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Open AccessArticle

Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401

1
Key Laboratory of Traditional Chinese Medicine Research and Development of Hebei Province, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde 067000, China
2
Department of Human Anatomy, Chengde Medical University, Chengde 067000, China
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(13), 2394; https://doi.org/10.3390/molecules24132394
Received: 1 May 2019 / Revised: 23 June 2019 / Accepted: 28 June 2019 / Published: 28 June 2019
(This article belongs to the Special Issue Probes for Detection, Sensing and Imaging)
To explore the molecular mechanisms of BAY R3401, four types of novel photoaffinity probes bearing different secondary tags were synthesized. Their potency for glycogenolysis was evaluated in primary human liver HL-7702 cells and HepG2 cells. Probe 2d showed the best activity in primary human liver HL-7702 cells and HepG2 cells, with IC50 values of 4.45 μM and 28.49 μM, respectively. Likewise, probe 5d showed IC50 values of 6.46 μM in primary human liver HL-7702 cells and 15.29 μM in HepG2 cells, respectively. Photoaffinity labeling experiments were also performed and protein bands larger than 170 kDa were specifically tagged by probe 2d. The results suggest that the synthesized probe 2d might be a very promising tool for the isolation of the target proteins of BAY R3401. View Full-Text
Keywords: BAY R3401; molecular mechanism; type 2 diabetes; photoaffinity probe; glycogenolysis; photoaffinity labeling; target proteins BAY R3401; molecular mechanism; type 2 diabetes; photoaffinity probe; glycogenolysis; photoaffinity labeling; target proteins
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MDPI and ACS Style

Zhang, L.; Yan, Z.; Wang, Y.; Song, C.; Miao, G. Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401. Molecules 2019, 24, 2394. https://doi.org/10.3390/molecules24132394

AMA Style

Zhang L, Yan Z, Wang Y, Song C, Miao G. Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401. Molecules. 2019; 24(13):2394. https://doi.org/10.3390/molecules24132394

Chicago/Turabian Style

Zhang, Liying; Yan, Zhiwei; Wang, Youde; Song, Chengjun; Miao, Guangxin. 2019. "Design, Synthesis, and Biological Application of Novel Photoaffinity Probes of Dihydropyridine Derivatives, BAY R3401" Molecules 24, no. 13: 2394. https://doi.org/10.3390/molecules24132394

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