Target identification and validation of natural products with label-free methodology: A critical review from 2005 to 2020

Dai，Lingyun1,2,3; Li，Zhijie1,2; Chen，Dan3; Jia，Lin4; Guo，Jinan1; Zhao，Tianyun3; Nordlund，Pär3,5

2020-12-01

10.1016/j.pharmthera.2020.107690

PHARMACOLOGY & THERAPEUTICS   影响因子和分区

0163-7258

Natural products (NPs) have been an important source of therapeutic drugs in clinic use and contributed many chemical probes for research. The usefulness of NPs is however often marred by the incomplete understanding of their direct cellular targets. A number of experimental methods for drug target identification have been developed over the years. One class of methods, termed "label-free" methodology, exploits the energetic and biophysical features accompanying the association of macromolecules with drugs and other compounds in their native forms. Herein we review the working principles, assay implementations, and key applications of the most important approaches, and also give examples where they have been applied to NPs. We also assess the key advantages and limitations of each method. Furthermore, we address when and how the label-free methodology can be particularly useful considering some of the unique features of NP chemistry and bioactivation. (C) 2020 Published by Elsevier Inc.

Natural product Target identification Target validation Label-free methodology Mechanism of action

SCI

英语

第一 ; 通讯

National Natural Science Foundation of China[81902787]

Pharmacology & Pharmacy

Pharmacology & Pharmacy

WOS:000594690000010

PERGAMON-ELSEVIER SCIENCE LTD

Web of Science

1.Department of Urology,Shenzhen People's Hospital (The Second Clinical Medical College,Jinan University,The First Affiliated Hospital,Southern University of Science and Technology),Shenzhen Urology Minimally Invasive Engineering Center,Shenzhen,518020,China
2.Department of Geriatrics,Shenzhen People's Hospital (The Second Clinical Medical College,Jinan University,The First Affiliated Hospital,Southern University of Science and Technology),Shenzhen,518020,China
3.Institute of Molecular and Cell Biology,A*STAR,Singapore,138673,Singapore
4.School of Biomedical Sciences,Li Ka Shing Faculty of Medicine,The University of Hong Kong,Hong Kong,999077,Hong Kong
5.Department of Oncology and Pathology,Karolinska Institutet,Stockholm,171 77,Sweden

Dai，Lingyun,Li，Zhijie,Chen，Dan,et al. Target identification and validation of natural products with label-free methodology: A critical review from 2005 to 2020[J]. PHARMACOLOGY & THERAPEUTICS,2020,216.

Dai，Lingyun.,Li，Zhijie.,Chen，Dan.,Jia，Lin.,Guo，Jinan.,...&Nordlund，Pär.(2020).Target identification and validation of natural products with label-free methodology: A critical review from 2005 to 2020.PHARMACOLOGY & THERAPEUTICS,216.

Dai，Lingyun,et al."Target identification and validation of natural products with label-free methodology: A critical review from 2005 to 2020".PHARMACOLOGY & THERAPEUTICS 216(2020).