Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor

被引：107

作者：

Juteau, HN ^{[1
]}

Gareau, Y ^{[1
]}

Labelle, M ^{[1
]}

Sturino, CF ^{[1
]}

Sawyer, N ^{[1
]}

Tremblay, N ^{[1
]}

Lamontagne, S ^{[1
]}

Carrière, MC ^{[1
]}

Denis, D ^{[1
]}

Metters, KM ^{[1
]}

机构：

[1] Merck Frosst Canada & Co, Pointe Claire, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 08期

关键词：

D O I：

10.1016/S0968-0896(01)00110-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Potent and selective antagonists of the human EP3 receptor have been identified. The structure-activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K-i values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP3 receptor was also investigated. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1977 / 1984

页数：8

共 23 条

[1]

The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs [J].

Abramovitz, M ;

Adam, M ;

Boie, Y ;

Carrière, MC ;

Denis, D ;

Godbout, C ;

Lamontagne, S ;

Rochette, C ;

Sawyer, N ;

Tremblay, NM ;

Belley, M ;

Gallant, M ;

Dufresne, C ;

Gareau, Y ;

Ruel, R ;

Juteau, H ;

Labelle, M ;

Ouimet, N ;

Metters, KM .

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS, 2000, 1483 (02) :285-293

[2]

ABRAMOVITZ M, 1994, J BIOL CHEM, V269, P2632

[3]

CLONING AND EXPRESSION OF 3 ISOFORMS OF THE HUMAN EP(3) PROSTANOID RECEPTOR [J].

ADAM, M ;

BOIE, Y ;

RUSHMORE, TH ;

MULLER, G ;

BASTIEN, L ;

MCKEE, KT ;

METTERS, KM ;

ABRAMOVITZ, M .

FEBS LETTERS, 1994, 338 (02) :170-174

[4]

SUBSTITUENT EFFECTS .8. SYNTHESIS OF SUBSTITUTED ALPHA- AND BETA-FLUORONAPHTHALENS [J].

ADCOCK, W ;

DEWAR, MJS .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1967, 89 (02) :386-&

[5]

[Anonymous], J ORG CHEM

[6]

BASTIEN L, 1994, J BIOL CHEM, V269, P11873

[7]

MOLECULAR-CLONING AND CHARACTERIZATION OF THE HUMAN PROSTANOID DP RECEPTOR [J].

BOIE, Y ;

SAWYER, N ;

SLIPETZ, DM ;

METTERS, KM ;

ABRAMOVITZ, M .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1995, 270 (32) :18910-18916

[8]

BOIE Y, 1994, J BIOL CHEM, V269, P12173

[9]

COLEMAN RA, 1994, PHARMACOL REV, V46, P205

[10]

ANTIHYPERGLYCEMIC ACTIVITY OF NOVEL NAPHTHALENYL 3H-1,2,3,5-OXATHIADIAZOLE 2-OXIDES [J].

ELLINGBOE, JW ;

LOMBARDO, LJ ;

ALESSI, TR ;

NGUYEN, TT ;

GUZZO, F ;

GUINOSSO, CJ ;

BULLINGTON, J ;

BROWNE, ENC ;

BAGLI, JF ;

WRENN, J ;

STEINER, K ;

MCCALEB, ML .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (17) :2485-2493

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