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Titolo:
Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: The importance of the peptide backbone
Autore:
Fukumizu, A; Tsuda, Y; Wanaka, K; Tada, M; Okamoto, S; Hijikata-Okunomiya, A; Okada, Y;
Indirizzi:
Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 6512180, JapanKobe Gakuin Univ Kobe Hyogo Japan 6512180 Ku, Kobe, Hyogo 6512180, Japan Kobe Res Project Thrombosis & Haemostasis, Tarumi Ku, Kobe, Hyogo 6550033,Japan Kobe Res Project Thrombosis & Haemostasis Kobe Hyogo Japan 6550033 ,Japan Kobe Univ, Sch Med, Fac Hlth Sci, Suma Ku, Kobe, Hyogo 6540142, Japan KobeUniv Kobe Hyogo Japan 6540142 i, Suma Ku, Kobe, Hyogo 6540142, Japan
Titolo Testata:
CHEMICAL & PHARMACEUTICAL BULLETIN
fascicolo: 8, volume: 47, anno: 1999,
pagine: 1141 - 1144
SICI:
0009-2363(199908)47:8<1141:AAAPLS>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVATION; DESIGN;
Keywords:
plasma kallikrein inhibitor; pseudo-peptide bond; psi(CH2-NH); synthesis; biological activity;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
19
Recensione:
Indirizzi per estratti:
Indirizzo: Okada, Y Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 6512180, Japan Kobe Gakuin Univ Kobe Hyogo Japan 6512180 , Hyogo 6512180, Japan
Citazione:
A. Fukumizu et al., "Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: The importance of the peptide backbone", CHEM PHARM, 47(8), 1999, pp. 1141-1144

Abstract

Pseudo-peptide analogs of trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-4-aminophenyl acetic acid (PKSI-527, plasma kallikrein selective inhibitor), in which an amide bond (peptide bond) has been replaced by a CH2-NHbond, ie, trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-psi(CH2-NH)-4-aminophenyl acetic acid (I), trans-4-aminomethylcyclohexanecarbonyl-psi(CH2-NH)-L-phenylalanyl-4-aminophenyl acetic acid (II) and trans-4-aminomethylcyclohexanecarbonyl-D-phenylalanyl-psi(CH2-NH)-4-aminophenyl acetic acid(III) were synthesized, These pseudo-peptide analogs did not exhibit any detectable inhibitory activity against plasma kallikrein (PK), plasmin (PL),urokinase (UK), thrombine (TH) or trypsin (TRY), These results indicate that both carbonyl groups in the PKSI-527 are important for the manifestationof potent inhibitory activity against plasma kallikrein.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 01/10/20 alle ore 00:29:58