Expanding the range of 'druggable' targets with natural product-based libraries: an academic perspective

被引：124

作者：

Bauer, Renato A. ^{[1
]}

Wurst, Jacqueline M. ^{[1
]}

Tan, Derek S. ^{[1
,2
,3
]}

机构：

[1] Mem Sloan Kettering Canc Ctr, Tri Inst Training Program Chem Biol, New York, NY 10065 USA

[2] Mem Sloan Kettering Canc Ctr, Mol Pharmacol & Chem Program, New York, NY 10065 USA

[3] Mem Sloan Kettering Canc Ctr, Tri Inst Res Program, New York, NY 10065 USA

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 2010年 / 14卷 / 03期

关键词：

DIVERSITY-ORIENTED SYNTHESIS; SPLICING FACTOR SF3B; ATROP-ABYSSOMICIN-C; DRUG DISCOVERY; SCREENING LIBRARIES; SMALL-MOLECULE; PHYSICOCHEMICAL PROPERTIES; CANCER; TRANSCRIPTION; INHIBITOR;

D O I：

10.1016/j.cbpa.2010.02.001

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：

Existing drugs address a relatively narrow range of biological targets. As a result, libraries of drug-like molecules have proven ineffective against a variety of challenging targets, such as protein-protein interactions, nucleic acid complexes, and antibacterial modalities. In contrast, natural products are known to be effective at modulating such targets, and new libraries are being developed based on underrepresented scaffolds and regions of chemical space associated with natural products. This has led to several recent successes in identifying new chemical probes that address these challenging targets.

引用

页码：308 / 314

页数：7