A new structural class of selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome

被引：29

作者：

Garcia-Echeverría, C ^{[1
]}

Imbach, P

France, D

Fürst, P

Lang, M

Noorani, M

Scholz, D

Zimmermann, J

Furet, P

机构：

[1] Novartis Pharma Inc, Oncol Res, CH-4002 Basel, Switzerland

[2] Novartis Pharma Inc, Oncol Res, Summit, NJ 07901 USA

[3] Novartis Res Inst, A-1235 Vienna, Austria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)00205-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe the identification and in vitro characterization of a series of 2-aminobenzylstatine derivatives that inhibit non-covalently the chymotrypsin-like activity of the 20S proteasome. Our initial SAR data demonstrate that the 2-aminobenzylstatine core structure can effectively serve as the basis for designing potent, selective and non-covalent inhibitors of the chymotrypsin-like activity of the 20S proteasome. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1317 / 1319

页数：3

共 22 条

[1]

Adams J, 1999, CANCER RES, V59, P2615

[2] Proteasome inhibition: a new strategy in cancer treatment [J].

Adams, J ;

Palombella, VJ ;

Elliott, PJ .

INVESTIGATIONAL NEW DRUGS, 2000, 18 (02) :109-121

[3] An inhibitor of HIV-1 protease modulates proteasome activity, antigen presentation, and T cell responses [J].

André, P ;

Groettrup, M ;

Klenerman, P ;

de Giuli, R ;

Booth, BL ;

Cerundolo, V ;

Bonneville, M ;

Jotereau, F ;

Zinkernagel, RM ;

Lotteau, V .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1998, 95 (22) :13120-13124

[4]

Andre P., 1999, PCT Int. Appl., Patent No. [WO 99 63998, 9963998]

[5]

BILLICH A, 1995, ANTIVIR CHEM CHEMOTH, V6, P327, DOI 10.1177/095632029500600507

[6] Proteasome inhibitors as potential novel anticancer agents [J].

Dou, QP ;

Li, BY .

DRUG RESISTANCE UPDATES, 1999, 2 (04) :215-223

[7] Pharmacological proteasome inhibitors and their therapeutic potential [J].

Dou, QP ;

Nam, S .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2000, 10 (08) :1263-1272

[8]

Elliot P J, 1999, Curr Opin Drug Discov Devel, V2, P484

[9] Modeling of the binding mode of a non-covalent inhibitor of the 20S proteasome.: Application to structure-based analogue design [J].

Furet, P ;

Imbach, P ;

Fürst, P ;

Lang, M ;

Noorani, M ;

Zimmermann, J ;

Garcia-Echeverría, C .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (10) :1321-1324

[10]

Goldberg AL, 1997, BIOL CHEM, V378, P131

← 1 2 3 →