Serendipity in discovery of proteasome inhibitors

被引：4

作者：

Dunn, Derek ^{[1
]}

Iqbal, Mohamed ^{[1
]}

Husten, Jean ^{[1
]}

Ator, Mark A. ^{[1
]}

Chatterjee, Sankar ^{[1
]}

机构：

[1] Cephalon Inc, W Chester, PA 19380 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 10期

关键词：

Proteasome; Peptidomimetic; Cancer; 20S PROTEASOME; PROTEOLYTIC PATHWAY; CANCER; POTENT; EXPRESSION; BORTEZOMIB; RESOLUTION; APOPTOSIS; SYSTEM;

D O I：

10.1016/j.bmcl.2012.03.086

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Among its various catalytic activities, the 'chymotrypsin-like' activity of the proteasome, a large multicatalytic proteinase complex has emerged as the focus of drug discovery efforts in cancer therapy. Herein, a series of first generation (2S, 3R)-2-amino-3-hydroxybutyric acid derived proteasome inhibitors that were discovered serendipitously en route to original goal of generating a series of sterically constrained oxazoline derivatives has been reported. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3503 / 3505

页数：3

共 29 条

[1] Involvement of the ubiquitin-proteasome pathway and molecular chaperones in oculopharyngeal muscular dystrophy
Abu-Baker, A
Messaed, C
Laganiere, J
Gaspar, C
Brais, B
Rouleau, GA
[J]. HUMAN MOLECULAR GENETICS, 2003, 12 (20) : 2609 - 2623
[2] Novel dipeptidyl proteasome inhibitors overcome Bcl-2 protective function and selectively accumulate the cyclin-dependent kinase inhibitor p27 and induce apoptosis in transformed, but not normal, human fibroblasts
An, B
Goldfarb, RH
Siman, R
Dou, QP
[J]. CELL DEATH AND DIFFERENTIATION, 1998, 5 (12) : 1062 - 1075
[3] [Anonymous], 2011, U.S. Patent, Patent No. [7,915,236, 7915236]
[4] Adaptation of the ubiquitin-proteasome proteolytic pathway in cancer cachexia
Attaix, D
Combaret, L
Tilignac, T
Taillandier, D
[J]. MOLECULAR BIOLOGY REPORTS, 1999, 26 (1-2) : 77 - 82
[5] 20S proteasome and its inhibitors: Crystallographic knowledge for drug development
Borissenko, Ljudmila
Groll, Michael
[J]. CHEMICAL REVIEWS, 2007, 107 (03) : 687 - 717
[6] P′-extended α-ketoamide inhibitors of proteasome
Chattejee, S
Dunn, D
Mallya, S
Ator, MA
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (17) : 2603 - 2606
[7] Proteasomal processing of nuclear autoantigens in systemic autoimmunity
Chen, M
von Mikecz, A
[J]. AUTOIMMUNITY REVIEWS, 2005, 4 (03) : 117 - 122
[8] Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer
Dorsey, Bruce D.
Iqbal, Mohamed
Chatterjee, Sankar
Menta, Ernesto
Bernardini, Raffaella
Bernareggi, Alberto
Cassara, Paolo G.
D'Arasmo, Germano
Ferretti, Edmondo
De Munari, Sergio
Oliva, Ambrogio
Pezzoni, Gabriella
Allievi, Cecilia
Strepponi, Ivan
Ruggeri, Bruce
Ator, Mark A.
Williams, Michael
MallamoT, John P.
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (04) : 1068 - 1072
[9] An alternative synthesis of peptidyl α-keto-2-oxazolines
Dunn, D
Chatterjee, S
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (10) : 1273 - 1276
[10] Structure of 20S proteasome from yeast at 2.4 angstrom resolution
Groll, M
Ditzel, L
Lowe, J
Stock, D
Bochtler, M
Bartunik, HD
Huber, R
[J]. NATURE, 1997, 386 (6624) : 463 - 471

← 1 2 3 →