Label-free screening assays: a strategy for finding better drug candidates

被引:9
|
作者
Lunn, Charles A. [1 ]
机构
[1] New Lead Discovery Merck Res Labs, Kenilworth, NJ 07033 USA
关键词
SCINTILLATION PROXIMITY ASSAY; HETEROTRIMERIC G-PROTEINS; SMALL-MOLECULE ACTIVATORS; CANNABINOID RECEPTOR; MASS-SPECTROMETRY; FUNCTIONAL SELECTIVITY; ALLOSTERIC MODULATORS; STEM-CELLS; BONE MASS; CB2;
D O I
10.4155/FMC.10.246
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena However, these advances have not led to improvements in drug-discovery success Drug programs must find new ways to identify superior compounds Advances in label-free assay technologies may provide advantages needed for improved drug discovery In this article, we will discuss high-throughput MS, a technology that allows screening with native substrates and with targets inaccessible to standard assay formats We will then discuss cell-based label-free biosensors, focusing on the increased information content available when using these platforms We will conclude with speculation on the future and ways to obtain relevant biological information early in development to ensure the best compounds are promoted to medicinal chemistry campaigns
引用
收藏
页码:1703 / 1716
页数:14
相关论文
共 50 条
  • [1] Advantages and application of label-free detection assays in drug screening
    Cunningham, Brian T.
    Laing, Lance G.
    EXPERT OPINION ON DRUG DISCOVERY, 2008, 3 (08) : 891 - 901
  • [2] The development of label-free cellular assays for drug discovery
    Fang, Ye
    EXPERT OPINION ON DRUG DISCOVERY, 2011, 6 (12) : 1285 - 1298
  • [3] Label-free cell-based assays for GPCR screening
    Fang, Ye
    Frutos, Anthony G.
    Verklereen, Ronald
    COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING, 2008, 11 (05) : 357 - 369
  • [4] Label-Free Cell Phenotypic Assays for Assessing Drug Polypharmacology
    Wang, Jixia
    Zhang, Xiuli
    Fang, Ye
    Liang, Xinmiao
    CURRENT PHARMACEUTICAL DESIGN, 2016, 22 (21) : 3190 - 3200
  • [5] A Label-Free Sensor System for Chemotherapeutic Drug Screening
    van den Driesche, Sander
    Vellekoop, Michael J.
    Iuliano, Filippo
    Breiteneder, Heimo
    Hafner, Christine
    2011 IEEE SENSORS, 2011, : 280 - 283
  • [6] A label-free electrochemical strategy for highly sensitive methyltransferase activity assays
    Zhou, Jiawan
    Zhang, Xiaohua
    Xiong, Erhu
    Yu, Peng
    Chen, Jinhua
    CHEMICAL COMMUNICATIONS, 2015, 51 (24) : 5081 - 5084
  • [7] Troubleshooting and deconvoluting label-free cell phenotypic assays in drug discovery
    Fang, Ye
    JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, 2013, 67 (02) : 69 - 81
  • [8] Label-free assays on the BIND system
    Cunningham, BT
    Li, P
    Schulz, S
    Lin, B
    Baird, C
    Gerstenmaier, J
    Genick, C
    Wang, F
    Fine, E
    Laing, L
    JOURNAL OF BIOMOLECULAR SCREENING, 2004, 9 (06) : 481 - 490
  • [9] ELECTRONIC LABEL-FREE BIOSENSING ASSAYS
    Reed, Mark A.
    2013 IEEE SENSORS, 2013, : 20 - 20
  • [10] Label-free drug interaction screening via Raman microscopy
    Altangerel, Narangerel
    Neuman, Benjamin W.
    Hemmer, Philip R.
    Yakovlev, Vladislav V.
    Rajil, Navid
    Yi, Zhenhuan
    Sokolov, Alexei V.
    Scully, Marlan O.
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2023, 120 (30)