Affinity-based protein profiling-driven discovery of myricanol as a Nampt activator

doi:10.1016/j.bioorg.2023.106435

UM > Faculty of Health Sciences > DEPARTMENT OF PHARMACEUTICAL SCIENCES

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	Affinity-based protein profiling-driven discovery of myricanol as a Nampt activator
	Lyu, Peng 1; Li, Shengrong 2; Han, Ying 3; Shen, Shengnan 1; Feng, Zheling 1; Hao, Piliang 3; Li, Zhengqiu 2; Lin, Ligen1
	2023-04-01
Source Publication	Bioorganic Chemistry
ISSN	0045-2068
Volume	133
Abstract	Herein, we synthesized an affinity-based probe of myricanol (pMY) with a photo-affinity cross-linker to initiate a bioconjugation reaction, which was applied for target identification in live C2C12 myotubes. Pull-down of biotinylated pMY coupled with mass spectroscopy and Western blotting revealed that pMY can bind with nicotinamide phosphoribosyltransferase (Nampt), a rate-limiting enzyme in the nicotinamide adenine dinucleotide salvage pathway. Cellular thermal shift assay, drug affinity responsive target stability assay and recombinant protein labeling further validated the direct interaction between myricanol and Nampt. Myricanol did not affect the protein expression of Nampt, but enhanced its activity. Knock-down of Nampt totally abolished the promoting effect of myricanol on insulin-stimulated glucose uptake in C2C12 myotubes. Taken together, myricanol sensitizes insulin action in myotubes through binding with and activating Nampt.
Keyword	Activity-based protein profiling Myotubes Myricanol Nampt Photo-affinity probe
DOI	10.1016/j.bioorg.2023.106435
URL	View the original
Language	英語English
Scopus ID	2-s2.0-85149020185
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	DEPARTMENT OF PHARMACEUTICAL SCIENCES Institute of Chinese Medical Sciences
Affiliation	1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau, 999078, China 2.International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development (MOE), MOE Key Laboratory of Tumor Molecular Biology, School of Pharmacy, Jinan University, Guangzhou, 510632, China 3.School of Life Science and Technology, ShanghaiTech University, Shanghai, 393 Middle Huaxia Road, 201210, China
First Author Affilication	Institute of Chinese Medical Sciences
Recommended Citation GB/T 7714	Lyu, Peng,Li, Shengrong,Han, Ying,et al. Affinity-based protein profiling-driven discovery of myricanol as a Nampt activator[J]. Bioorganic Chemistry, 2023, 133.
APA	Lyu, Peng., Li, Shengrong., Han, Ying., Shen, Shengnan., Feng, Zheling., Hao, Piliang., Li, Zhengqiu., & Lin, Ligen (2023). Affinity-based protein profiling-driven discovery of myricanol as a Nampt activator. Bioorganic Chemistry, 133.
MLA	Lyu, Peng,et al."Affinity-based protein profiling-driven discovery of myricanol as a Nampt activator".Bioorganic Chemistry 133(2023).

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