Designed calix[8]arene-based ligands for selective tryptase surface recognition

被引：46

作者：

Mecca, T ^{[1
]}

Consoli, GML ^{[1
]}

Geraci, C ^{[1
]}

Cunsolo, F ^{[1
]}

机构：

[1] CNR, Ist Chim Biomol, Sez Catania, I-95028 Valverde, CT, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2004年 / 12卷 / 19期

关键词：

D O I：

10.1016/j.bmc.2004.07.037

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Basic amino acid calix[8]arene receptors for tryptase surface recognition have been synthesized. The tetrameric arrangement and the negative charge distribution close to the active sites of the enzyme, have suggested the design of complementary multifunctional receptors that might bind to the active region of the protein blocking the approach of the substrate. Kinetic inhibition analysis on recombinant lung tryptase have showed a time-dependent competitive inhibition with both initial and steady-state rate constants in the nanomolar range. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5057 / 5062

页数：6

共 34 条

[1] Inactivation of human lung tryptase: Evidence for a re-activatable tetrameric intermediate and active monomers [J].

Addington, AK ;

Johnson, DA .

BIOCHEMISTRY, 1996, 35 (42) :13511-13518

[2] REGULATION OF HUMAN MAST-CELL TRYPTASE - EFFECTS OF ENZYME CONCENTRATION, IONIC-STRENGTH AND THE STRUCTURE AND NEGATIVE CHARGE-DENSITY OF POLYSACCHARIDES [J].

ALTER, SC ;

METCALFE, DD ;

BRADFORD, TR ;

SCHWARTZ, LB .

BIOCHEMICAL JOURNAL, 1987, 248 (03) :821-827

[3] Design of GFB-111, a platelet-derived growth factor binding molecule with antiangiogenic and anticancer activity against human tumors in mice [J].

Blaskovich, MA ;

Lin, Q ;

Delarue, FL ;

Sun, J ;

Park, HS ;

Coppola, D ;

Hamilton, AD ;

Sebti, SM .

NATURE BIOTECHNOLOGY, 2000, 18 (10) :1065-1070

[4] Potent selective nonpeptidic inhibitors of human lung tryptase [J].

Burgess, LE ;

Newhouse, BJ ;

Ibrahim, P ;

Rizzi, J ;

Kashem, MA ;

Hartman, A ;

Brandhuber, BJ ;

Wright, CD ;

Thomson, DS ;

Vigers, GPA ;

Koch, K .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1999, 96 (15) :8348-8352

[5]

Caughey G. H, 1995, MAST CELL PROTEASES

[6] Of mites and men: Trypsin-like proteases in the lungs [J].

Caughey, GH .

AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY, 1997, 16 (06) :621-628

[7]

Clark James M., 1996, Drugs of the Future, V21, P811

[8] TRYPTASE INHIBITORS BLOCK ALLERGEN-INDUCED AIRWAY AND INFLAMMATORY RESPONSES IN ALLERGIC SHEEP [J].

CLARK, JM ;

ABRAHAM, WM ;

FISHMAN, CE ;

FORTEZA, R ;

AHMED, A ;

CORTES, A ;

WARNE, RL ;

MOORE, WR ;

TANAKA, RD .

AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 1995, 152 (06) :2076-2083

[9]

Copeland R. A., 2004, ENZYMES PRACTICAL IN

[10] Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone [J].

Costanzo, MJ ;

Yabut, SC ;

Almond, HR ;

Andrade-Gordon, P ;

Corcoran, TW ;

de Garavilla, L ;

Kauffman, JA ;

Abraham, WM ;

Recacha, R ;

Chattopadhyay, D ;

Maryanoff, BE .

JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (18) :3865-3876

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