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Titolo:
Enzyme-controlling medicines: Introduction
Autore:
Okamoto, S; Hijikata-Okunomiya, A; Wanaka, K; Okada, Y; Okamoto, U;
Indirizzi:
Kobeanes Projects Thrombosis & Haemostasis, Tarumi Ku, Kobe, Hyogo 655, Jap Kobe Res Projects Thrombosis & Haemostasis Kobe Hyogo Japan 655 655, Jap Kobe Univ, Sch Med, Fac Hlth Sci, Suma Ku, Kobe, Hyogo 65121, Japan Kobe Univ Kobe Hyogo Japan 65121 h Sci, Suma Ku, Kobe, Hyogo 65121, Japan Kobe Gakuin Univ, Fac Pharmaceut Sci, Nishi Ku, Kobe, Hyogo 65121, Japan Kobe Gakuin Univ Kobe Hyogo Japan 65121 ishi Ku, Kobe, Hyogo 65121, Japan
Titolo Testata:
SEMINARS IN THROMBOSIS AND HEMOSTASIS
fascicolo: 6, volume: 23, anno: 1997,
pagine: 493 - 501
SICI:
0094-6176(1997)23:6<493:EMI>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
SYNTHETIC SELECTIVE INHIBITORS; CENTER-DIRECTED PLASMIN; THROMBIN INHIBITOR; TRANEXAMIC ACID; KALLIKREIN; BINDING; COAGULATION; ARGATROBAN; ARTHRITIS;
Keywords:
thrombin inhibitors; plasmin inhibitors; argatroban; epsilon aminocaproic acid (EACA); tranexamic acid (t-AMCHA);
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Okamoto, S KobeKobe,Projects Thrombosis & Haemostasis, Tarumi Ku, 3-15-18 Asahigaoka, Kobe Res Projects Thrombosis & Haemostasis 3-15-18 Asahigaoka Kobe Hyogo Japan 655
Citazione:
S. Okamoto et al., "Enzyme-controlling medicines: Introduction", SEM THROMB, 23(6), 1997, pp. 493-501

Abstract

A short history of the research work of S, Okamoto and co-workers, for theprevious 50 years, is briefly described. In the 1950s, when the physiologic role of fibrinolysis had not been established, they began to seek for compounds that inhibit the action of plasmin, They examined approximately 200 lysine derivatives and discovered epsilon aminocaproic acid (EACA) and tranexamic acid (t-AMCHA),In the 1970s, we selected thrombin as the target enzyme to be controlled; structure-activity relationship studies, taking arginine as the skeleton structure, led to the discovery of the selective thrombin inhibitor No. 205 (4-ethyl-1-[N-2-(5-dimethylamino-1-naphthalenesulfonyl)-L-arginyl]-1-piperidine), and further attempts to minimize the toxicity finally led to No. 805 (argatroban, MD-805, (2R,4R)-4-methyl-1-(N-2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)-sulfonyl]-L-arginyl)-2-piperidine carboxylic acid). Argatroban, without any cofactor, inhibits thrombin competitively. The high selectivity of the action of argatroban is promising for treating thrombosis in clinical practice. More recently, taking advantage of our knowledge obtained through previous studies, active center-directed plasmin inhibitors and a selective inhibitor of kallikrein have been found.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 13:43:00