Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Hybrid peptides constructed from RES-701-1, an endothelin B receptor antagonist, and endothelin; Binding selectivity for endothelin receptors and their pharmacological activity
Autore:
Shibata, K; Suzawa, T; Ohno, T; Yamada, K; Tanaka, T; Tsukuda, E; Matsuda, Y; Yamasaki, M;
Indirizzi:
Kyowa Hakko Kogyo Co Ltd, Tokyo Res Labs, Machida, Tokyo 1948533, Japan Kyowa Hakko Kogyo Co Ltd Machida Tokyo Japan 1948533 Tokyo 1948533, Japan Kyowaaizumi,Kogyo Co Ltd, Pharmaceut Res Inst, Drug Discovery Res labs, Nag Kyowa Hakko Kogyo Co Ltd Nagaizumi Shizuoka Japan 4118731 y Res labs, Nag
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 12, volume: 6, anno: 1998,
pagine: 2459 - 2467
SICI:
0968-0896(199812)6:12<2459:HPCFRA>2.0.ZU;2-7
Fonte:
ISI
Lingua:
ENG
Soggetto:
STREPTOMYCES SP RE-701; ET(B) RECEPTORS; POTENT; ANALOGS; VASOCONSTRICTOR; IRL-1620; AGONIST; ET(A);
Keywords:
receptors; agonists; antagonists; peptides and polypeptides;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
24
Recensione:
Indirizzi per estratti:
Indirizzo: Yamasaki, M Kyowa Hakko Kogyo Co Ltd, Tokyo Res Labs, 3-6-6 Asahi Machi, Machida, Tokyo Kyowa Hakko Kogyo Co Ltd 3-6-6 Asahi Machi Machida Tokyo Japan 1948533
Citazione:
K. Shibata et al., "Hybrid peptides constructed from RES-701-1, an endothelin B receptor antagonist, and endothelin; Binding selectivity for endothelin receptors and their pharmacological activity", BIO MED CH, 6(12), 1998, pp. 2459-2467

Abstract

Hybrid peptides were constructed from endothelin B receptor (ETB) selective antagonist RES-701-1 (1) and endothelin (ET-1). They have N-terminal 10 amino acids derived from 1 and C-terminal 10 amino acids derived from ET-1. RES-701-1(1-10)-[Ala15]ET-1(12-21) and its analogues substituted or truncated at the residues derived from RES-701-1 had proved to possess high receptor binding activity selective for ETB as well as 1. Substitutions at the residues derived from ET-1 had produced some analogues that possessed high affinity not only for ETB but for ETA. Although all analogues had antagonistic effects on ETA, some analogues had proved to function as agonist on ETB confirmed by the changes in intracellular calcium concentrations of ET receptor-transfected COS-7 cells, We have found four types of ET receptor-binding peptides: (1) ETB-selective agonist with weak ETA antagonism (3, KT7421);(2) ETB-selective antagonist with weak ETA antagonism (29, KT7539); (3) ETB agonist with potent ETA antagonism (27, KT7538); and (4) non-selective ETA/ETB antagonist (26, KT7540). (C) 1998 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/07/20 alle ore 20:24:50