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Titolo:
Structure-inhibitory activity relationship of plasmin and plasma kallikrein inhibitors
Autore:
Tsuda, Y; Tada, M; Wanaka, K; Okamoto, U; Hijikata-Okunomiya, A; Okamoto, S; 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 Gakuin Univ, High Technol Res Ctr, Nishi Ku, Kobe, Hyogo 6512180, Japan Kobe Gakuin Univ Kobe Hyogo Japan 6512180 Ku, Kobe, Hyogo 6512180, Japan Kobe Res Projects Thrombosis & Haemostasis, Tarumi Ku, Kobe, Hyogo 6550033, Japan Kobe Res Projects 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: 11, volume: 49, anno: 2001,
pagine: 1457 - 1463
SICI:
0009-2363(200111)49:11<1457:SAROPA>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVATOR; CELLS;
Keywords:
enzyme-selective inhibitor; plasma kallikrein inhibitor; plasmin inhibitor; structure-inhibitory activity relationship;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
32
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:
Y. Tsuda et al., "Structure-inhibitory activity relationship of plasmin and plasma kallikrein inhibitors", CHEM PHARM, 49(11), 2001, pp. 1457-1463

Abstract

Based on the structure of Tra-Tyr(O-Pic)-octylamide, a portion of the octylamine was replaced with moieties bearing hydrophobic, basic or acidic groups. Replacement of the C-terminal residue with a moiety bearing a hydrophobic group gave the proper affinity of the inhibitor to both plasmin (PL) andplasma kallikrein (PK). While addition of a basic residue did not improve the affinity of the inhibitor, a carboxylic acid attached to the phenyl ring increased the PK selectivity of the inhibitor.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/09/20 alle ore 10:28:29