The Role of HTS in Drug Discovery at the University of Michigan

被引：7

作者：

Larsen, Martha J. ^{[1
]}

Larsen, Scott D. ^{[2
]}

Fribley, Andrew ^{[3
]}

Grembecka, Jolanta ^{[4
]}

Homan, Kristoff ^{[5
]}

Mapp, Anna ^{[6
]}

Haak, Andrew ^{[7
]}

Nikolovska-Coleska, Zaneta ^{[8
]}

Stuckey, Jeanne A. ^{[5
,9
]}

Sun, Duxin ^{[10
]}

Sherman, David H. ^{[5
,11
]}

机构：

[1] Univ Michigan, Inst Life Sci, Ctr Chem Genom, Ann Arbor, MI 48109 USA

[2] Univ Michigan, Coll Pharm, Vahlteich Med Chem Core, Ann Arbor, MI 48109 USA

[3] Wayne State Univ, Sch Med, Dept Pediat, Detroit, MI 48201 USA

[4] Univ Michigan, Dept Pathol, Ann Arbor, MI 48109 USA

[5] Univ Michigan, Inst Life Sci, Ann Arbor, MI 48109 USA

[6] Univ Michigan, Inst Life Sci, Dept Chem, Ann Arbor, MI 48109 USA

[7] Univ Michigan, Dept Pharmacol, Ann Arbor, MI 48109 USA

[8] Univ Michigan, Sch Med, Dept Pathol, Ann Arbor, MI 48109 USA

[9] Univ Michigan, Dept Biol Chem, Ann Arbor, MI 48109 USA

[10] Univ Michigan, Coll Pharm, Dept Pharmaceut Sci, Ann Arbor, MI 48109 USA

[11] Univ Michigan, Dept Med Chem, Ann Arbor, MI 48109 USA

来源：

COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING | 2014年 / 17卷 / 03期

关键词：

Drug discovery; high throughput screening; medicinal chemistry; pharmacokinetics; protein crystallography; structural biology; PROTEIN-PROTEIN INTERACTIONS; SMALL-MOLECULE INHIBITOR; TRANSCRIPTION FACTOR-BINDING; MLL FUSION PROTEINS; RECEPTOR KINASE 2; KIX DOMAIN; ER-STRESS; HEART-FAILURE; CANCER; GENE;

D O I：

10.2174/1386207317666140109121546

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

High throughput screening (HTS) is an integral part of a highly collaborative approach to drug discovery at the University of Michigan. The HTS lab is one of four core centers that provide services to identify, produce, screen and follow-up on biomedical targets for faculty. Key features of this system are: protein cloning and purification, protein crystallography, small molecule and siRNA HTS, medicinal chemistry and pharmacokinetics. Therapeutic areas that have been targeted include anti-bacterial, metabolic, neurodegenerative, cardiovascular, anti-cancer and anti-viral. The centers work in a coordinated, interactive environment to affordably provide academic investigators with the technology, informatics and expertise necessary for successful drug discovery. This review provides an overview of these centers at the University of Michigan, along with case examples of successful collaborations with

引用

页码：210 / 230

页数：21

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