Development of a biochemical and biophysical suite for integral membrane protein targets: A review

被引:9
|
作者
Haffke, Matthias [1 ,2 ]
Duckely, Myriam [1 ]
Bergsdorf, Christian [1 ]
Jaakola, Veli-Pekka [3 ]
Shrestha, Binesh [1 ]
机构
[1] Novartis Pharma AG, Novartis Inst BioMed Res, Chem Biol & Therapeut, Novartis Campus, CH-4002 Basel, Switzerland
[2] Novartis Pharma AG, Novartis Inst BioMed Res, Global Discovery Chem, Novartis Campus, CH-4002 Basel, Switzerland
[3] Confo Therapeut, Technol Pk 94, B-9052 Zwijnaarde, Belgium
关键词
Integral membrane proteins; G protein coupled receptors; GPCR; Mammalian cells; Insect cells; Expression; SIZE-EXCLUSION CHROMATOGRAPHY; RADIOLIGAND BINDING; LIGHT-SCATTERING; MAMMALIAN-CELLS; CRYSTALLIZATION; EXPRESSION; RECEPTOR; ASSAY; OVEREXPRESSION; PURIFICATION;
D O I
10.1016/j.pep.2019.105545
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The generation of integral membrane proteins (IMPs) in heterologous systems and their characterization remains a major challenge in biomedical research. Significant efforts have been invested both in academia and in the pharmaceutical industry to establish technologies for the expression, isolation and characterization of IMPs. Here we summarize some of the key aspects, which are important to support structure-based drug design (SBDD) in drug discovery projects. We furthermore include timeline estimates and an overview of the target selection and biophysical screening approaches.
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收藏
页数:7
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