES, 58(3), 2001, pp. 246-256

Abstract

The peptide, EMTPVNPG, derived from alpha-fetoprotein, inhibits estrogen-stimulated growth of immature mouse uterus and estrogen-dependent proliferation of human breast cancer cells. However, the biological activities of thepeptide diminish over time in storage, even when in the lyophilized state,probably because of peptide aggregation through hydrophobic interaction among monomers. Two analogs of EMTPVNPG were designed with the intent of minimizing aggregation and retaining biological activity during prolonged storage. EMTOVNOG, where O is 4-hydroxyproline, is a linear peptide generated bysubstituting 4-hydroxyproline for the two prolines, thereby increasing peptide hydrophilicity. This analog exhibited a dose-dependent inhibition of estrogen-stimulated growth of immature mouse uterus similar to that of EMTPVNPG (maximal activity at 1 mug/mouse). A second analog, cyclo-(EMTOVNOGQ), a hydrophilic, cyclic analog with increased conformational constraint, was as potent as the other peptides in its inhibition of estrogen-dependent growth of immature mouse uterus, and had an expanded effective dose range. Both linear and cyclized hydroxyproline-substituted analogs exhibited indefinite shelf-life. Furthermore, both analogs inhibited the estrogen-dependent growth of MCF-7 human breast cancer growing as a xenograft in SCID mice. These analogs may become significant, novel agents for the treatment of breastcancer.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/11/20 alle ore 09:01:17